in vitro PHARMACOLOGY 2011 CATALOG - Cerep

in vitro
pharmacology
2011 catalog

❚ france
[Laboratories]
Le Bois l’Evêque
86600 CELLE L’EVESCAULT
tel. +33 (0)5 49 89 30 00
sales@cerep.com
❚ usa
[Laboratories]
15318 N.E. 95th Street
Redmond, WA 98052
tel. +1 (425) 895 8666
sales@cerep.com
❚ japan
[Sales Office]
Namiki Shoji Co., Ltd.
Kenseishinjuku Bldg. 5-5-3
Shinjuku, Shinjuku-ku
TOKYO, 160-0022
tel. +81 (0)3 3354 4026
ishimoto@namiki-s.co.jp
❚ china
[Laboratories]
上 海 张 江 高 科 技 区 爱 迪 生 路 326 号 302-1 室
(326 Aidisheng Road, B 302-1)
Zhangjiang High-Tech Park
Shanghai 201203
tel. +86 21 5132 0568
sales@cerep-ltd.com
❚ www.cerep.com
•
•
• •

Cerep services p. 4
Receptors
[GPCrs - Nuclear receptors - Other receptors] p. 13
Ion channels p. 93
Transporters p. 103
Kinases p. 107
Epigenetic & DNA-related enzymes p. 157
Other enzymes p. 163
Specialized cellular assays p. 185
Standard profiles p. 195
Testing conditions p. 203
Ordering information p. 209
Assay list& index p. 215

4 in vitro pharmacology 2011 catalog
cerep services
Cerep offers in vitro pharmacology, in vitro ADME-Tox and in vivo PK services, and provides solutions allowing faster and
cost-effective drug discovery by identifying at early stages the most promising drug candidates as well as eliminating those
compounds likely to fail in development.
Cerep’s services benefit annually to more than 450 pharmaceutical and biotechnological companies worldwide including
most of the top pharmaceutical firms.
Both standard and custom research solutions are available.
Standard research services include:
compound management,
high-throughput screening,
in vitro safety profiling,
lead optimization (or SAR) profiling,
in vitro ADME profiling,
in vivo PK.
Custom research services encompass assay development, profile design as well as data interpretation and provide scientistto-scientist
communications to understand and address client’s needs.
Over the past 12 years, Cerep has developed BioPrint ® , a unique database and related IT tools (see page 7), which allows
the modeling of clinical effects of drug candidates from their molecular properties. BioPrint ® may be used to interpret complex
profiling data, prioritize lead or drug candidates or design lead optimization profiles.
To ensure the highest quality and provide the most reproducible data, Cerep produces in-house biological material that are
used in most Cerep assays and qualifies its suppliers for best quality reagents and plasticware.
In 2010 Cerep has established a laboratory in Shanghai which is now fully operational to effectively support drug discovery
projects that are run in Asia by providing the same high quality data that made Cerep’s reputation in the market.
The success of this endeavor could only be achieved through the adaptation, set-up and implementation of processes which
have proven their superiority in terms of quality, reproducibility, cost effectiveness and reduced timelines.
❚ broad profiling/screening services
Cerep continues to expand and diversify the assay families, with an average of 100 assays added or updated each year.
These assays are either integrated in the Cerep catalog, or are exclusively available to sponsor.
The in vitro pharmacology and ADME-Tox & PK 2011 catalogs regroup about 1,300 assays, of which 473 GPCRs,
including 134 cellular functional targets (agonist and antagonist effects), 255 biochemical kinases and 32 cellular kinase
assays (activator and inhibitor effects), 51 ion channels, 61 CYPs (phenotyping, inhibition, induction), 20 epigenetic and
DNA-related enzymes, 14 PDEs, 24 phosphatases ...
Cerep’s platforms cover a wide range of target classes including ADME-Tox related targets, GPCRs, various enzymes,
transporters, nuclear receptors and ion channels; employing methods and assay types such as radioligand binding assays,
calcium mobilization and cAMP measurement using TR-FRET, transporter/uptake assays, and bioluminescent and other
fluorescent-based assays.
❚ assay design and development
The customized assay development services include a full range of assays and technologies adapted to clients’ specific
projects and needs.
Cerep has an extensive and integrated suite of core competencies valuable to any drug discovery programs.
The tool boxes shown below provide information about Cerep’s know-how and expertise in assay development. They are
extendable to other studies, targets and technologies depending on your needs.
Please contact us for a specific solution adapted to your specific request at: customresearch@cerep.com.

5
❚ tool-box for cell-based assay development
In order to study compounds activity in a living cellular background, Cerep can design cellular assays for any target. For
this purpose, Cerep offers a broad panel of cell-based assay solutions, for which principal families are represented here.
These assays can be applied either on recombinant models or more physiologically relevant models such as primary
cells.
Cerep
services
Ion
channels
G protein-coupled
receptors
Growth factor
receptors
Cytokine
receptors
Secretions
ELISA
Alphalisa
Transporters
Receptors
Patch-clamp
Ca 2+
Fluorescence
IP1
TR-FRET
Ca 2+
PLC
Fluorescence
Luminescence
PKC
Gq
Gi
AC
cAMP
TR-FRET
Impedance
CDS
Gs
G12/13
Customized cellular assays developed at Cerep on non-recombinant models
Rho
ELISA
AlphaScreen
Kinases
AlphaScreen
Proliferation
Luminescence
Radioactivity
STATs
AlphaScreen
Cytotoxicity
Luminescence
Imaging
Uptake
Radioactivity
SPA
Ion
channels
Transporters
Kinases
Epigenetic &
DNA-related
enzymes
EYES
ECSC: x
TM: x
CSM: x
Iris: x
AIRWAY
A7R5: NKCC1, L Ca channel
BSMC: beta 2 , H 1
NHBE: PAR1, ROCK
CARDIOVASCULAR
ECV304: OT
HUVEC: H 1 , PAR1, VEGF, ROCK
eEPC: CxCR
HCAEC: PAR1
HMVEC: PAR1
PASMC: aCGRP
SKIN
A431: EGF
B16F1: MC 1
3T3: FGF, PDGF
NHEK: beta 2 , MOP, MC 2
NHDF: NKCC1
Preadipocytes: x
Adipocytes: x
BLOOD CELLS
HL60d: CxCR2
THP1: CCR1, CCR2, CxCR4
MM6: CxCR4
Neutrophils: CXCR1/2
PBMC: IL
Macrophages: x
Dendritic: x
Platelets: x
BONE
SaOS2: PTH1
hMSC: LTB 4
Osteoblasts: LTB 4
Osteoclasts: x
HAIR
HHDPC: x
NEURAL
PC12: A2 A, neurite outgrowth
SK-N-MC: ETA, Y 1 , β3
SK-N-SH: Na channel
SH-SY-5Y: MOP, DOP
NG108-15: DOP, AT 2 , CB 1
IMR32: SST2
Neurons: CB 1
RC4BC: grehlin
U373MG: NK 1 , CB 1
C6: 5-HT 2A
1321N1: H 1 , beta 2 , M 3 , PAR1
Astrocytes: mGluR5, beta 2 , ET A
MAMMARY
T47D: calcitonin
MDA-MB-231: PAR1/2, IGF1, HGF, EGF
PANCREATIC
betaTC6: GLP-1
HIT-T15: GPR119
LIVER
HepG2: GLP-1, INS, Tox
Hepatocytes: INS, CYPs, BA transport
KIDNEY
HEK: TP, AT 1 , JNK1/3
COLON
HT29: VPAC 1
UTERUS
HELA: alpha 2A , beta 2 , H 1 , EGF
OVARY
CHO: 5-HT 1B , EP 2
Red: Primary cells
x: Undisclosed target (confi dentiality agreement)
Other
enzymes
Specialized
cellular
assays
Standard
profiles
Testing
conditions
Ordering
information
Assay list
& index

6 in vitro pharmacology 2011 catalog
❚ assay design & development
❚ tool-box for biochemical assays
In addition to cellular assays, Cerep offers multiple biochemical assays to accurately study the interaction of compounds
with the target of interest. These assays can be developed on recombinant material or native tissues.
Targets Binding assays Functional assays
GPCR Radioligand binding GTPgS
Ion channel Radioligand binding –
Kinases TR-FRET TR-FRET
Other enzymes Radioligand binding Multiple technologies
Growth factor receptors Radioligand binding –
Cytokine receptors Radioligand binding –
Nuclear receptors Radioligand binding AlphaScreen
Transporters Radioligand binding –
Customized binding assays developed at Cerep on native animal tissues:
Serotonin 5-HT 1A , 5-HT 2A in rat brain, 5-HT 3 , 5-HT 6 , 5-HT 7 in rat cDNA
Muscarinic M 1 , M 3 in rat brain, M 2 in rat heart
Endothelin ET A in rat A-10 cells, ET B in rat cerebellum
Cholecystokinin CCK A , CCK B in rodent
Dopamine D 1 , D 2 in rat striatum
Transporters choline, dopamine and norepinephrine in rat striatum, 5-HT in rat brain
...
For a complete list, please contact us at customresearch@cerep.com.
❚ tool-box for gpcrs
Depending on the type of target, study and model, Cerep can recommend the most adapted technology.
Studies Targets Gi Gq Gs G12/13
Affinity
Kon/Koff
Agonist
Antagonist
Allosteric (PAM & NAM)
Inverse agonist
Weak agonist
Slow agonist
RLB 1
RLB 1
RLB 1
RLB 1
SPA 2 SPA 2 SPA 2 SPA 2
GTPgS
TR-FRET cAMP
CDS 3
Aequorin 4
GTPgS
TR-FRET cAMP
CDS 3
GTPgS
TR-FRET cAMP
CDS 3
TR-FRET IP1
Fluorescence
CDS 3
Aequorin 4
TR-FRET IP1
CDS 3
TR-FRET IP1
CDS 3
TR-FRET cAMP
CDS 3
Aequorin 4
ELISA
CDS 3
Aequorin 4
TR-FRET cAMP
CDS 3 CDS 3
TR-FRET cAMP
CDS 3 CDS 3
Deorphanization CDS 3
CDS 3
CDS 3
CDS 3
Aequorin 4 Aequorin 4 Aequorin 4 Aequorin 4
Coupling mechanism CDS 3 CDS 3 CDS 3 CDS 3
Kinase phosphorylation AlphaScreen AlphaScreen AlphaScreen AlphaScreen
1
RLB: RadioLigand Binding
2
SPA: Scintillation Proximity Assay
3
CDS: Cellular Dielectric Spectroscopy
4
Expression of chimeric or promiscuous G proteins may be required.

7
❚ profile design
Cerep offers a profile design service based on the experience and knowhow of its scientists for both content and execution
of profiles. Cerep BioPrint ® database (see below), various publicly available databases, and the scientific literature are
used to design different types of profiles according to your needs.
Cerep
services
❚ tool-box for profile design
Type Content Applications
Disease profile
Side effect profile
Predictive profile
Targets that are
associated to a
particular disease
Targets that are
associated to a
particular side effect
Targets that are
susceptible to be
hit by a given
compound
- Find a therapeutic indication for a given compound or marketed drug (repositioning)
- Find the target(s) responsible for the therapeutic effect (mechanism of action)
- Lead optimization
- Anticipate an unwanted sife effect
- Find the target(s) responsible for the therapeutic effect (mechanism of action)
- Lead optimization
- Assess the target selectivity of a given compound
- Find a therapeutic indication for a given compound or marketed drug (repositioning)
- Find the target(s) responsible for the therapeutic effect (mechanism of action)
- Anticipate an unwanted sife effect
- Find the target(s) responsible for the therapeutic effect (mechanism of action)
- Lead optimization
Receptors
Ion
channels
Transporters
❚ bioprint ® profile & services
Kinases
BioPrint ® is a large, homogenous pharmacology and ADME
database, which provides a unique resource for supporting
decision making in drug discovery. The database is composed
of three main data sets:
chemical descriptors (structures and chemical information,
2D and 3D descriptors),
in-house generated in vitro pharmacology and ADME
data, also considered as compound descriptors,
collected and curated in vivo effects of drugs.
Chemical and pharmacophoric descriptors together form
a data set for QSAR generation supporting organ safety
modeling.
BioPrint ® positions a new drug candidate in the context of
marketed drugs, anticipating potential in vivo liabilities,
predicting off-target activities, and ADME characteristics
(Drug profile interpretation). In another application, BioPrint ®
serves to identify secondary targets that are not genetically
parented to a test target (target profile design). Both these
applications are available as custom services.
2,450 compounds
chemical
properties
2D structures
and 3D descriptors
in vitro data
consistent
in vitro
pharmacology
& ADME profiles
on 159 assays
QSAR
clinical
observations
organ safety
side effects
PK
therapeutic effects
Epigenetic &
DNA-related
enzymes
Other
enzymes
Specialized
cellular
assays
Standard
profiles
❚ BIOPRINT ® PROFILE
The BioPrint ® profile includes the assays used to explore the properties of about 2,450 BioPrint ® compounds (mainly
marketed drugs and reference compounds), establishing individual Pharma-ADME fingerprints for each compound.
Offered on a standard basis, this profile is mainly based on target diversity and includes today 105 binding assays (GPCRs,
nuclear and other receptors, ion channels and transporters), 34 enzyme assays (including 10 kinases, 10 proteases and
5 phosphodiesterases), as well as 20 ADME-Tox assays (Solubility, Absorption, Metabolism and CYP-mediated drug-drug
interaction). More than 70% are human targets. The 159 assays of this profile represent a rationalized panel from a larger
assay collection in the database, selected for highest information content.
For list of assays included in BioPrint ® profile, please go to www.cerep.com catalog online
❚ BIOPRINT ® DRUG PROFILE INTERPRETATION
Any compound in drug development, when run as a test compound on the BioPrint ® profile, can be placed in the context
of already marketed drugs, when similar in vitro profiles exist in the database. Hypotheses on clinical behavior of the test
Testing
conditions
Ordering
information
Assay list
& index

8 in vitro pharmacology 2011 catalog
❚ bioprint ® profile & services [drug profile interpretation]
compounds can be drawn by comparison with data on BioPrint ® compounds that have been collected and analyzed
over the last twelve years, including:
Clinical effects of drugs with a similar profile or sub-profile.
Adverse Drug Reactions (ADRs) correlated with in vitro assays: more than 5,000 significant statistical associations
have been identified between the activity of molecules on a specific target and the occurrence of an ADR in man.
Probability of occurrence of clinical effects or ADRs estimated with multivariate models using the complete in vitro profile:
today more than 170 ADRs have been modeled.
Deliverables – Phase A
Primary screening + IC 50 s (with a 10% hits hypothesis) on BioPrint ® profile
If statistical neighbors are identified, then the following deliverables will be provided as part of the report. In case no
pharmacological neighbors exist, the client will be informed at no extra charge.
Deliverables – Phase B
Individual hit analysis (similar hits of drugs on the market, known liabilities)
Profile similarity analysis (nearest neighbor compounds by whole profile analysis, known liabilities)
List of ADR associations (ADRs associated to hits of test compound and nearest neighbors)
Strength of hits (with respect to a threshold of significance and PK comparison)
Follow-up (suggestion on further assays and other tests)
Option
Neighbor compound % of inhibition and IC 50 s
❚ BIOPRINT ® TARGET PROFILE DESIGN
Any target, run as a test target on the BioPrint ® compound library, can be compared to any other target in BioPrint ® , based
on its pharmacological profile (compounds that interact with a given target). Analysis of cross-reacting compounds between
targets (number and intensity of common hits), allows to identify targets that are “pharmacophorically related” to the test target.
Interestingly, a profile of pharmacophorically related targets can differ significantly to a list of genetically related targets.
BioPrint ® target profile design represents highly valuable information, when setting up secondary screening tests, anticipating
secondary targets and effectively supporting lead optimization to monitor potential secondary target related liability
issues. If the test target is already part of BioPrint ® assays, BioPrint ® target profile design is limited to data-analysis and
establishment of a profile of secondary targets. If the test target is not part of the BioPrint ® assay panel, Cerep can develop
the assay and run the BioPrint ® compounds on an exclusive or shared data basis.
Deliverables I – Analysis
When relevant statistical correlations can be drawn, an analysis including the followings will be performed (in case no
strong correlations are identified, no charge will be incurred):
Total number of compounds in BioPrint ® that hit test target
Number of compounds hitting secondary target
Average number of BioPrint ® targets hit by compounds reacting with test target
Identity of up to 20 nearest neighbor targets (including closest CYP 450s)
Prioritization of neighbor targets by number of cross-reacting compounds
Digest, suggesting a selected set of assays to cover major cross-reactivity issues
Option
Literature search for relevant associated targets
Deliverables II – Test-target profiling + Profile design (shared or exclusive data)
Total number and ID of BioPrint ® compounds hitting test target (% of inhibition, IC 50 s)
Cross-reacting compound IDs, % of inhibition and IC 50 s
Deliverables I included
REFERENCES
The BioPrint ® approach for the evaluation of ADMET properties: application to the prediction of cytochrome P450 2D6 inhibition - Gozalbes, R., et al. (2006) in
Pharmacokinetic profiling in drug Research, VHCA, Zürich, WILEY-VCH, Weinheim.
Can we rationally design promiscuous drugs? - Hopkins et al. (2006) et al. (2005), Current Opinion in Structural Biology, 16:127-136
Construction of a homogeneous and informative in vitro profiling database for anticipating the clinical effects of drugs - Froloff, N. et al. (2006) in Chemogenomics
knowledge-based approaches to Drug discovery, Imperial College Press, London.
QSAR modeling of in vitro inhibition of cytochrome P450 3A4 - Mao, B., et al. (2006) J. of Chem. Inf. and Modeling, 46: 2125-2134.
Pharmacological and pharmaceutical profiling: new trends - Hamon, V., et al. (2006) in The Process of New Drug Discovery and Development (2 nd Edition), Smith,
C.G. & O’Donnell, J.T. (Eds.), Informa Healthcare, New York..
Analysis of drug-induced effect patterns to link structure and side effects of medicines - Fliri, F. A. et al. (November 2005), Nature Chemical Biology
Biological spectra analysis: Linking biological activity profiles to molecular structure - Fliri, F. A. et al. (2005), PNAS, 102: 261-266
G-protein-coupled receptor affinity prediction based on the use of a profiling dataset: QSAR design, synthesis, and experimental validation - Rolland C., et al. (2005)
Journal of Medicinal Chemistry, 48: 6563-6574.
Probing drug action using in vitro pharmacological profiles - Froloff, N. (2005) Trends in Biotechnology, 23: 488-490.
Predicting ADME properties and side effects: The BioPrint approach - Krejsa C.M., et al. (2003) Curr. Opin. Drug. Discov. Devel., 6: 470-480
Neighborhood behavior of in silico structural spaces with respect to in vitro activity spaces – A novel understanding of the molecular similarity principle in the context
of multiple receptor binding profiles - Horvath D. and Jeandenans C. (2003). J. Chem. Inf. & Comp. Sci., 43: 680-690.
Neighborhood behavior of in silico structural spaces with respect to in vitro activity spaces – A benchmark for neighborhood behavior assessment of different in silico
similarity metrics - Horvath D. and Jeandenans C. (2003) J. Chem. Inf. & Comp. Sci., 43: 691-698.
Method of identification of leads or active compounds - Jean, T. and Chapelain, B. (1999) - EP 1018008B1.

9
❚ data online
A powerful web-based, secure system to view your study information in real-time.
Cerep
services
Download your data and reports directly
Cerep’s Data Online service can be accessed using Internet Explorer 5+, Netscape Navigator 6+ and Mozilla.
To experience the power and convenience of Data Online, go to https://www.cerep.com/secure, and use “Demo” as
login and password.
❚
❚
Two options
- The real-time data option enables the sponsor to view study data as they are produced, and also to convert them into
MSExcel.
- The final report option enables the sponsor to download complete study reports and other related documents as they
are generated.
Security
- To deliver the world’s highest level of trust, a company specialized in providing High-Assurance SSL Certificates authenticates
our organization, enabling end users to verify our site and communicate via state-of-the-art SSL encryption.
- Our server supports all browser SSL encryption types (40 bit, 56 bit, and 128 bit strong encryption).
- Passwords are not stored in any database; they are owned and encrypted by the operating system security mechanism.
Only the sponsor has knowledge of the password.
- You can safely enter your password and download files from the secure server.
- Our network topology to access the Data Online web server is also secured via state-of-the-art network security solutions.
- Server operating systems and software are updated immediately upon receipt of the provider’s security bulletin.
To experience the power and convenience of Data Online, please go to www.cerep.com
data online
Receptors
Ion
channels
Transporters
Kinases
Epigenetic &
DNA-related
enzymes
Other
enzymes
Specialized
cellular
assays
❚ see also ADME-Tox & PK 2011 catalog
ADME-Tox & PK
2011 CATALOG
IN VITRO ADME
Solution properties
Drug absorption/drug transport
Drug metabolism
Drug-drug interactions
IN VITRO TOXICITY
Cardiac toxicity
Cytotoxicity
Genetic toxicity
IN VIVO PK/BIOANALYTICAL
In vivo PK
Bioanalytical
ASSAY SELECTION GUIDE
STANDARD profiles
APPLICATION NOTES
Standard
profiles
Testing
conditions
Ordering
information
Assay list
& index

10 in in vitro pharmacology 2011 catalog

11
in vitro
pharmacology
assays
Receptors
[GPCrs]
[Nuclear receptors]
[Other receptors]
p. 13
p. 79
p. 83
Ion channels p. 93
Transporters p. 103
Kinases p. 107
Epigenetic & DNA-related enzymes p. 157
Other enzymes p. 163
Specialized cellular assays p. 185

12 in vitro pharmacology 2011 catalog
❚ notes
❚ see also ADME-Tox & PK 2011 catalog
ADME-Tox & PK
2011 CATALOG
IN VITRO ADME
Solution properties
Drug absorption/drug transport
Drug metabolism
Drug-drug interactions
IN VITRO TOXICITY
Cardiac toxicity
Cytotoxicity
Genetic toxicity
IN VIVO PK/BIOANALYTICAL
In vivo PK
Bioanalytical
ASSAY SELECTION GUIDE
STANDARD PROFILES
APPLICATION NOTES

13
Cerep
services
receptors
Receptors
[GPCRs]
[g protein-coupled receptors]
Ion
channels
❚ Adenosine
Transporters
A 1 - antagonist radioligand
binding
Ref. 0002
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]DPCPX (1 nM)
1.7 nM
DPCPX (1 µM)
DPCPX (IC 50 : 1 nM)
Townsend-Nicholson, A. and Schofield, P.R. (1994) J. Biol. Chem., 269: 2373-2376
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
DPCPX
CPA
NECA
CGS 21680
Kinases
Epigenetic &
DNA-related
enzymes
A 1 - agonist radioligand
binding
Ref. 0442
Q 3 weeks
Included in:
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]CCPA (1 nM)
0.7 nM
CPA (10 µM)
CPA (IC 50 : 1.84 nM)
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4
CPA
DPCPX
CGS 21680
log [drug] (M)
Rivkees, S.A. et al. (1995) J. Biol. Chem., 270: 20485-20490.
[CUSTOM OFFER] rat cerebral cortex model (Ref. 0001), please contact us at customresearch@cerep.com
Other
enzymes
Specialized
cellular
assays
A 1
cellul ar
Ref. 2814
Ref. 2820
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product impedance
Detection method cellular dielectric spectroscopy
Agonist effect Control CPA (1 µM)
Reference CPA (EC 50 : 1 nM)
Antagonist effect Stimulant CPA (10 nM)
Reference DPCPX (IC 50 : 39 nM)
Cordeaux, Y. et al. (2004) Brit. J. Pharmacol., 143: 705-714.
[Solvent] must be kept 0.1%
Standard
profiles
Testing
conditions
A 1 - inverse agonist effect
cellul ar
Ref. 2408
Q 3 weeks
Source
Measured product cAMP
Detection method HTRF
human recombinant (CHO cells)
Control
CGS 15943 (10 µM)
Reference CGS 15943 (EC 50 : 161 nM)
[Solvent] must be kept ≤ 0.3%
Shryock, J.C. et al. (1998) Mol. Pharmacol., 53: 886-893.
Ordering
information
Assay list
& index

14 in vitro pharmacology 2011 catalog
❚ Adenosine
A 1
tissue
Ref. 0294
Q 4 weeks
Source
Agonist CPA (pD 2 = 7.2)
Antagonist DPCPX (pA 2 = 8.1)
guinea-pig left atrium (electrically paced)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Collis, M.G. (1983) Brit. J. Pharmacol., 78: 207-212.
tension (% of control)
100
50
-10 -9 -8 -7 -6 -5 -4
log [agonist] (M)
DPCPX
none
10 nM
30 nM
100 nM
A 2A - agonist radioligand
binding
Ref. 0004
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (HEK-293 cells)
[ 3 H]CGS 21680 (6 nM)
27 nM
NECA (10 µM)
NECA (IC 50 : 28 nM)
specific binding (% of control)
100
50
0
-10 -9 -8 -7 -6 -5
log [drug] (M)
Luthin, D.R. et al. (1995) Mol. Pharmacol., 47: 307-313.
[CUSTOM OFFER] rat striatum model (Ref. 0003), please contact us at customresearch@cerep.com
NECA
CGS 21680
CPA
DPCPX
A 2A
cellul ar
Ref. 2055
Ref. 2056
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
PC12 cells (endogenous)
Measured product cAMP
Detection method HTRF
Agonist effect Control NECA (1 µM)
Reference NECA (EC 50 : 18.7 nM)
Antagonist effect Stimulant NECA (300 nM)
Reference ZM 241385 (IC 50 : 1.6 nM)
Gao, Z. et al. (2001) J. Pharmacol. Exp. Ther., 298: 209-218.
[Solvent] must be kept 0.3%
A 2A - agonist effect
cellul ar
Ref. 2527
Q 3 weeks
Source
human recombinant (HEK-293 cells)
Measured product impedance
Detection method cellular dielectric spectroscopy
Control
NECA (1 µM)
Reference NECA (EC 50 : 35 nM)
[Solvent] must be kept ≤ 0.1%
Gao, Z. et al. (2001) J. Pharmacol. Exp. Ther., 298: 209-218.
A 2A - inverse agonist effect
cellul ar
Ref. 2409
Q 3 weeks
Source
Measured product cAMP
Detection method HTRF
Control
Reference
[Solvent] must be kept ≤ 0.3%
human recombinant (HEK-293 cells)
ZM 241385 (300 nM)
ZM 241385 (EC 50 : 6.33 nM)
Klinger, M. et al. (2002) Naun.-Sch. Arch. Pharmacol., 366: 287-298.
A 2A
tissue
Ref. 0295
Q 4 weeks
Source
guinea-pig trachea
(precontracted with 0.1 µM carbachol)
Agonist NECA (pD 2 = 6.7)
Antagonist CGS 15943A (pA 2 = 7.3)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Ghai, G. et al. (1987) J. Pharmacol. Exp. Ther., 242: 784-790.
tension (% of control)
100
50
0
-9 -8 -7 -5 -6
log [agonist] (M)
CGS 15943A
none
0.1 µM
0.3 µM
1 µM

15
Adenosine ❚
A 2B - antagonist radioligand
binding
Ref. 0005
Q 3 weeks
Included in:
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (HEK-293 cells)
[ 3 H]MRS 1754 (2 nM)
1 nM
NECA (100 µM)
NECA (IC 50 : 1.5 µM)
Ji, X. et al.(2001) Biochem. Pharmacol., 61: 657-663.
Cerep
services
Receptors
[GPCRs]
A 2B
cellul ar
Ref. 0452
Ref. 0455
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
human recombinant (HEK-293 cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control NECA (10 µM)
Reference NECA (EC 50 : 330 nM)
Antagonist effect Stimulant NECA (1 µM)
Reference XAC (IC 50 : 51 nM)
Cooper, J. et al. (1997) Brit. J. Pharmacol., 122: 546-550.
cAMP modulation (% of control)
100
100
50
50
0
0
-9 -8 -7 -6 -5 -4
-9 -8 -7 -6 -5 -4
log [agonist] (M)
log [antagonist] (M)
NECA
XAC
adenosine
CGS 15943
CPA
DPCPX
IB-MECA
MRS 1754
[Solvent] must be kept ≤ 0.3%
Ion
channels
Transporters
A 2B
tissue
Source
guinea-pig aorta
(precontracted with 1 µM phenylephrine)
Agonist NECA (pD 2 = 6.4)
Antagonist 8-phenyltheophylline (pA 2 = 6.2)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
tension (% of control)
100
50
0
8-phenyltheophylline
none
1 µM
3 µM
10 µM
Kinases
Ref. 0783
Q 4 weeks
[Solvent] must be kept ≤ 0.1%
Gurden, M.F. et al. (1993) Brit. J. Pharmacol., 109: 693-698.
-8 -7 -6 -5 -4
log [agonist] (M)
Epigenetic &
DNA-related
enzymes
A 3 - agonist radioligand
binding
Ref. 0006
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (HEK-293 cells)
[ 125 I]AB-MECA (0.15 nM)
0.22 nM
IB-MECA (1 µM)
IB-MECA (IC 50 : 0,27 nM)
Salvatore, C.A. et al. (1993) Proc. Natl. Acad. Sci. USA, 90: 10365-10369.
Other
enzymes
Specialized
cellular
assays
A 3
cellul ar
Ref. 0982
Ref. 0983
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control IB-MECA (100 nM)
Reference IB-MECA (EC 50 : 1.5 nM)
Antagonist effect Stimulant IB-MECA (30 nM)
Reference MRS 1220 (IC 50 : 125 nM)
Yates, L. et al. (2006) Auton. Autacoid. Pharmacol., 26: 191-200.
[Solvent] must be kept 0.3%
❚ See other Adenosine assays, page 103
Standard
profiles
Testing
conditions
❚ For radioligand binding assays, how should I choose between the agonist and the antagonist models when both are
available?
For some binding assays two models are available using either agonist or antagonist as radioligand.
G-protein-coupled receptors have both high-affinity and low-affinity states that are bound differently by agonists and antagonists. Whereas
the antagonists bind with an equal affinity to both affinity states, agonists bind poorly to the low affinity state of the receptor. Therefore,
it is advisable to use an antagonist radioligand to evaluate the binding of antagonists knowing that this may fail to reveal the binding
of agonists. On the other hand, an assay using an agonist radioligand is suitable to evaluate both agonists and antagonists.
The testing of a compound in both assays and the comparison of its competition curves against each radioligand may provide information
about its functional activity at the receptor.
Ordering
information
Assay list
& index

16 in vitro pharmacology 2011 catalog
❚ Adrenergic
alpha 1 (non-selective) - antagonist radioligand
binding
Ref. 0008
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]prazosin (0.25 nM)
0.09 nM
prazosin (0.5 µM)
prazosin (IC 50 : 0.182 nM)
Greengrass, P. and Bremner, R. (1979) Eur. J. Pharmacol., 55: 323-326.
specific binding (% of control)
100
50
prazosin
WB 4101
spiperone
0
phentolamine
-12 -11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
alpha 1 (non-selective)
tissue
Ref. 0296
Q 4 weeks
Source
rabbit aorta (endothelium-denuded)
Agonist phenylephrine (pD 2 = 6.5)
Antagonist prazosin (pA 2 = 9.1)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Docherty, J.R. et al. (1981) Naun.-Sch. Arch. Pharmacol., 317: 5-7.
tension (% of max.)
100
50
0
-8 -7 -6 -5 -4
log [agonist] (M)
prazosin
none
3 nM
10 nM
30 nM
alpha 1A - antagonist radioligand
binding
Ref. 2338
Q 3 weeks
Included in:
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]prazosin (0.1 nM)
0.1 nM
epinephrine (0.1 mM)
WB 4101 (IC 50 : 0.36 nM)
Schwinn, D.A. et al. (1990) J. Biol. Chem., 265: 8183-8189.
alpha 1A - antagonist radioligand
Source
rat salivary glands
Ligand
[ 3 H]prazosin (0.06 nM)
Kd
0.066 nM
Non specific phentolamine (10 µM)
binding
Reference WB 4101 (IC 50 : 0.12 nM)
Ref. 0009
Q 3 weeks
Michel, A.D. et al. (1989) Brit. J. Pharmacol., 98: 883-889.
specific binding (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5
log[drug] (M)
WB 4101
spiperone
phentolamine
oxymetazoline
alpha 1A
cellul ar
Ref. 1500 Agonist effect
Ref. 1501 Antagonist effect
Q 3 weeks
Included in:
Cellular functional GPCR profile
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control epinephrine (30 nM)
Reference epinephrine (EC 50 : 0.4 nM)
Antagonist effect Stimulant epinephrine (3 nM)
Reference WB 4101 (IC 50 : 7 nM)
Vicentic, A. et al. (2002) J. Pharmacol. Exp. Ther., 302: 58-65.
Ca 2+ mobilization (% of control)
100
50
0
-10 -9 -8 -7
-12 -11 -10 -9 -8 -7 -6 -5
log [agonist] (M)
epinephrine
A61603
cirazoline
oxymetazoline
100
[Solvent] must be kept ≤ 0.1%
50
0
log [antagonist] (M)
WB 4101
prazosin
L765314
BMY7378
-11 -10
-9 -8 -7 -6 -5 -4
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
-12 -11
-10 -9 -8 -7
-12 -11 -10 -9 -8 -7
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
-12 -11 -10 -9 -8 -7 -6 -5
Assay developed in 2010 New assay conditions Human Q Standard turnaround time
-9 -8 -7 -6 -5
-10 -4
-11 -10
-9 -8 -7 -6 -5 -4

17
alpha 1B - antagonist radioligand
binding
Ref. 1633
Q 3 weeks
Included in:
BioPrint ® profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]prazosin (0.15 nM)
0.055 nM
phentolamine (10 µM)
prazosin (IC 50 : 0.25 nM)
specific binding (% of control)
100
50
0
-12
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
Ford, A.P.D.W. et al. (1997) Brit. J. Pharmacol., 121: 1127-1135.
[CUSTOM OFFER] rat liver model (Ref. 0010), please contact us at customresearch@cerep.com
adrenergic ❚
prazosin
BMY7378
oxymetazoline
phenylephrine
Cerep
services
Receptors
[GPCRs]
alpha 1B
cellul ar
Ref. 1901
Ref. 1902
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control epinephrine (10 µM)
Reference epinephrine (EC 50 : 207 nM)
Antagonist effect Stimulant epinephrine (1 µM)
Reference L765314 (IC 50 : 24 nM)
Schwinn, D.A. et al. (1995) J. Pharmacol. Exp. Ther., 272: 134-142.
cAMP modulation (% of control)
100
100
50
50
0
0
-9 -8 -7 -6 -5 -4 -12 -11 -10 -9 -8 -7 -6 -5
log [agonist] (M)
log [antagonist] (M)
epinephrine
L765314
norepinephrine
prazosin
M6434
BMY7378
phenylephrine
corynanthine
Ion
channels
Transporters
alpha 1D - antagonist radioligand
Source
human recombinant (CHO cells)
Ligand
[ 3 H]prazosin (0.2 nM)
binding
Kd
0.15 nM
Ref. 1942
Non specific phentolamine (10 µM)
Q 3 weeks
Reference prazosin (IC 50 : 0.38 nM)
Included in:
Organ safety profile
Kenny, B.A. et al. (1995) Brit. J. Pharmacol., 115: 981-986.
specific binding (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
prazosin
WB 4101
BMY7378
oxymetazoline
Kinases
Epigenetic &
DNA-related
enzymes
alpha 2 (non-selective) - antagonist radioligand
binding
Ref. 0011
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]RX 821002 (0.5 nM)
0.38 nM
(-)epinephrine (100 µM)
yohimbine (IC 50 : 58.7 nM)
Uhlen, S. and Wikberg, J.E. (1991) Pharmacol. Toxicol., 69: 341-350.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5
log [drug] (M)
yohimbine
RX 821002
oxymetazoline
prazosin
Other
enzymes
Specialized
cellular
assays
selected cerep assays
❚ binding assays
Binding assays are developed according to the competition assay principle. There are three assay formats used: filtration, scintillation
proximity assay (SPA) and centrifugation. All formats utilize a radiolabeled ligand and a source of receptor (membranes, soluble/purified).
Large batches of cells, from which prepared membranes are frozen and stored, are produced in-house. Membrane preparations are
quality controlled before use.
❚ cellular Functional GPCR assays
Functional GPCR assays are cell-based assays to measure agonist-like, inverse agonist, antagonist and modulator activity of compounds.
Various technologies are used: TR-FRET to determine cAMP concentration and IP1 levels, real time fluorescence to monitor calcium flux,
cellular dielectric spectroscopy to measure impedance modulation. Large batches of cells, from which whole cells are frozen and stored
for functional assays, are produced in-house. Cells are quality controlled before use. A novel patented host cell line was designed and
constructed for Gi protein coupled receptors.
❚ tissue bioassays
Tissue bioassays are functional assays designed to evaluate the agonist and antagonist activities of compounds at various receptors and
ion channels in whole tissues. The tissues used are isolated from contractile cardiac and smooth muscles of the cardiovascular, respiratory,
gastrointestinal and urogenital tracts of rodents, rabbit or human. The selected tissues are assayed in organ bath systems to record the
contractile activity in conditions as selective as possible to avoid any potential interaction with other receptors known to be present in
the tissue used.
Standard
profiles
Testing
conditions
Ordering
information
Assay list
& index

18 in vitro pharmacology 2011 catalog
❚ adrenergic
alpha 2 (non-selective)
tissue
Ref. 0297
Q 4 weeks
Source
rabbit ear vein
Agonist clonidine (pD 2 = 7.9)
Antagonist yohimbine (pA 2 = 8.1)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Daly, C.J. et al. (1988) Brit. J. Pharmacol., 94: 1085-1090.
tension (% of max.)
100
50
0
-10 -9 -8 -7 -6 -5
log [agonist] (M)
yohimbine
none
30 nM
100 nM
300 nM
alpha 2A - antagonist radioligand
binding
Ref. 0013
Q 3 weeks
Included in:
BioPrint ® profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]RX 821002 (1 nM)
0.8 nM
(-)epinephrine (100 µM)
yohimbine (IC 50 : 5.5 nM)
Langin, D. et al. (1989) Eur. J. Pharmacol., 167: 95-104.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5
log [drug] (M)
yohimbine
prazosin
RX 821002
oxymetazoline
alpha 2A - agonist radioligand
Source
human recombinant (CHO cells)
Ligand
[ 3 H](-)epinephrine (1 nM)
binding
Kd
0.7 nM
Ref. 1669
Non specific RX 821002 (1 µM)
Q 3 weeks
Reference epinephrine (IC 50 : 2.6 nM)
Included in:
Organ safety profile
Senard, J.M. et al. (1989) Eur. J. Pharmacol., 162: 225-236.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5
log [drug] (M)
epinephrine
oxymetazoline
RX 821002
prazosin
alpha 2A
cellul ar
Ref. 2558
Ref. 2559
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product impedance
Detection method cellular dielectric spectroscopy
Agonist effect Control epinephrine (100 nM)
Reference epinephrine (EC 50 : 4 nM)
Antagonist effect Stimulant epinephrine (10 nM)
Reference RX 821002 (IC 50 : 14 nM)
Bavadekar, S.A. et al. (2006) J. Pharmacol. Exp. Ther., 31: 739-748.
[Solvent] must be kept 0.1%
alpha 2B - antagonist radioligand
binding
Ref. 1344
Q 3 weeks
Included in:
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]RX 821002 (2.5 nM)
5 nM
(-)epinephrine (100 µM)
yohimbine (IC 50 : 5.2 nM)
specific binding (% of control)
100
50
0
-10
-9 -8 -7 -6 -5
yohimbine
RX 821002
prazosin
oxymetazoline
log [drug] (M)
Devedjian, J.-C. et al. (1994) Eur. J. Pharmacol., 252: 43-49.
[CUSTOM OFFER] mouse NG108-15 cells model (Ref. 0014), please contact us at customresearch@cerep.com
alpha 2B
cellul ar
Ref. 1813
Ref. 0299
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (HEK-293 cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control dexmedetomidine (1 µM)
Reference dexmedetomidine (EC 50 : 5.5 nM)
Antagonist effect Stimulant dexmedetomidine (30 nM)
Reference yohimbine (IC 50 : 320 nM)
Eason, M.G. et al. (1992) J. Biol. Chem., 267: 15795-15801.
[Solvent] must be kept 0.3%

19
adrenergic ❚
alpha 2C - antagonist radioligand
binding
Ref. 0016
Q 3 weeks
Included in:
BioPrint ® profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]RX 821002 (2 nM)
0.95 nM
(-)epinephrine (100 µM)
yohimbine (IC 50 : 1.9 nM)
Devedjian, J.-C. et al. (1994) Eur. J. Pharmacol., 252: 43-49.
specific binding (% of control)
100
50
0
-10 -9 -8 -7 -6 -5
log [drug] (M)
yohimbine
RX 821002
prazosin
oxymetazoline
Cerep
services
Receptors
[GPCRs]
alpha 2C - agonist radioligand
Source
human recombinant (CHO cells)
Ligand
[ 3 H](-)epinephrine (1 nM)
binding
Kd
0.9 nM
Ref. 1682
Non specific RX 821002 (1 µM)
Q 3 weeks
Reference epinephrine (IC 50 : 2.87 nM)
Included in:
Organ safety profile
Bylund, D.B. et al. (1992) Mol. Pharmacol., 42: 1-5.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5
log [drug] (M)
epinephrine
oxymetazoline
RX 821002
prazosin
Ion
channels
Transporters
alpha 2C
cellul ar
Ref. 1736
Ref. 1737
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control epinephrine (1 µM)
Reference epinephrine (EC 50 : 2.6 nM)
Antagonist effect Stimulant epinephrine (100 nM)
Reference rauwolscine (IC 50 : 55 nM)
Regan, J.W. et al. (1988) Biochem., 85: 6301-6305.
cAMP modulation (% of control)
100
50
0
-12 -11
-10 -9 -8 -7 -6 -5
log [agonist] (M)
epinephrine
oxymetazoline
clonidine
UK 14,304
100
50
0
-9 -8 -7 -6 -5
-10 -4
log [antagonist] (M)
rauwolscine
yohimbine
prazosin
RX 821002
Kinases
Epigenetic &
DNA-related
enzymes
beta 1 - agonist radioligand
binding
Ref. 0018
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (HEK-293 cells)
[ 3 H](-)CGP 12177 (0.15 nM)
0.39 nM
alprenolol (50 µM)
atenolol (IC 50 : 278 nM)
specific binding (% of control)
-12 -11
100
-10 -9 -8 -7 -6 -5
50
-9 -8 -7 -6 -5
-10 -4
0
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
Levin, M.C. et al. (2002) J. Biol.Chem., 277: 30429-30435.
[CUSTOM OFFER] rat heart model (Ref. 0017), please contact us at customresearch@cerep.com
atenolol
CGP 20712A
propranolol
ICI 118551
Other
enzymes
Specialized
cellular
assays
beta 1
cellul ar
Ref. 1605
Ref. 1606
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
human recombinant (HEK-293 cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control isoproterenol (100 nM)
Reference isoproterenol (EC 50 : 0.3 nM)
Antagonist effect Stimulant isoproterenol (1 nM)
Reference atenolol (IC 50 : 150 nM)
Frielle, T. et al. (1987) Proc. Natl. Acad. Sci. USA, 84: 7920-7924.
cAMP modulation (% of control)
100
100
50
50
0
0
-12 -11 -10 -9 -8 -7 -6 -5 -4 -3 -9 -8 -7 -6 -5 -4
log [agonist] (M)
log [antagonist] (M)
isoproterenol
atenolol
norepinephrine
propranolol
xamoterol
CGP 20712A
salbutamol
ICI 118551
[Solvent] must be kept ≤ 0.3%
Standard
profiles
Testing
conditions
beta 1 - inverse agonist effect
cellul ar
Ref. 2377
Q 3 weeks
Source
human recombinant (HEK-293 cells)
Measured product cAMP
Detection method HTRF
Control
ICI 118551 (10 µM)
Reference ICI 118551 (EC 50 : 93.8 nM)
[Solvent] must be kept ≤ 0.3%
Lattion, A.L. et al. (1999) FEBS Lett., 457: 302-306.
-12 -11 -10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
Ordering
information
Assay list
& index

20 in vitro pharmacology 2011 catalog
❚ adrenergic
beta 1
tissue
Ref. 0298
Q 4 weeks
Source
guinea-pig right atrium
Agonist isoproterenol (pD 2 = 8.3)
Antagonist atenolol (pA 2 = 7.2)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
O’Donell, S.R. and Wanstall, J.C. (1979) Naun.-Sch. Arch. Pharm., 308: 183-190.
frequency (% of max.)
100
50
0
-11 -10 -9 -8 -7 -6
log [agonist] (M)
atenolol
none
0.1 µM
0.3 µM
1 µM
beta 2 - agonist radioligand
binding
Ref. 0020
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H](-)CGP 12177 (0.3 nM)
0.15 nM
alprenolol (50 µM)
ICI 118551 (IC 50 : 0.8 nM)
Joseph, S.S. et al. (2004) Naun.-Sch. Arch. Pharm., 369: 525-532.
beta 2
cellul ar
Ref. 1976
Ref. 1977
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control isoproterenol (0.1 µM)
Reference isoproterenol (EC 50 : 0.83 nM)
Antagonist effect Stimulant isoproterenol (3 nM)
Reference ICI 118551 (IC 50 : 6 nM)
Baker, J.G. (2005) Brit. J. Pharmacol., 144: 317-322.
cAMP modulation (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5
log [agonist] (M)
isoproterenol
salbutamol
salmeterol
denopamine
100
50
0
-11 -10 -9 -8 -7 -6 -5
log [antagonist] (M)
ICI 118551
CGP 20712A
SR 59230A
propranolol
beta 2 - inverse agonist effect
cellul ar
Ref. 2407
Q 3 weeks
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Control
ICI 118551 (1 µM)
Reference ICI 118551 (EC 50 : 3.8 nM)
[Solvent] must be kept ≤ 0.3%
Baker, J.G. et al. (2003) Mol. Pharmacol., 64: 1357-1369.
-12 -11
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
beta 2
tissue
Source
guinea-pig trachea
(precontracted with 0.1 µM carbachol)
Agonist salbutamol (pD 2 = 7.7)
Antagonist ICI 118551 (pA 2 = 9.1)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
tension (% of control)
100
50
0
ICI 118551
none
3 nM
10 nM
30 nM
Ref. 0299
Q 4 weeks
[Solvent] must be kept ≤ 0.1%
O’Donell, S.R. and Wanstall, J.C. (1979) Naun.-Sch.Arch. Pharm.,308: 183-190.
-10 -9 -8 -7 -6 -5
log [agonist] (M)
beta 3 - antagonist radioligand
binding
Ref. 0227
Q 3 weeks
Included in:
BioPrint ® profile
Source
Ligand
Kd
Non specific
Reference
SK-N-MC cells (endogenous)
[ 125 I]CYP (0.6 nM) (+ 0.1 µM (-)propranolol)
0.7 nM
(-)propranolol (1 mM)
cyanopindolol (IC 50 : 37 nM)
Curran, P.K. and Fishman, P.H. (1996) Cell Signal., 8: 355-364.
specific binding (% of control)
100
50
0
-10 -9 -8 -7 -6 -5 -4 -3
log [drug] (M)
cyonopindolol
(-)propranolol
ICI 118551
atenolol

adrenergic ❚
21
beta 3
cellul ar
Ref. 2189
Ref. 0020
Q 3 weeks
Agonist effect
Antagonist effect
Source
SK-N-MC cells (endogenous)
Measured product cAMP
Detection method HTRF
Agonist effect Control isoproterenol (100 µM)
Reference isoproterenol (EC 50 : 2.7 µM)
Antagonist effect Stimulant isoproterenol (5 µM)
Reference cyanopindolol (IC 50 : 300 nM)
Curran, P.K. and Fishman, P.H. (1996) Cell signal., 8: 355-364.
[Solvent] must be kept 0.3%
Cerep
services
Receptors
[GPCRs]
beta 3
tissue
Ref. 0300
Q 4 weeks
Source
rat colon (precontracted with 30 mM KCl)
Agonist isoproterenol (pD 2 = 6.6)
Antagonist (-)cyanopindolol (pA 2 = 8.8)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
McLaughlin, D.P. and Macdonald, A. (1990) Brit. J. Pharmacol., 101: 569-574.
tension (% of control)
100
50
(-)cyanopindolol
none
0.1 µM
0
1 µM
10 µM
-10 -9 -8 -7 -6 -5 -4 -3
log [agonist] (M)
Ion
channels
Transporters
❚ Angiotensin II
Kinases
AT 1 - antagonist radioligand
binding
Ref. 0024
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (HEK-293 cells)
[ 125 I][Sar 1 ,Ile 8 ]-AT-II (0.05 nM)
0.05 nM
angiotensin-II (10 µM)
saralasin (IC 50 : 0.63 nM)
Le, M.T. et al. (2005) Eur. J. Pharmacol., 513: 35-45.
specific binding (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5
log [drug] (M)
saralasin
ZD 7155
angiotensin-II
PD 123319
Epigenetic &
DNA-related
enzymes
Other
enzymes
AT 1
cellul ar
Ref. 1912
Ref. 1913
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (HEK-293 cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control angiotensin-II (100 nM)
Reference angiotensin-II (EC 50 : 0.85 nM)
Antagonist effect Stimulant angiotensin-II (3 nM)
Reference saralasin (IC 50 : 16.8 nM)
Martin, M.M. et al. (2001) Mol. Endocrinol. 15: 281-293.
Ca 2+ mobilization (% of control)
100
50
0
-12 -11
-10 -9 -8 -7 -6 -5
log [agonist] (M)
angiotensin-II
angiotensin-I
CGP 42112A
100
[Solvent] must be kept ≤ 0.1%
50
0
-11 -10 -9 -8 -7
-12 -6
log [antagonist] (M)
saralasin
ZD 7255
[Sar 1 ,leu 8 ]-AT-II
PD 123319
Specialized
cellular
assays
Standard
profiles
AT 1
tissue
Ref. 0301
Q 4 weeks
Source
rabbit aorta
Agonist angiotensin-II (pD 2 = 8.9)
Antagonist saralasin (pA 2 = 9.7)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Pendleton, G.G. et al. (1989) J. Pharmacol. Exp. Ther., 248: 637-643.
tension (% of max.)
-12 -11
-12 -11
-12 -11
100-12 -11
-10 -9 -8 -7
-10 -9 -8 -7
50
-10 -9 -8 -7 -6 -5
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
0
-11 -10
-10 -9 -8 -7
log [agonist] (M)
-11 -10 -9 -8 -7 -6 -5 -4 -3
-9 -8 -7 -6 -5 -4
saralasin
none
3 nM
10 nM
30 nM
Testing
conditions
Ordering
information
-11 -10
-9 -8 -7 -6 -5 -4
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Assay developed in 2010 New assay conditions Human Q Standard turnaround time
Assay list
& index

22 in vitro pharmacology 2011 catalog
❚ angiotensin II
AT 2 - agonist radioligand
binding
Ref. 0026
Q 3 weeks
Included in:
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (HEK-293 cells)
[ 125 I]CGP 42112A (0.01 nM)
0.01 nM
angiotensin-II (1 µM)
angiotensin-II (IC 50 : 0.14 nM)
Tsuzuki, S., et al. (1994) Biochem. Biophys. Res. Commun., 200: 1449-1454.
❚ Apelin
APJ (apelin) - agonist radioligand
binding
Ref. 2154
Q 3 weeks
Included in:
BioPrint ® profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 125 I](Glp 65 ,Nle 75 ,Tyr 77 )-apelin-13 (0.03 nM)
0.06 nM
apelin-13 (1 µM)
apelin-13, TFA (IC 50 : 0.2 nM)
Katugampola, S.D. et al. (2001) Brit. J. Pharmacol., 132: 1255-1260.
APJ (apelin)
cellul ar
Ref. 2844 Agonist effect
Ref. 2850 Antagonist effect
Q 3 weeks
❚ BOMBESIN
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control apelin-13 (30 nM)
Reference apelin-13 (EC 50 : 0.07 nM)
Antagonist effect Stimulant apelin-13 (1 nM)
Reference unavailable
Medhurst, A.D. et al. (2003) J. Neurochem., 84: 1162-1172.
❚ For Atrial natriuretic peptide and Benzodiazepine assays, see page 83
BB (non-selective) - agonist radioligand
Source
rat cerebral cortex
Ligand
[ 125 I][Tyr 4 ]bombesin (0.01 nM)
binding
Kd
0.71 nM
Ref. 0030
Non specific bombesin (1 µM)
Q 3 weeks
Reference bombesin (IC 50 : 0.205 nM)
Included in:
High-throughput profile
Guark, S. et al. (1993) Eur. J. Pharmacol., 240: 177-184.
BB 1 - agonist radioligand
Source
human recombinant (CHO cells)
Ligand
[ 125 I][Tyr 4 ]bombesin (0.1 nM)
binding
Kd
0.1 nM
Ref. 2193
Non specific neuromedin B (1 µM)
Q 3 weeks
Reference neuromedin B (IC 50 : 0.04 nM)
Included in:
Organ safety profile
Ryan, R.R. et al. (1999) J. Pharmacol. Exp. Ther., 290: 1202-1211.

-12 -11 -10 -9 -8 -7 -6 -5 -4 -3
bombesin ❚
23
BB 1
cellul ar
Ref. 2846
Ref. 2852
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control neuromedin B (10 nM)
Reference neuromedin B (EC 50 : 0.007 nM)
Antagonist effect Stimulant neuromedin B (0.1 nM)
Reference PD 168368 (IC 50 : 200 nM)
Mason, S. et al. (2002) Eur. J. Pharmacol., 438: 25-34.
[Solvent] must be kept 0.1%
Cerep
services
Receptors
[GPCRs]
BB 1
tissue
Ref. 0303
Q 4 weeks
Source
rat urinary bladder
Agonist bombesin (pD 2 = 7.9)
Antagonist not available
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Rouissi, N. et al. (1991) Brit. J. Pharmacol., 103: 1141-1147.
tension (% of max.)
100
50
0
-9 -7
-10 -8
log [agonist] (M)
Ion
channels
Transporters
BB 2 - agonist radioligand
Source
human recombinant (HEK-293 cells)
Ligand
[ 125 I][Tyr 4 ]bombesin (0.04 nM)
binding
Kd
0.04 nM
Ref. 1986
Non specific bombesin (1 µM)
Q 3 weeks
Reference GRP (IC 50 : 0.041 nM)
Included in:
Organ safety profile
Ashnood, V. et al. (1998) Bio. Med. Chem. Lett., 8: 2589-2594.
specific binding (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5
log [drug] (M)
GRP
bombesin
neuromedin B
ICI 216,140
Kinases
Epigenetic &
DNA-related
enzymes
BB 2
cellul ar
Ref. 1915
Ref. 1916
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (HEK-293 cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control GRP (3 nM)
Reference GRP (EC 50 : 0.015 nM)
Antagonist effect Stimulant GRP (0.1 nM)
Reference ICI 216,140 (IC 50 : 510 nM)
Mason, S. et al. (2002) Eur. J. Pharmacol., 438: 25-34.
Ca 2+ mobilization (% of control)
100
100
50
50
0
0
-13 -12 -11 -10 -9 -8 -7
-9 -8 -7 -6 -5
log [agonist] (M)
log [antagonist] (M)
GRP
ICI 216,140
Bn(6-14)
bombesin
neuromedin B
[Solvent] must be kept ≤ 0.1%
Other
enzymes
Specialized
cellular
assays
BB 3 - agonist radioligand
binding
Ref. 0472
Q 3 weeks
Included in:
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 125 I]Bn(6-14) (0.1 nM)
0.16 nM
Bn(6-14) (1 µM)
Bn(6-14) (IC 50 : 8.5 nM)
Mantey, S.A. et al. (1997) J. Biol. Chem., 272: 26062-26071.
-11 -10
-12 -11
-12 -11
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7
-10 -9 -8 -7
-12 -11
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
-11 -10 -9 -8 -7 -6 -5 -4 -3
-13 -12
-11 -10 -9 -8 -7
Standard
profiles
Testing
conditions
BB 3
cellul ar
Ref. 1319
Ref. 1764
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control Bn(6-14) (1 µM)
Reference Bn(6-14) (EC 50 : 9.7 nM)
Antagonist effect Stimulant Bn(6-14) (30 nM)
Reference unavailable
Weber, D. et al. (2003) J. Med. Chem., 46: 1918-1930.
Ca 2+ mobilization (% of control)
100
50
0
-10
-9 -8 -7 -6 -5
log [agonist] (M)
Bn(6-14)
bombesin
neuromedin B
GRP
[Solvent] must be kept ≤ 0.1%
antagonist effect:
no graph available
Ordering
information
Assay list
& index
-11 -10
-9 -8 -7 -6 -5 -4
-12 -11
-10 -9 -8 -7
-11 -10
-9 -8 -7 -6 -5 -4

24 in vitro pharmacology 2011 catalog
❚ bradykinin
B 1 - agonist radioligand
binding
Ref. 1189
Q 3 weeks
Included in:
Diversity profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]desArg 10 -KD (0.35 nM)
0.085 nM
desArg 9 [Leu 8 ]-BK (10 µM)
desArg 10 -KD (IC 50 : 0.77 nM)
Jones, C. et al. (1999) Eur. J. Pharmacol., 374: 423-433.
specific binding (% of control)
100
50
0
-12
desArg 10 -KD
desArg 9 [Leu 8 ]-BK
desArg 9 -BK
-11 -10 -9 -8 -7 -6 -5
log [drug] (M)
B 1
cellul ar
Ref. 1108
Ref. 1109
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control LysdesArg 9 -BK (30 nM)
Reference LysdesArg 9 -BK (EC 50 : 0.81 nM)
Antagonist effect Stimulant LysdesArg 9 -BK (3 nM)
Reference LysdesArg 9 [Leu 8 ]-BK (IC 50 : 3 nM)
Simpson, P.B. et al. (2000) Eur. J. Pharmacol., 392: 1-9.
Ca 2+ mobilization (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5
-10 -9 -8 -7 -6 -5 -4
log [agonist] (M)
LysdesArg 9 -BK
desArg 9 -BK
Lys-BK
bradykinin
100
[Solvent] must be kept ≤ 0.1%
50
0
log [antagonist] (M)
LysdesArg 9 -[Leu 8 ]-BK
desArg 9 -[Leu 8 ]-BK
[desArg 10 ]-HOE140
NPC 567
B 1
tissue
Ref. 0935
Q 4 weeks
Source
human umbilical vein
Agonist LysdesArg 9 -BK (pD 2 = 8.5)
Antagonist LysdesArg 9 -[Leu 8 ]-BK (pA 2 = 7.8)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Gobeil, F et al. (1996) Brit. J. Pharmacol., 118: 289-294.
tension (% of max.)
-12 -11
-11 -10 -9 -8 -7 -6 -5 -4
-12 -11 -10 -9 -8 -7
100
-11 -10 -9 -8 -7 -6 -5 -4
-10 -9 -8 -7
-12 -11 50 -10 -9 -8 -7 -6 -5
LysdesArg9-[Leu8]
-10 -9 -8 -7 -6 -5 -4
-BK
none
30 nM
100 nM
0
300 nM
-10 -9 -8 -7 -6 -5
log [agonist] (M)
B 1
tissue
Ref. 0304
Q 4 weeks
Source
rabbit aorta (endothelium-denuded)
Agonist desArg 9 -BK (pD 2 = 7.3)
Antagonist desArg 9 -[Leu 8 ]-BK (pA 2 = 7.3)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Rhaleb, N.-E. et al. (1990) Brit. J. Pharmacol., 99: 445-448.
tension (% of max.)
100
50
0
-9 -8 -7 -6 -5
log [agonist] (M)
desArg 9-[Leu8]-BK
none
0.1 µM
0.3 µM
1 µM
B 2 - agonist radioligand
binding
Ref. 0033
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]bradykinin (0.2 nM)
0.32 nM
bradykinin (1 µM)
NPC 567 (IC 50 : 18 nM)
Pruneau, D. et al. (1998) Brit. J. Pharmacol., 125: 365-372.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5
log [drug] (M)
NPC 567
HOE 140
bradykinin
desArg 9 -BK
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Assay developed in 2010 New assay conditions Human Q Standard turnaround time

adykinin ❚
25
B 2
cellul ar
Ref. 1263
Ref. 1743
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control bradykinin (10 nM)
Reference bradykinin (EC 50 : 0.009 nM)
Antagonist effect Stimulant bradykinin (0.1 nM)
Reference HOE 140 (IC 50 : 85 nM)
Simpson, P.B. et al. (2000) Eur. J. Pharmacol., 392: 1-9.
Ca 2+ mobilization (% of control)
100
50
0
-13-12-11-10 -9 -8 -7 -6 -5 -4
log [agonist] (M)
bradykinin
desArg 9 -BK
kallidin
desArg 10 -KD
100
[Solvent] must be kept ≤ 0.1%
50
0
-12-11 -10 -9 -8 -7 -6 -5 -4
log [antagonist] (M)
HOE 140
NPC 567
LysdesArg 9 [Leu 8 ]-BK
bradyzide
Cerep
services
Receptors
[GPCRs]
B 2
tissue
Ref. 0623
Q 4 weeks
Source
human umbilical vein
Agonist bradykinin (pD 2 = 8.5)
Antagonist HOE 140 (pA 2 = 8.9)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Gobeil, F et al. (1996) Brit. J. Pharmacol., 118: 289-294.
-12 -11
-12 -11
-12 -11 -10 -9 -8 -7
-11 -10 -9 -8 -7 -6 -5 -4
-10 -9 -8 -7
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
Ion
channels
Transporters
-11 -10 -9 -8 -7 -6 -5 -4
B 2
tissue
Ref. 0305
Q 4 weeks
Source
rabbit jugular vein
Agonist [Hyp 3 ,Tyr(Me) 8 ]-BK (pD 2 = 9.3)
Antagonist D-Arg[Hyp 3 ,D-Phe 7 ,Leu 8 ]-BK (pA 2 = 8.4)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Rhaleb, N.-E et al. (1990) Brit. J. Pharmacol., 99: 445-448.
tension (% of max.)
100
50
0
-11 -10 -9 -8 -7
log [agonist] (M)
D-Arg[Hyp3,D-Phe7,
Leu8]-BK
none
10 nM
30 nM
100 nM
Kinases
Epigenetic &
DNA-related
enzymes
Other
enzymes
❚ calcitonin
Specialized
cellular
assays
CT (calcitonin) - agonist radioligand
Source
T47D cells (endogenous)
Ligand
[ 125 I]calcitonin (salmon) (0.05 nM)
Kd
0.045 nM
Non specific calcitonin (salmon) (0.5 µM)
binding
Reference calcitonin (salmon) (IC 50 : 0.5 nM)
Ref. 0728
Q 6 weeks
Kurokawa, M. et al. (1991) J. Endocrinol., 130: 321-326.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5
log [drug] (M)
calcitonin
salmon
human
eel
porcine
Standard
profiles
Testing
conditions
CT (calcitonin)
cellul ar
Ref. 1964 Agonist effect
Ref. 1965 Antagonist effect
Q 3 weeks
Source
T47D cells (endogenous)
Measured product cAMP
Detection method HTRF
Agonist effect Control human calcitonin (1 µM)
Reference human calcitonin (EC 50 : 1.9 nM)
Antagonist effect Stimulant human calcitonin (30 nM)
Reference salmon calcitonin 8-32
(IC 50 : 25.8 nM)
Zimmermann, U. et al. (1997) J. Endocrinol., 155: 423-431.
cAMP modulation (% of control)
100
50
0
log [agonist] (M)
human calcitonin
salmon calcitonin
amylin
hCGRPα
100
-11 -10 -9 -8 -7 -6 -5 -11 -10 -9 -8 -7 -6 -5
[Solvent] must be kept ≤ 0.3%
50
0
log [antagonist] (M)
salmon calcitonin 8-32
CGRP 8-37
Ordering
information
Assay list
& index
-11 -10
-9 -8 -7 -6 -5 -4
-12 -11
-10 -9 -8 -7
-11 -10
-9 -8 -7 -6 -5 -4

26 in vitro pharmacology 2011 catalog
❚ calcitonin gene-related peptide
CGRP - agonist radioligand
binding
Ref. 0373
Q 3 weeks
Included in:
High-throughput profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 125 I]hCGRPa (0.03 nM)
0.06 nM
hCGRPa (1 µM)
hCGRPa (IC 50 : 0.032 nM)
Aiyar, N. et al. (1996) J. Biol. Chem., 271: 11325-11329.
specific binding (% of control)
100
50
0
-13 - 12 -11 - 10 -9 -8 -7 -6
log [drug] (M)
hCGRPα
CGRP 8-37
adrenomedullin
human calcitonin
CGRP
cellul ar
Ref. 1621
Ref. 1622
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control hCGRPa (10 nM)
Reference hCGRPa (EC 50 : 0.11 nM)
Antagonist effect Stimulant hCGRPa (0.3 nM)
Reference hCGRPa (8-37) (IC 50 : 26 nM)
Aiyar, N. et al. (1996) J. Biol. Chem., 271: 11325-11329.
cAMP modulation (% of control)
100
50
0
-13 -12 -11 -10 -9 -8 -7 -6 -5
log [agonist] (M)
hCGRPα
adrenomedullin
amylin
100
50
0
-10 -9 -8 -7 -6 -5
log [antagonist] (M)
hCGRPα (8-37)
CGRP
tissue
Ref. 0306
Q 4 weeks
Source
rat vas deferens (field-stimulated)
Agonist hCGRPa (pD 2 = 9)
Antagonist hCGRPa (8-37) (pA 2 = 6.3)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Longmore, J. et al. (1994) Eur. J. Pharmacol., 265: 53-59.
tension (% of control)
-12 -11
-12 -11
-11 -10
-12 -11
100
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7
-10 -9 -8 -7
50 -10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
0
-11 -10
-11 -10 -9 -8 -7
log [agonist] (M)
-9 -8 -7 -6 -5 -4
hCGRPα (8-37)
none
1 µM
❚ calcium sensing
CaS
cellul ar
Ref. 2144
Ref. 2146
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (HEK-293 cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control neomycin (100 µM)
Reference neomycin (EC 50 : 11 µM)
Antagonist effect Stimulant neomycin (30 µM)
Reference unavailable
Quinn, S.J. et al. (1997) Am. J. Physiol., 273: 1315-1323.
Ca 2+ mobilization (% of control)
100
50
0
-7 -6 -5 -4 -3 -2
log [agonist] (M)
neomycin
gadolinium (III) chloride hexahydrate
spermine
CaCl2
[Solvent] must be kept ≤ 0.1%
antagonist effect:
no graph available
-11 -10
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7
❚ For radioligand binding assays, how should I choose between the agonist and the antagonist models when both are
-11 -10 -9 -8 -7 -6 -5 -4
available?
-12 -11 -10 -9 -8 -7 -6 -5 -4 -3
-12 -11 -10 -9 -8 -7
For some binding assays two models are available using either agonist or antagonist as radioligand.
-12 -11 -10 -9 -8 -7 -6 -5
G-protein-coupled receptors have both high-affinity and low-affinity states that are bound differently by agonists and antagonists. Whereas
-10 -9 -8 -7 -6 -5 -4
the antagonists bind with an equal affinity to both affinity states, agonists bind poorly to the low affinity state of the receptor. Therefore,
it is advisable to use an antagonist radioligand to evaluate the binding of antagonists knowing that this may fail to reveal the binding
of agonists. On the other hand, an assay using an agonist radioligand is suitable to evaluate both agonists and antagonists.
The testing of a compound in both assays and the comparison of its competition curves against each radioligand may provide information
about its functional activity at the receptor.
-12 -11

27
❚ cannabinoid
CB 1 - agonist radioligand
binding
Ref. 0036
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]CP 55940 (0.5 nM)
3.5 nM
WIN 55212-2 (10 µM)
CP 55940 (IC 50 : 0.58 nM)
specific binding (% of control)
100
50
0
-11 - 10 -9 -8 -7 -6 -5
CP 55940
WIN 55212-2
AM 281
anandamide
log [drug] (M)
Rinaldi-Carmona, M. et al. (1996) J. Pharmaco. Exp. Ther., 278: 871-878.
[CUSTOM OFFER] at cerebellum model (Ref. 0035), please contact us at customresearch@cerep.com
Cerep
services
Receptors
[GPCRs]
Ion
channels
CB 1
cellul ar
Ref. 1744
Ref. 1745
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control CP 55940 (100 nM)
Reference CP 55940 (EC 50 : 0.8 nM)
Antagonist effect Stimulant CP 55940 (10 nM)
Reference AM 281 (IC 50 : 100 nM)
Felder, C.C. et al. (1995) Mol. Pharmacol., 48: 443-450.
cAMP modulation (% of control)
100
100
50
50
0
0
-12 -11 -10 -9 -8 -7 -6 -5 -4 -12 -11 -10 -9 -8 -7 -6 -5
log [agonist] (M)
log [antagonist] (M)
CP 55940
AM 281
WIN 55212-2
AM 251
anandamide
AM 630
JWH 133
[Solvent] must be kept ≤ 0.3%
Transporters
Kinases
CB 1 - inverse agonist effect
cellul ar
Ref. 2378
Q 3 weeks
Source
Measured product cAMP
Detection method HTRF
human recombinant (CHO cells)
Control
AM 281 (3 µM)
Reference AM 281 (EC 50 : 33.2 nM)
[Solvent] must be kept ≤ 0.3%
Ross, R.A. et al. (1999) Brit. J. Pharmacol., 126: 665-672.
-12 -11
-11 -10
-12 -11
-12 -11
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7
-10 -9 -8 -7
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
-11 -10
-9 -8 -7 -6 -5 -4
Epigenetic &
DNA-related
enzymes
Other
enzymes
CB 1
tissue
Ref. 0307
Q 4 weeks
Source
mouse vas deferens (field-stimulated)
Agonist CP 55940 (pD 2 = 8.7)
Antagonist AM 281
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Rinaldi-Carmona, M. et al. (1994) FEBS Lett., 350: 240-244.
tension (% of control)
100
50
0
-9 -7 -6
-10 -8
log [agonist] (M)
CP 55940
anandamide
Specialized
cellular
assays
Standard
profiles
CB 2 - agonist radioligand
binding
Ref. 0037
Q 3 weeks
Included in:
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]WIN 55212-2 (0.8 nM)
1.5 nM
WIN 55212-2 (5 µM)
WIN 55212-2 (IC 50 : 1 nM)
Munro, S. et al. (1993) Nature, 365: 61-65.
Testing
conditions
Ordering
information
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Assay developed in 2010 New assay conditions Human Q Standard turnaround time
Assay list
& index

28 in vitro pharmacology 2011 catalog
❚ cannabinoid
CB 2
cellul ar
Ref. 0647
Ref. 1746
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control WIN 55212-2 (100 nM)
Reference WIN 55212-2 (EC 50 : 0.67 nM)
Antagonist effect Stimulant WIN 55212-2 (10 nM)
Reference AM 630 (IC 50 : 5.2 µM)
Felder, C.C. et al. (1995) Mol. Pharmacol., 48: 443-450.
cAMP modulation (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5 -4
log [agonist] (M)
WIN 55212-2
CP 55940
anandamide
JWH 133
100
[Solvent] must be kept ≤ 0.3%
50
0
-8 -7 -6 -5 -4 -3
log [antagonist] (M)
AM 630
AM 281
AM 251
CB 2 - inverse agonist effect
cellul ar
Ref. 2379
Q 3 weeks
Source
Measured product cAMP
Detection method HTRF
Control
Reference
[Solvent] must be kept ≤ 0.3%
human recombinant (CHO cells)
AM 630 (10 µM)
AM 630 (EC 50 : 74.5 nM)
Ross, R.A. et al. (1999) Brit. J. Pharmacol., 126: 665-672.
-12 -11
-12 -11
-11 -10
-12 -11
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7
-10 -9 -8 -7
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
-11 -10
-9 -8 -7 -6 -5 -4
-13 -12 -11 -10 -9 -8 -7 -6
-12 -11 -10 -9 -8 -7 -6 -5 -4
❚ See other cannabinoid assays, page 103
❚ chemokines
CCR1 - agonist radioligand
binding
Ref. 0361
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (HEK-293 cells)
[ 125 I]MIP-1a (0.01 nM)
0.02 nM
MIP-1a (100 nM)
MIP-1a (IC 50 : 0.04 nM)
Neote, K. et al. (1993) Cell, 72: 415-425.
specific binding (% of control)
100
50
0
-14 -13
-12 -11 -10 -9 -8 -7 -6
log [drug] (M)
MIP-1α
MIP-1β
MCP-1
RANTES
(CCL5)
CCR1
cellul ar
Ref. 2502 Agonist effect
Ref. 2503 Antagonist effect
Q 3 weeks
Source
human recombinant (CHO cells)
Measured product impedance
Detection method cellular dielectric spectroscopy
Agonist effect Control MIP-1a (100 nM)
Reference MIP-1a (EC 50 : 0.2 nM)
Antagonist effect Stimulant MIP-1a (1 nM)
Reference J 113863 (IC 50 : 7.5 nM)
Chou, C.C. et al. (2002) Brit. J. Pharmacol., 137: 663-675.
α
[Solvent] must be kept 0.1%
CCR2 - agonist radioligand
binding
Ref. 0362
Q 3 weeks
Included in:
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (HEK-293 cells)
[ 125 I]MCP-1 (0.01 nM)
0.007 nM
MCP-1 (10 nM)
MCP-1 (IC 50 : 0.022 nM)
Berkhout, T.A. et al. (1997) J. Biol. Chem., 272: 16404-16413.
specific binding (% of control)
100
50
MCP-1
MCP-4
MIP-1α
0
MIP-1β
-13 -12 -11 -10 -9 -8 -7 -6
log [drug] (M)

29
chemokines ❚
CCR2
cellul ar
Ref. 2497
Ref. 2501
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control MCP-1 (100 nM)
Reference MCP-1 (EC 50 : 2.7 nM)
Antagonist effect Stimulant MCP-1 (30 nM)
Reference MIP-II (IC 50 : 47 nM)
Jarnagin, K. et al. (1999) Biochemistry, 38: 16167-16177.
α
β
Cerep
services
Receptors
[GPCRs]
CCR3 - agonist radioligand
Source
human recombinant (K562 cells)
Ligand
[ 125 I]eotaxin (0.1 nM)
Kd
0.73 nM
Non specific eotaxin (0.3 µM)
binding
Reference eotaxin (IC 50 : 0.34 nM)
Ref. 0481
Q 3 weeks
White, J.R. et al. (1997) J. Leuk. Biol., 62: 667-675.
specific binding (% of control)
100
50
0
log [drug] (M)
-12 -11 -10 -9 -8 -7 -6
[Solvent] must be kept 0.3%
eotaxin
Ion
channels
Transporters
CCR3
cellul ar
Ref. 2136
Ref. 2137
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product impedance
Detection method cellular dielectric spectroscopy
Agonist effect Control eotaxin 2 (100 nM)
Reference eotaxin 2 (EC 50 : 5.9 nM)
Antagonist effect Stimulant eotaxin 2 (10 nM)
Reference J 113863 (IC 50 : 5 nM)
Daugherty, B.L. et al. (1996) J. Exp. Med. 183: 2349-2354.
α
[Solvent] must be kept 0.1%
Kinases
Epigenetic &
DNA-related
enzymes
CXCR2 (IL-8B) - agonist radioligand
binding
Ref. 0419
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (HEK-293 cells)
[ 125 I]IL-8 (0.025 nM)
0.022 nM
IL-8 (30 nM)
IL-8 (IC 50 : 0.115 nM)
White, J.R. et al. (1998) J. Biol. Chem., 273: 10095-10098.
specific binding (% of control)
100
50
IL-8
IL-2
IL-1α
0
GRO-α
-12 -11 -10 -9 -8 -7
log [drug] (M)
Other
enzymes
Specialized
cellular
assays
CXCR2 (IL-8B)
cellul ar
Ref. 2480 Agonist effect
Ref. 2482 Antagonist effect
Q 3 weeks
Source
human recombinant (HEK-293 cells)
Measured product impedance
Detection method cellular dielectric spectroscopy
Agonist effect Control IL-8 (100 nM)
Reference IL-8 (EC 50 : 1.2 nM)
Antagonist effect Stimulant IL-8 (3 nM)
Reference SB 225002 (IC 50 : 4.9 µM)
White, J.R. et al. (1998) J. Biol. Chem., 273: 10095-10098.
α
β
[Solvent] must be kept 0.1%
Standard
profiles
Testing
conditions
CXCR4 - agonist radioligand
binding
Ref. 1022
Q 3 weeks
Included in:
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 125 I]SDF-1a (0.01 nM)
0.046 nM
SDF-1a (10 nM)
SDF-1a (IC 50 : 0.018 nM)
Zhou, N. et al. (2002) J. Biol. Chem., 277:17476-17485.
α
Ordering
information
Assay list
& index

30 in vitro pharmacology 2011 catalog
❚ chemokines
CXCR4
cellul ar
Ref. 2464 Agonist effect
Ref. 2466 Antagonist effect
Q 3 weeks
Source
human recombinant (CHO cells)
Measured product impedance
Detection method cellular dielectric spectroscopy
Agonist effect Control SDF-1a (30 nM)
Reference SDF-1a (EC 50 : 0.43 nM)
Antagonist effect Stimulant SDF-1a (1 nM)
Reference MIP-II (IC 50 : 55 nM)
Zhou, Y. et al. (2002) J. Biol. Chem., 277: 49481-49487.
α
[Solvent] must be kept 0.1%
❚ cholecystokinin
CCK 1 (CCK A ) - agonist radioligand
binding
Ref. 0039
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 125 I]CCK-8s (0.08 nM)
0.24 nM
CCK-8s (1 µM)
CCK-8s (IC 50 : 0.1 nM)
Bignon, E. et al. (1999) J. Pharmacol. Exp. Ther., 289: 742-751.
specific binding (% of control)
100
50
CCK-8s
SR 27897B
LY 225910
0
devazepide
-12 -11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
CCK 1 (CCK A )
cellul ar
Ref. 1876
Ref. 1877
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control CCK-8s (10 µM)
Reference CCK-8s (EC 50 : 52 nM)
Antagonist effect Stimulant CCK-8s (300 nM)
Reference devazepide (IC 50 : 0.98 nM)
Wu, V. et al. (1997) J. Biol. Chem., 272: 9037-9042.
cAMP modulation (% of control)
100
50
0
-9 -8 -7 -6 -5 -4 -11 -10 -9 -8 -7 -6 -5 -4
log [agonist] (M)
CCK-8s
CCK-8ns
100
50
0
log [antagonist] (M)
devazepide
lorglumide
LY 225910
CCK 1 (CCK A )
tissue
Ref. 0308
Q 4 weeks
Source
guinea-pig gall bladder
Agonist CCK-8s (pD 2 = 7.5)
Antagonist SR 27897 (pA 2 = 9.5)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Gully, D. et al. (1993) Eur. J. Pharmacol., 232: 13-19.
tension (% of max.)
-12 -11
-12 -11
-11 -10
-12 -11
100
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7
-10 -9 -8 -7
50 -10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
0
-13
-12 -11
-11 -10
log [agonist] (M)
-10 -9 -8
-9 -8 -7 -6 -5 -4
-12 -11 -10 -9 -8 -7 -6 -5 -4
-10 -9 -8 -7 -6 -5
SR 27897
none
1 nM
3 nM
10 nM
CCK 2 (CCK B ) - agonist radioligand
binding
Ref. 0041
Q 3 weeks
Included in:
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 125 I]CCK-8s (0.08 nM)
0.054 nM
CCK-8s (1 µM)
CCK-8s (IC 50 : 0.098 nM)
Lee, Y.-M. et al. (1993) J. Biol. Chem., 268: 8164-8169.
specific binding (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5
log [drug] (M)
CCK-8s
LY 225910
SR 27897B
devazepide
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Assay developed in 2010 New assay conditions Human Q Standard turnaround time

31
cholecystokinin ❚
CCK 2 (CCK B )
cellul ar
Ref. 1878 Agonist effect
Ref. 1879 Antagonist effect
Q 3 weeks
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control CCK-8s (100 nM)
Reference CCK-8s (EC 50 : 1.4 nM)
Antagonist effect Stimulant CCK-8s (30 nM)
Reference YM022 (IC 50 : 1.8 nM)
Wu, S.V. et al. (1999) Mol. Pharmacol., 55: 795-803.
cAMP modulation (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -11 -10 -9 -8 -7 -6 -5 -4
log [agonist] (M)
CCK-8s
CCK-8ns
CCK-4
gastrin
100
50
0
log [antagonist] (M)
YM022
lorglumide
LY 225910
Cerep
services
Receptors
[GPCRs]
-11 -10
-9 -8 -7 -6 -5 -4
❚ complement 5a
-12 -11
-12 -11
-12 -11
-10 -9 -8 -7
-10 -9 -8 -7
-10 -9 -8 -7 -6 -5
-13
-12 -11
-11 -10
-10 -9 -8
-9 -8 -7 -6 -5 -4
-12 -11 -10 -9 -8 -7 -6 -5 -4
Ion
channels
C5a - agonist radioligand
Source
human recombinant (HEK-293 cells)
Ligand
[ 125 I]hC5a (0.02 nM)
Kd
0.089 nM
Non specific hC5a (0.1 µM)
binding
Reference hC5a (IC 50 : 0.46 nM)
Ref. 0042
Q 4 weeks
Gerard, N.P. and Gerard, C. (1991) Nature, 349: 614-617.
-9 -8 -7 -6 -5
-10 -4
specific binding (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6
log [drug] (M)
hC5a
hC5a inhibitory
sequence
fMLP
Transporters
Kinases
C5a
cellul ar
Ref. 2089
Ref. 2098
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (HEK-293 cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control hC5a (100 nM)
Reference hC5a (EC 50 : 0.29 nM)
Antagonist effect Stimulant hC5a (10 nM)
Reference unavailable
Jacobs, A.A. et al. (1995) J. Leuk. Biol., 57: 679-686.
[Solvent] must be kept 0.3%
Epigenetic &
DNA-related
enzymes
Other
enzymes
❚
corticotropin releasing factor
Specialized
cellular
assays
CRF 1 - agonist radioligand
binding
Ref. 1467
Q 3 weeks
Included in:
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 125 I]sauvagine (0.075 nM)
0.12 nM
sauvagine (0.5 µM)
sauvagine (IC 50 : 0.3 nM)
Palchaudhuri, M.R. et al. (1998) Eur. J. Biochem., 258: 78-84.
Standard
profiles
Testing
conditions
CRF 1
cellul ar
Ref. 0504
Ref. 0505
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control ovine CRF (100 nM)
Reference ovine CRF (EC 50 : 1.8 nM)
Antagonist effect Stimulant ovine CRF (10 nM)
Reference astressin (IC 50 : 24.7 nM)
Chen, R. et al. (1993) Proc. Natl. Acad. Sci. USA, 90: 8967-8971.
cAMP modulation (% of control)
100
50
0
-12 -11 -10 -9 -8 -7
log [agonist] (M)
ovine CRF
sauvagine
human urocortin 1
100
50
0
-10 -9 -8 -7 -6
log [antagonist] (M)
astressin
α-helical-CRF
Ordering
information
Assay list
& index
-11 -10
-9 -8 -7 -6 -5 -4
-12 -11
-10 -9 -8 -7
-13 -12 -11 -10 -9 -8
-8 -6 -5 -11 -10 -9 -7 -4

32 in vitro pharmacology 2011 catalog
❚ corticotropin releasing factor
CRF 2a - agonist radioligand
Source
human recombinant (HEK-293 cells)
Ligand
[ 125 I]sauvagine (0.1 nM)
binding
Kd
0.05 nM
Ref. 2036
Non specific urocortine (1 µM)
Q 3 weeks
Reference sauvagine (IC 50 : 1.1 nM)
Included in:
Organ safety profile
Dautzenberg, F.M. et al. (2001) J. Pharmacol. Exp. Ther., 296: 113-120.
α
CRF 2a
cellul ar
Ref. 2085
Ref. 2086
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (HEK-293 cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control human CRF (1 µM)
Reference human CRF (EC 50 : 11 nM)
Antagonist effect Stimulant human CRF (30 nM)
Reference astressin (IC 50 : 22 nM)
Dautzenberg, F.M. et al. (2001) J. Pharmacol. Exp. Ther., 296: 113-120.
cAMP modulation (% of control)
100
50
0
-11 -10 -9 -8 -7 -6
-10 -9 -8 -7 -6 -5
log [agonist] (M)
human CRF
sauvagine
urocortin
urotensin-I
100
[Solvent] must be kept ≤ 0.3%
50
0
log [antagonist] (M)
astressin
α-helical-CRF
-11 -10 -9 -8 -7 -6 -5 -4
❚ For Cytokine assays, see "Other receptors", page 83
-12 -11 -10 -9 -8 -7
-13 -12 -11 -10 -9 -8
-11 -10 -9 -8 -7 -6 -5 -4
-12 -11
-12 -11
-10 -9 -8 -7
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
-12 -11 -10 -9 -8 -7 -6 -5 -4
❚ dopamine
D 1 - antagonist radioligand
binding
Ref. 0044
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]SCH 23390 (0.3 nM)
0.2 nM
SCH 23390 (1 µM)
SCH 23390 (IC 50 : 0.242 nM)
specific binding (% of control)
100
50
0
-13 -12 -11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
Zhou, Q.-Y. et al. (1990) Nature, 347: 76-80.
[CUSTOM OFFER] rat striatum model (Ref. 0043), please contact us at customresearch@cerep.com
SCH 23390
A68930
dopamine
SKF 82958
D 1
cellul ar
Ref. 1685
Ref. 1686
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control dopamine (10 µM)
Reference dopamine (EC 50 : 58 nM)
Antagonist effect Stimulant dopamine (300 nM)
Reference SCH 23390 (IC 50 : 1.7 nM)
Zhou, Q.-Y. et al. (1990) Nature, 347: 76-80.
cAMP modulation (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5
log [agonist] (M)
dopamine
7-OH-DPAT
A68930
bromocriptyne
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5 -4 -3
log [antagonist] (M)
SCH 23390
L-741,626
L-745,870
GR 103691
D 1
tissue
Ref. 0309
Q 4 weeks
Source
rabbit splenic artery
(precontracted with 0.1 µM U-46619)
Agonist SKF 82958 (pD 2 = 6.7)
Antagonist SCH 23390
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Zanzottera, D. et al. (1998) Brit. J. Pharmacol., 123: 730-736.
tension (% of control)
-13
100
50 -12 -11 -10 -9 -8 -7 -6 -5
-12 -11 -10 -9 -8 -7 -6 -5 -4 -3
-9 -8 -7 -6 -5
-10 -4
0
-8 -7 -6 -5
log [agonist] (M)

33
dopamine ❚
D 2S - antagonist radioligand
binding
Ref. 0046
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (HEK-293 cells)
[ 3 H]methylspiperone (0.3 nM)
0.15 nM
(+)butaclamol (10 µM)
(+)butaclamol (IC 50 : 1.64 nM)
Grandy, D.K. et al. (1989) Proc. Natl. Acad. Sci. USA, 86: 9762-9766.
specific binding (% of control)
100
50
0
-10 -9 -8 -7 -6 -5 -4 -3
log [drug] (M)
(+)butaclamol
dopamine
SCH 23390
clozapine
Cerep
services
Receptors
[GPCRs]
D 2S - agonist radioligand
binding
Ref. 1322
Q 3 weeks
Included in:
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (HEK-293 cells)
[ 3 H]7-OH-DPAT (1 nM)
0.68 nM
butaclamol (10 µM)
7-OH-DPAT (IC 50 : 0.95 nM)
Grandy, D.K. et al. (1989) Proc. Natl. Acad. Sci. USA, 86: 9762-9766.
specific binding (% of control)
100
50
0
7-OH-DPAT
dopamine
spiperone
haloperidol
-10 -9 -8 -7 -6
log [drug] (M)
Ion
channels
Transporters
D 2S
cellul ar
Ref. 2566
Ref. 2569
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (HEK-293 cells)
Measured product impedance
Detection method cellular dielectric spectroscopy
Agonist effect Control dopamine (3 µM)
Reference dopamine (EC 50 : 2.1 nM)
Antagonist effect Stimulant dopamine (30 nM)
Reference butaclamol (IC 50 : 30.5 nM)
Payne, S.L. et al. (2002) J. Neurochem., 82: 1106-1117.
[Solvent] must be kept 0.1%
Kinases
Epigenetic &
DNA-related
enzymes
D 2L - antagonist radioligand
Source
human recombinant (HEK-293 cells)
Ligand
[ 3 H]methylspiperone (0.3 nM)
Kd
0.1 nM
Non specific butaclamol (10 µM)
binding
Reference butaclamol (IC 50 : 2.9 nM)
Ref. 1405
Q 3 weeks
Hall, D.A. and Strange, P.G. (1997) Brit. J. Pharmacol., 121: 731-736.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4 -3
log [drug] (M)
butaclamol
dopamine
clozapine
SCH 23390
Other
enzymes
Specialized
cellular
assays
D 2
tissue
Ref. 0310
Q 4 weeks
Source
rabbit ear artery (field-stimulated)
Agonist quinpirole (pD 2 = 7.3)
Antagonist (-)sulpiride (pA 2 = 7.5)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Steinsland, O.S. and Hieble, J.P. (1978) Science, 199: 443-445.
tension (% of control)
100
50
0
-9 -8 -7 -6
log [agonist] (M)
(-)sulpiride
none
30 nM
100 nM
300 nM
Standard
profiles
Testing
conditions
D 3 - antagonist radioligand
binding
Ref. 0048
Q 3 weeks
Included in:
High-throughput profile
Diversity profile
BioPrint ® profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]methylspiperone (0.3 nM)
0.085 nM
(+)butaclamol (10 µM)
(+)butaclamol (IC 50 : 1.4 nM)
Mackenzie, R.G. et al. (1994) Eur. J. Pharmacol., 266: 79-85.
Ordering
information
Assay list
& index

34 in vitro pharmacology 2011 catalog
❚ dopamine
D 3 - agonist radioligand
Source
human recombinant (CHO cells)
Ligand
[ 3 H]7-OH-DPAT (0.15 nM)
binding
Kd
0.5 nM
Ref. 1660
Non specific (+)butaclamol (10 µM)
Q 3 weeks
Reference 7-OH-DPAT (IC 50 : 1.5 nM)
Included in:
Organ safety profile
Ricci, A. et al. (1998) J. Neuroimmunol., 92: 191-195.
specific binding (% of control)
100
50
0
7-OH-DPAT
dopamine
SCH 23390
(+)butaclamol
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
D 3
cellul ar
Ref. 0683
Ref. 0684
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control dopamine (300 nM)
Reference dopamine (EC 50 : 1.5 nM)
Antagonist effect Stimulant dopamine (10 nM)
Reference (+)butaclamol (IC 50 : 78 nM)
Missale, C. et al. (1998) Physiol. Rev., 78: 189-225.
cAMP modulation (% of control)
100
50
0
-9 -8 -7 -6 -5
-11 -10 -10 -9 -8 -7 -6 -5
-12 -11 -4
log [agonist] (M)
dopamine
7-OH-DPAT
bromocryptine
PD 168077
100
50
0
log [antagonist] (M)
(+)butaclamol
SCH 23390
L741626
spiperone
D 4.4 - antagonist radioligand
binding
Ref. 0049
Q 3 weeks
Included in:
High-throughput profile
Diversity profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]methylspiperone (0.3 nM)
0.19 nM
(+)butaclamol (10 µM)
clozapine (IC 50 : 46.5 nM)
Van Tol, H.H.M. et al. (1992) Nature, 358: 149-152.
specific binding (% of control)
-12 -11
-12 -11
-11 -10
100-12 -11
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7
-10 -9 -8 -7
50
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
0
-11 -10
log [drug] (M)
-9 -8 -7 -6 -5
-10 -9 -8 -7 -6 -5 -4 -3
clozapine
haloperidol
(+)butaclamol
SCH 23390
D 4.4
cellul ar
Ref. 1699
Ref. 1700
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control dopamine (300 nM)
Reference dopamine (EC 50 : 7.9 nM)
Antagonist effect Stimulant dopamine (100 nM)
Reference clozapine (IC 50 : 350 nM)
Missale, C. et al. (1998) Physiol. Rev., 78: 189-225.
cAMP modulation (% of control)
100
50
0
-11 -10 -9 -8 -7 -6
log [agonist] (M)
dopamine
quimpirole
PD 168077
7-OH-DPAT
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5
log [antagonist] (M)
clozapine
haloperidol
SCH 23390
spiperone
D 5 - antagonist radioligand
Source
human recombinant (GH4 cells)
Ligand
[ 3 H]SCH 23390 (0.3 nM)
binding
Kd
0.25 nM
Ref. 0050
Non specific SCH 23390 (10 µM)
Q 3 weeks
Reference SCH 23390 (IC 50 : 0.39 nM)
Included in:
High-throughput profile
Sunahara, R.K. et al. (1991) Nature, 350: 614-619.
specific binding (% of control)
-1350
-12 -11 -10 -9 -8 -7 -6 -5
-11 -10 -9 -8 -7 -6
-9 -8 -7 -6 -5
-10 -4
-12 -11 -10 -9 -8 -7 -6
-12 -11
100
-10 0 -9 -8 -7 -6 -5
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
SCH 23390
(+)butaclamol
clozapine
(-)sulpiride
D 5 - agonist radioligand
Source
human recombinant (GH4 cells)
Ligand
[ 3 H]dopamine (7.5 nM)
binding
Kd
3.2 nM
Ref. 1733
Non specific SCH 23390 (10 µM)
Q 3 weeks
Reference dopamine (IC 50 : 6.68 nM)
Included in:
Organ safety profile
Sunahara, R.K. et al. (1991) Nature, 350: 614-619.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5
log [drug] (M)
dopamine
SKF 38393
SCH 23390
butaclamol

dopamine ❚
35
D 5
cellul ar
Ref. 1688
Ref. 1689
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (GH4 cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control dopamine (1 µM)
Reference dopamine (EC 50 : 21 nM)
Antagonist effect Stimulant dopamine (50 nM)
Reference SCH 23390 (IC 50 : 0.6 nM)
Sunahara, R.K. et al. (1991) Nature, 350: 614-619.
cAMP modulation (% of control)
100
100
50
50
0
0
-11 -10 -9 -8 -7 -6 -5 -4 -3 -12 -11 -10 -9 -8 -7 -6 -5 -4 -3
log [agonist] (M)
log [antagonist] (M)
dopamine
SCH 23390
SKF 88393
L-741,626
7-OH-DPAT
L-745,870
bromocryptine
GR 103691
❚ See other dopamine assays, page 104
Cerep
services
Receptors
[GPCRs]
-13
-12 -11 -10 -9 -8 -7 -6 -5
-11 -10 -9 -8 -7 -6
Ion
channels
-9 -8 -7 -6 -5
-10 -4
❚ endothelin
-12 -11 -10 -9 -8 -7 -6
-12 -11
-10 -9 -8 -7 -6 -5
-12 -11 -10 -9 -8 -7 -6 -5 -4 -3
Transporters
ET A - agonist radioligand
binding
Ref. 0054
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 125 I]endothelin-1 (0.03 nM)
0.03 nM
endothelin-1 (100 nM)
endothelin-1 (IC 50 : 0.038 nM)
specific binding (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
endothelin-1
endothelin-3
sarafotoxin S6c
BQ-788
Buchan, K.W. et al. (1994) Brit. J. Pharmacol., 112: 1251-1257.
[CUSTOM OFFER] rat A-10 cells model (Ref. 0053), please contact us at customresearch@cerep.com
Kinases
Epigenetic &
DNA-related
enzymes
ET A
cellul ar
Ref. 1264
Ref. 2257
Q 3 weeks
Agonist effect
Antagonist effect
Source
SK-N-MC cells (endogenous)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control endothelin-1 (100 nM)
Reference endothelin-1 (EC 50 : 1.1 nM)
Antagonist effect Stimulant endothelin-1 (10 nM)
Reference BQ-123 (IC 50 : 0.37 nM)
Heinroth-Hoffmann, I. et al. (1998) Brit. J. Pharmacol., 125: 1202-1211.
Ca 2+ mobilization (% of control)
100
100
50
50
0
0
-11 -10 -9 -8 -7 -6 -5 -4 -11 -10 -9 -8 -7 -6 -5 -4
log [agonist] (M)
log [antagonist] (M)
endothelin-1
BQ-123
endothelin-3
FR 139317
sarafotoxin S6c
BQ-788
BQ-3020
PD 142,893
[Solvent] must be kept ≤ 0.1%
Other
enzymes
Specialized
cellular
assays
ET A
Source
rat aorta (endothelium-denuded)
100-12 -11 -10 -9 -8 -7
-11 -10 -9 -8 -7 -6 -5 -4
-11 -10 -9 -8 -7 -6 -5 -4
tissue
Ref. 0311
Q 4 weeks
Agonist endothelin-1 (pD 2 = 8.9)
Antagonist BQ-123
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Warner, T.D. et al. (1993) Brit. J. Pharmacol., 110: 777-782.
tension (% of max.)
-12 -11
-12 -11
-10 -9 -8 -7
50
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
0
-10 -9 -8 -7
log [agonist] (M)
Standard
profiles
Testing
conditions
ET B - agonist radioligand
binding
Ref. 0056
Q 3 weeks
Included in:
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 125 I]endothelin-1 (0.03 nM)
0.04 nM
endothelin-1 (0.1 µM)
endothelin-3 (IC 50 : 0.0154 nM)
specific binding (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5
log [drug] (M)
endothelin-3
endothelin-1
sarafotoxin S6c
BQ-788
Fuchs, S. et al. (2001) Mol. Med., 7: 115-124.
[CUSTOM OFFER] rat cerebellum model (Ref. 0055), please contact us at customresearch@cerep.com
Ordering
information
Assay list
& index

36 in vitro pharmacology 2011 catalog
❚ endothelin
ET B
cellul ar
Ref. 1762
Ref. 1763
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control endothelin-1 (10 nM)
Reference endothelin-1 (EC 50 : 0.12 nM)
Antagonist effect Stimulant endothelin-1 (1 nM)
Reference BQ-788 (IC 50 : 42 nM)
Hayasaki-Kafiwara, Y. et al. (1999) Brit. J. Pharmacol., 127: 1415-1421.
[Solvent] must be kept 0.3%
ET B
tissue
Ref. 0312
Q 4 weeks
Source
rabbit pulmonary artery
(endothelium-denuded)
Agonist sarafotoxin 6c (pD 2 = 9.1)
Antagonist BQ-788
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Fukuroka, T. et al. (1994) Brit. J. Pharmacol., 113: 336-338.
tension (% of max.)
100
50
0
-10 -9 -8
log [agonist] (M)
❚ n-formyl peptide
fMLP - agonist radioligand
Source
human recombinant (CHO cells)
Ligand
[ 3 H]fMLP (0.4 nM)
Kd
0.32 nM
Non specific fMLP (1 µM)
binding
Reference fMLP (IC 50 : 0.93 nM)
Ref. 0407
Q 4 weeks
Quehenberger, O. et al. (1993) J. Biol. Chem., 268: 18167-18175.
fMLP
cellul ar
Ref. 2090
Ref. 2097
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control fMLP (10 nM)
Reference fMLP (EC 50 : 0.24 nM)
Antagonist effect Stimulant fMLP (3 nM)
Reference unavailable
Wenzel-Seifert, K. et al. (1998) J. Biol. Chem., 273: 24181-24189.
[Solvent] must be kept 0.3%
For some binding assays two models are available using either agonist or antagonist as radioligand.
❚ For radioligand binding assays, how should I choose between the agonist and the antagonist models when both are
available?
G-protein-coupled receptors have both high-affinity and low-affinity states that are bound differently by agonists and antagonists. Whereas
the antagonists bind with an equal affinity to both affinity states, agonists bind poorly to the low affinity state of the receptor. Therefore,
it is advisable to use an antagonist radioligand to evaluate the binding of antagonists knowing that this may fail to reveal the binding
of agonists. On the other hand, an assay using an agonist radioligand is suitable to evaluate both agonists and antagonists.
The testing of a compound in both assays and the comparison of its competition curves against each radioligand may provide information
about its functional activity at the receptor.

37
Cerep
services
❚ Free fatty acid
Receptors
[GPCRs]
FFA1 (GPR40)
cellul ar
Ref. 2665 Agonist effect
Ref. 2669 Antagonist effect
Q 3 weeks
Source
human recombinant (HEK-293 cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control linoleic acid (100 µM)
Reference linoleic acid (EC 50 : 2.2 µM)
Antagonist effect Stimulant linoleic acid (10 µM)
Reference unavailable
Briscoe, C.P. et al. (2006) Brit. J. Pharmacol., 148: 619-628.
[Solvent] must be kept 0.1%
Ion
channels
Transporters
FFA2 (GPR43)
cellul ar
Ref. 2710 Agonist effect
Ref. 2714 Antagonist effect
Q 3 weeks
FFA3 (GPR41)
cellul ar
Ref. 2819 Agonist effect
Ref. 2823 Antagonist effect
Q 3 weeks
Source
human recombinant (HEK-293 cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control sodium acetate (3 mM)
Reference sodium acetate (EC 50 : 350 µM)
Antagonist effect Stimulant sodium acetate (1 mM)
Reference unavailable
Le Poul, E. et al. (2003) J. Biol. Chem., 278: 25481-25489.
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control sodium propionate (1 mM)
Reference sodium propionate (EC 50 : 6 µM)
Antagonist effect Stimulant sodium propionate (30 µM)
Reference unavailable
Le Poul, E. et al. (2003) J. Biol. Chem., 278: 25481-25489.
[Solvent] must be kept 0.3%
Kinases
Epigenetic &
DNA-related
enzymes
Other
enzymes
Specialized
cellular
assays
selected cerep assays
proximity assay (SPA) and centrifugation. All formats utilize a radiolabeled ligand and a source of receptor (membranes, soluble/purified).
❚ binding assays
Binding assays are developed according to the competition assay principle. There are three assay formats used: filtration, scintillation
Large batches of cells, from which prepared membranes are frozen and stored, are produced in-house. Membrane preparations are
quality controlled before use.
❚ cellular Functional GPCR assays
Functional GPCR assays are cell-based assays to measure agonist-like, inverse agonist, antagonist and modulator activity of compounds.
Various technologies are used: TR-FRET to determine cAMP concentration and IP1 levels, real time fluorescence to monitor calcium flux,
cellular dielectric spectroscopy to measure impedance modulation. Large batches of cells, from which whole cells are frozen and stored
for functional assays, are produced in-house. Cells are quality controlled before use. A novel patented host cell line was designed and
constructed for Gi protein coupled receptors.
❚ tissue bioassays
Tissue bioassays are functional assays designed to evaluate the agonist and antagonist activities of compounds at various receptors and
ion channels in whole tissues. The tissues used are isolated from contractile cardiac and smooth muscles of the cardiovascular, respiratory,
gastrointestinal and urogenital tracts of rodents, rabbit or human. The selected tissues are assayed in organ bath systems to record the
contractile activity in conditions as selective as possible to avoid any potential interaction with other receptors known to be present in
the tissue used.
Standard
profiles
Testing
conditions
Ordering
information
Assay list
& index

38 in vitro pharmacology 2011 catalog
❚ GABA
GABA B(1b) - antagonist radioligand
binding
Ref. 0885
Q 3 weeks
Included in:
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]CGP 54626 (1 nM)
1 nM
CGP 52432 (100 µM)
CGP 54626 (IC 50 : 1.2 nM)
Green, A. et al. (2000) Brit. J. Pharmacol., 131: 1766-1774.
GABA B
cellul ar
Ref. 2525
Ref. 0885
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product impedance
Detection method cellular dielectric spectroscopy
Agonist effect Control 3-APMPA (100 µM)
Reference 3-APMPA (EC 50 : 327 nM)
Antagonist effect Stimulant 3-APMPA (3 µM)
Reference CGP 54626 (IC 50 : 74 nM)
Hirst, W.D. et al. (2003) Biochem. Pharmacol., 65: 1103-1113.
[Solvent] must be kept 0.1%
GABA B
tissue
Ref. 0315
Q 4 weeks
Source
guinea-pig ileum (field-stimulated)
Agonist (R+)-baclofen (pD 2 = 4.9)
Antagonist CGP 52432
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Kerr, D.I.B. et al. (1988) Neurosci. Lett., 92: 92-96.
tension (% of control)
100
50
0
-7 -6 -5 -4 -3
log [agonist] (M)
❚ See other GABA assays pp. 84, 97, and 104
❚ Galanin
galanin (non-selective) - agonist radioligand
Source
rat striatum
Ligand
[ 125 I]galanin (0.05 nM)
Kd
0.1 nM
Non specific galanin (30 nM)
binding
Reference galanin (IC 50 : 0.17 nM)
Ref. 0061
Q 4 weeks
Ogren, S.O. et al. (1993) Eur. J. Pharmacol., 242: 59-64.
specific binding (% of control)
100
50
0
-12 -11 -10 -9 -8
log [drug] (M)
galanin
GAL 1 - agonist radioligand
binding
Ref. 0062
Q 3 weeks
Included in:
High-throughput profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (HEK-293 cells)
[ 125 I]galanin (0.1 nM)
0.1 nM
galanin (1 µM)
galanin (IC 50 : 0.35 nM)
Sullivan, K.A. et al. (1997) Biochem. Biophys. Res. Commun., 233: 823-828.
specific binding (% of control)
100
50
0
galanin
M15
-11 -10 -9 -8 -7 -6
log [drug] (M)

39
galanin ❚
GAL 2 - agonist radioligand
binding
Ref. 0410
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 125 I]galanin (0.05 nM)
0.63 nM
galanin (1 µM)
galanin (IC 50 : 0.92 nM)
Bloomquist, B.T. et al. (1998) Biochem. Biophys. Res. Commun., 243: 474-479.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6
log [drug] (M)
galanin
C7
M15
Cerep
services
Receptors
[GPCRs]
GAL 2
cellul ar
Ref. 1292
Ref. 1893
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control human galanin (100 nM)
Reference human galanin (EC 50 : 0.29 nM)
Antagonist effect Stimulant human galanin (1 nM)
Reference unavailable
Fathi, Z. et al. (1998) Mol. Br. Research, 58: 156-169.
Ca 2+ mobilization (% of control)
100
50
0
-11 -10
log [agonist] (M)
human galanin
porcine galanin
M40
C7
-9 -8 -7 -6 -5
[Solvent] must be kept ≤ 0.1%
antagonist effect:
no graph available
Ion
channels
Transporters
-11 -10
-9 -8 -7 -6 -5 -4
❚ Glucagon
-12 -11
-12 -11
-12 -11
-10 -9 -8 -7
-10 -9 -8 -7
-10 -9 -8 -7 -6 -5
-11 -10
-9 -8 -7 -6 -5 -4
-12 -11 -10 -9 -8 -7 -6 -5 -4 -3
Kinases
GLP-1 - agonist radioligand
Source
bTC6 cells (endogenous)
Ligand
[ 125 I]GLP-1(7-36) (0.025 nM)
Kd
0.1 nM
Non specific GLP-1(7-36) (1 µM)
binding
Reference exendin-4 (IC 50 : 0.19 nM)
Ref. 0228
Q 3 weeks
Fehmann, H.C. et al. (1994) Peptides, 15: 453-456.
-9 -8 -7 -6 -5
-10 -4
Epigenetic &
DNA-related
enzymes
Other
enzymes
GLP-1
cellul ar
Ref. 2181
Ref. 2182
Q 3 weeks
Agonist effect
Antagonist effect
Source
bTC6 cells (endogenous)
Measured product cAMP
Detection method HTRF
Agonist effect Control GLP-1(7-37) (100 nM)
Reference GLP-1(7-37) (EC 50 : 0.18 nM)
Antagonist effect Stimulant GLP-1(7-37) (1 nM)
Reference exendin-3(9-39) (IC 50 : 4 nM)
Runge, S. et al. (2003) Brit. J. Pharmacol., 138: 787-794.
cAMP modulation (% of control)
100
100
50
50
0
0
-12 -11 -10 -9 -8 -7 -6 -13 -12 -10 -13 -11 -9 -8 -7 -6
log [agonist] (M)
log [antagonist] (M)
GLP-1(7-37)
exendin-3(9-39)
GLP-2(1-33)
[des-His
1 ,Glu 9 ]-
exendin-4
glucagon amide
glucagon
L168,049
[Solvent] must be kept ≤ 0.3%
Specialized
cellular
assays
Standard
profiles
GLP-2
cellul ar
Ref. 1993
Ref. 1998
Q 3 weeks
Agonist effect
Antagonist effect
Source
Measured product cAMP
Detection method HTRF
human recombinant (CHO cells)
Agonist effect Control GLP-2(1-34) (10 nM)
Reference GLP-2(1-34) (EC 50 : 0.04 nM)
Antagonist effect Stimulant GLP-2(1-34) (0.3 nM)
Reference unavailable
Munroe, D.G. et al. (1999) Proc. Nat. Acad. Sc. USA, 96: 1569-1573.
cAMP modulation (% of control)
-12 -11
-12 -11
-11 -10
-12 -11
100
50
-7 -6 -5 -9 -8 -4
-10 -9 -8 -7
-10 -9 -8 -7
-10 -9 -8 -7 -6 -5
0
-11 -10
-9 -8 -13 -7 -12 -11 -6 -10 -5
-10 -4-8 -9 -7 -6 -5
log [agonist] (M)
GLP-2(1-34)
GLP-2(1-33)
glucagon
GLP-1
[Solvent] must be kept ≤ 0.3%
-9 -8 -7 -6 -5 -4
-13 -12 -11 -10 -9 -8 -7 -6
antagonist effect:
no graph available
-12 -11 -10 -9 -8 -7 -6 -5 -4
Testing
conditions
Ordering
information
-11 -10
-9 -8 -7 -6 -5 -4
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
-12 -11
-10 -9 -8 -7
-12 -11 -10 -9 -8 -7
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
-12 -11 -10 -9 -8 -7 -6 -5
Assay developed in 2010 New assay conditions Human Q Standard turnaround time
-9 -8 -7 -6 -5
-10 -4
-11 -10
-9 -8 -7 -6 -5 -4
-12 -11 -10 -9 -8 -7 -6 -5 -4 -3
Assay list
& index

40 in vitro pharmacology 2011 catalog
❚ glucagon
glucagon - agonist radioligand
binding
Ref. 1407
Q 3 weeks
Included in:
BioPrint ® profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 125 I]glucagon (0.025 nM)
0.069 nM
glucagon (1 µM)
glucagon (IC 50 : 1.2 nM)
Chicchi, G.G. et al. (1997) J. Biol. Chem., 272: 7765-7769.
glucagon
cellul ar
Ref. 1839 Agonist effect
Ref. 1840 Antagonist effect
Q 3 weeks
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control glucagon (100 nM)
Reference glucagon (EC 50 : 0.21 nM)
Antagonist effect Stimulant glucagon (1 nM)
Reference [des-His 1 -Glu 9 ]-glucagon amide
(IC 50 : 2.14 µM)
Chichi, G.G. et al. (1997) J. Biol. Chem., 272: 7765-7769.
cAMP modulation (% of control)
100
50
0
-12 -11
-10 -9 -8 -7 -6 -5
log [agonist] (M)
glucagon
GLP-1(7-37)
GLP-2(1-34)
100
[Solvent] must be kept ≤ 0.3%
50
0
-9 -8 -7 -6 -5 -4 -3
log [antagonist] (M)
[des-His 1 ,Glu 9 ]-
glucagon amide
L168,049
exendin-3(9-39)
secretin
cellul ar
Ref. 2012
Ref. 2014
Q 3 weeks
Agonist effect
Antagonist effect
Source
Measured product cAMP
Detection method HTRF
human recombinant (CHO cells)
Agonist effect Control human secretin (3 nM)
Reference human secretin (EC 50 : 0.07 nM)
Antagonist effect Stimulant human secretin (0.3 nM)
Reference unavailable
Ishihara, T. et al. (1991) Embo. J., 10: 1635-1641.
-12 -11
-12 -11
-11 -10
-12 -11
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7
-10 -9 -8 -7
-10 -9 -8 -7 -6 -5
-11 -10
-9 -8 -7 -6 -5
-10 -4
[Solvent] must be kept 0.3%
-9 -8 -7 -6 -5 -4
-13 -12 -11 -10 -9 -8 -7 -6
-12 -11 -10 -9 -8 -7 -6 -5 -4
❚ For Glutamate and Glycine assays, see "Other receptors", pp. 86 and 87
❚ Glycoprotein hormone
TSH
cellul ar
Ref. 2237
Ref. 2239
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (HEK-293 cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control TSH (10 µM)
Reference TSH (EC 50 : 27.8 nM)
Antagonist effect Stimulant TSH (100 nM)
Reference unavailable
Rapoport, B. et al. (1998) Endocrinol. Rev., 19: 673-716.
[Solvent] must be kept 0.3%
❚ Gonadotrophin-releasing hormone
GnRH (LH-RH) - agonist radioligand
Source
rat pituitary gland
Ligand
[ 125 I][D-Trp 6 ]-LH-RH (0.05 nM)
Kd
0.1 nM
Non specific [D-Trp 6 ]-LH-RH (1 µM)
binding
Reference [D-Trp 6 ]-LH-RH (IC 50 : 0.096 nM)
Ref. 0456
Q 4 weeks
Halmos, G. et al. (1996) Proc. Natl. Acad. Sci. USA, 93: 2398-2402.

41
❚ Growth hormone-releasing hormone
Cerep
services
GHRH
cellul ar
Ref. 2236
Ref. 2238
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
50
50
Measured product cAMP
Detection method HTRF
0
0
Agonist effect Control human GHRF(1-29) (10 nM)
Reference human GHRF(1-29) (EC
log [agonist] (M)
50 : 0.3 nM)
human GHRH(1-29)
Antagonist effect Stimulant human GHRF(1-29) (1 nM)
GHRF(1-29)
glucagon
Reference [N-acetyl-Tyr 1 ,D-Arg 2 ]-GHRF
secretin
(IC 50 : 16 nM)
[Solvent] must be kept ≤ 0.3%
Gaudreau, P. et al. (1992) J. Med. Chem., 32: 1864-1869.
cAMP modulation (% of control)
100
-10 -9 -8
-12 -11 -10 -9 -8 -7 -6
-11 -10
-9 -8 -7 -6 -5 -4
100
log [antagonist] (M)
[N-acetyl-Tyr 1 ,D-Arg 2 ]-GHRF
JV-1-36
JV-1-38
[des-His 1 -Glu 9 ]-glucagon amide
❚ For Growth factors assays, see "Other receptors", page 87
Receptors
[GPCRs]
Ion
channels
❚ Histamine
H 1 - antagonist radioligand
binding
Ref. 0870
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (HEK-293 cells)
[ 3 H]pyrilamine (1 nM)
1.7 nM
pyrilamine (1 µM)
pyrilamine (IC 50 : 2.2 nM)
Smit, M.J. et al. (1996) Brit. J. Pharmacol., 117: 1071-1080.
-12 -11
-12 -11
-12 -11
-10 -9 -8 -7
-10 -9 -8 -7
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
specific binding (% of control)
100
50
0
-11 -10
-9 -8 -7 -6 -5 -4
-13 -12 -11 -10 -9 -8 -7 -6
log [drug] (M)
-12 -11 -10 -9 -8 -7 -6 -5 -4
-11 -10 -9 -8 -7 -6 -5 -4 -3
pyrilamine
histamine
cimetidine
Transporters
Kinases
Epigenetic &
DNA-related
enzymes
H 1 - antagonist radioligand
Source
guinea-pig cerebellum
Ligand
[ 3 H]pyrilamine (0.5 nM)
Kd
0.37 nM
Non specific triprolidine (100 µM)
binding
Reference pyrilamine (IC 50 : 0.39 nM)
Ref. 0077
Q 3 weeks
Dini, S. et al. (1991) Agents and Actions, 33: 181-184.
α
Other
enzymes
Specialized
cellular
assays
H 1
cellul ar
Ref. 2542
Ref. 2543
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
human recombinant (HEK-293 cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control histamine (10 µM)
Reference histamine (EC 50 : 47 nM)
Antagonist effect Stimulant histamine (300 nM)
Reference pyrilamine (IC 50 : 5.7 nM)
Miller, T.R. et al. (1999) J. Biomol. Screen., 4: 249-258.
α
[Solvent] must be kept 0.1%
Standard
profiles
Testing
conditions
H 1
tissue
Ref. 0316
Q 4 weeks
Source
guinea-pig trachea
Agonist 2-PEA (pD 2 = 4.9)
Antagonist pyrilamine (pA 2 = 9.4)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Rappen-Cremer, E. et al. (1989) Agents and Actions, 28: 218-223.
tension (% of max.)
100
50
pyrilamine
none
1 nM
0
3 nM
10 nM
-7 -6 -5 -4
log [agonist] (M)
Ordering
information
Assay list
& index

42 in vitro pharmacology 2011 catalog
❚ histamine
H 2 - antagonist radioligand
binding
Ref. 1208
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 125 I]APT (0.075 nM)
2.9 nM
tiotidine (100 µM)
cimetidine (IC 50 : 350 nM)
Leurs, R. et al. (1994) Brit. J. Pharmacol., 112: 847-854.
specific binding (% of control)
100
50
0
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
cimetidine
ranitidine
pyrilamine
histamine
H 2 - antagonist radioligand
Source
guinea-pig striatum
Ligand
[ 125 I]APT (0.1 nM)
Kd
0.48 nM
Non specific tiotidine (100 µM)
binding
Reference cimetidine (IC 50 : 1 µM)
Ref. 0079
Q 3 weeks
Ruat, M. et al. (1990) Proc. Natl. Acad. Sci. USA, 87: 1658-1662.
specific binding (% of control)
100
50
0
cimetidine
ranitidine
pyrilamine
histamine
-9 -8 -7 -6 -5 -4 -3 -2
log [drug] (M)
H 2
cellul ar
Ref. 1695
Ref. 1696
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control histamine (3 µM)
Reference histamine (EC 50 : 376 nM)
Antagonist effect Stimulant histamine (1 µM)
Reference cimetidine (IC 50 : 1.2 µM)
Leurs, R. et al. (1994) Brit. J. Pharmacol., 112: 847-854.
cAMP modulation (% of control)
100
50
0
-10 -4
-9 -8 -7 -6 -5 -9 -8 -7 -6 -5 -4
log [agonist] (M)
histamine
imetit
dimaprit
(R)α-Me-histamine
100
[Solvent] must be kept ≤ 0.3%
50
0
log [antagonist] (M)
cimetidine
tiotidine
ranitidine
H 2 - inverse agonist effect
cellul ar
Ref. 2380
Q 3 weeks
Source
Measured product cAMP
Detection method HTRF
Control
Reference
[Solvent] must be kept ≤ 0.3%
human recombinant (CHO cells)
ranitidine (100 µM)
ranitidine (EC 50 : 985 nM)
Smit, M.J. et al. (1996) Proc. Natl. Acad. Sci. USA, 93: 6802-6807.
-13
-12 -11 -10 -9 -8 -7 -6 -5
-11 -10 -9 -8 -7 -6
-9 -8 -7 -6 -5
-10 -4
-12 -11 -10 -9 -8 -7 -6
-12 -11
-10 -9 -8 -7 -6 -5
-12 -11 -10 -9 -8
-7 -6 -5 -4 -3
H 2
tissue
Ref. 0317
Q 4 weeks
Source
guinea-pig right atrium
Agonist dimaprit (pD 2 = 5.9)
Antagonist cimetidine (pA 2 = 6.7)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Krielaart, M.J. et al. (1990) Agents and Actions, 31: 23-35.
frequency (% of max.)
100
50
0
-8 -7 -6 -5 -4
-9
log [agonist] (M)
cimetidine
none
1 µM
3 µM
10 µM
H 3 - agonist radioligand
binding
Ref. 1332
Q 3 weeks
Included in:
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]N α -Me-histamine (1 nM)
0.32 nM
(R)α-Me-histamine (1 µM)
(R)α-Me-histamine (IC 50 : 2.56 nM)
Lovengerg, T.W. et al. (1999) Mol. Pharmacol., 55: 1101-1107.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
(R)α-Me-histamine
histamine
cimetidine
pyrilamine

43
H 3 - agonist radioligand
Source
rat cerebral cortex
Ligand
[ 3 H]N α -Me-histamine (1 nM)
Kd
0.68 nM
Non specific (R)α-Me-histamine (5 µM)
binding
Reference (R)α-Me-histamine (IC 50 : 3.1 nM)
Ref. 0080
Q 3 weeks
Arrang, J.M. et al. (1990) Eur. J. Pharmacol., 188: 219-227.
specific binding (% of control)
histamine ❚
100
50
(R)α-Me-histamine
histamine
pyrilamine
0
cimetidine
-10 -9 -8 -7 -6
log [drug] (M)
Cerep
services
Receptors
[GPCRs]
H 3
cellul ar
Ref. 1800
Ref. 1801
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control histamine (10 µM)
Reference histamine (EC 50 : 30 nM)
Antagonist effect Stimulant histamine (1 µM)
Reference thioperamide (IC 50 : 2.6 µM)
Lim, H.D. et al. (2005) J. Pharmacol. Exp. Ther., 314: 1310-1321.
cAMP modulation (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4
log [agonist] (M)
histamine
R(α)-Me-histamine
imetit
dimaprit
100
50
0
-10 -9 -8 -7 -6 -5 -4 -3
log [antagonist] (M)
thioperamide
pyrilamine
cimetidine
tiotidine
Ion
channels
Transporters
H 4 - agonist radioligand
binding
Ref. 1384
Q 3 weeks
Included in:
BioPrint ® profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (HEK-293 cells)
[ 3 H]histamine (10 nM)
7.6 nM
imetit (1 µM)
imetit (IC 50 : 4.28 nM)
Liu, C. et al. (2001) J. Pharmacol. Exp. Ther., 299: 121-130.
specific binding (% of control)
-11 -10 -9 -8 -7 -6 -5 -4
-1350
-12 -11 -10 -9 -8 -7 -6 -5
-11 -10 -9 -8 -7 -6
-9 -8 -7 -6 -5
-10 -4
-12 -11 -10 -9 -8 -7 -6
-12 -11
100
-10 0 -9 -8 -7 -6 -5
-11 -10 -9 -8 -7 -6 -5 -4 -3
log [drug] (M)
imetit
histamine
-12 -11 -10 -9 -8
(R)α-Me-histamine
-7 -6 -5 -4 -3
cimetidine
Kinases
Epigenetic &
DNA-related
enzymes
H 4
cellul ar
Ref. 2595
Ref. 2599
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (HEK-293 cells)
Measured product impedance
Detection method cellular dielectric spectroscopy
Agonist effect Control histamine (100 µM)
Reference histamine (EC 50 : 13 nM)
Antagonist effect Stimulant histamine (100 nM)
Reference JNJ 7777120 (IC 50 : 34 nM)
Lim, H.D. et al. (2005) J. Pharmacol. Exp. Ther., 314: 1310-1321.
α
[Solvent] must be kept 0.1%
❚ For imidazoline and insulin assays, see "Other receptors",
page 88
Other
enzymes
Specialized
cellular
assays
selected cerep assays
❚ binding assays
Binding assays are developed according to the competition assay principle. There are three assay formats used: filtration, scintillation
proximity assay (SPA) and centrifugation. All formats utilize a radiolabeled ligand and a source of receptor (membranes, soluble/purified).
Large batches of cells, from which prepared membranes are frozen and stored, are produced in-house. Membrane preparations are
quality controlled before use.
❚ cellular Functional GPCR assays
Functional GPCR assays are cell-based assays to measure agonist-like, inverse agonist, antagonist and modulator activity of compounds.
Various technologies are used: TR-FRET to determine cAMP concentration and IP1 levels, real time fluorescence to monitor calcium flux,
cellular dielectric spectroscopy to measure impedance modulation. Large batches of cells, from which whole cells are frozen and stored
for functional assays, are produced in-house. Cells are quality controlled before use. A novel patented host cell line was designed and
constructed for Gi protein coupled receptors.
❚ tissue bioassays
Tissue bioassays are functional assays designed to evaluate the agonist and antagonist activities of compounds at various receptors and
ion channels in whole tissues. The tissues used are isolated from contractile cardiac and smooth muscles of the cardiovascular, respiratory,
gastrointestinal and urogenital tracts of rodents, rabbit or human. The selected tissues are assayed in organ bath systems to record the
contractile activity in conditions as selective as possible to avoid any potential interaction with other receptors known to be present in
the tissue used.
Standard
profiles
Testing
conditions
Ordering
information
Assay list
& index

44 in vitro pharmacology 2011 catalog
❚ Leukotrienes
BLT 1 (LTB 4 ) - agonist radioligand
binding
Ref. 1209
Q 3 weeks
Included in:
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]LTB 4 (0.2 nM)
0.2 nM
LTB 4 (0.2 µM)
LTB 4 (IC 50 : 0.2 nM)
Yokomizo, T. et al. (2001) J. Biol. Chem., 276: 12454-12459.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5
log [drug] (M)
LTB4
LTD4
U75302
BLT 1 (LTB 4 )
cellul ar
Ref. 1245 Agonist effect
Ref. 1837 Antagonist effect
Q 3 weeks
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control LTB 4 (100 nM)
Reference LTB 4 (EC 50 : 1.2 nM)
Antagonist effect Stimulant LTB 4 (10 nM)
Reference unavailable
Yokomizo, T. et al. (2000) J. Exp. Med., 192: 421-431.
Ca 2+ mobilization (% of control)
100
50
0
-11
LTB 4
LTC4
LTD4
-10 -9 -8 -7
log [agonist] (M)
[Solvent] must be kept ≤ 0.1%
antagonist effect:
no graph available
CysLT 1 (LTD 4 ) - agonist radioligand
binding
Ref. 0086
Q 3 weeks
Included in:
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]LTD 4 (0.3 nM)
0.24 nM
LTD 4 (1 µM)
LTD 4 (IC 50 : 0,335 nM)
Martin V. et al. (2001) Biochem. Pharmacol., 62: 1193-1200.
specific binding (% of control)
-12 -11
-12 -11
-11 -10
100
-12 -11
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7
-10 -9 -8 -7
50 -10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
0
-11 -10
-9 -8 -7 -6 -5 -4
-12 -11 -10 -9 -8 -7 -6 -5 -4 -3
-12 -11 -10 -9 -8 -7 -6
log [drug] (M)
LTD4
LTB4
MK 571
CysLT 1 (LTD 4 )
cellul ar
Ref. 1383 Agonist effect
Ref. 1607 Antagonist effect
Q 3 weeks
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control LTD 4 (10 nM)
Reference LTD 4 (EC 50 : 0.33 nM)
Antagonist effect Stimulant LTD 4 (1 nM)
Reference MK 571 (IC 50 : 126 nM)
Sarau, H.M. et al. (1999) Mol. Pharmacol., 56: 657-663.
Ca 2+ mobilization (% of control)
100
50
0
100
50
0
-11 -10 -9 -8 -7 -6 -8 -7 -6
log [agonist] (M)
log [antagonist] (M)
LTD4
MK 571
LTC4
LTB 4
[Solvent] must be kept ≤ 0.1%
CysLT 2 (LTC 4 ) - agonist radioligand
Source
human recombinant (HEK-293 cells)
Ligand
[ 3 H]LTD 4 (1 nM)
Kd
1.5 nM
Non specific LTD 4 (1 µM)
binding
Reference LTC 4 (IC 50 : 7.2 nM)
Ref. 2050
Q 3 weeks
Hui, Y. et al. (2001) J. Biol. Chem., 276: 47489-47495.
specific binding (% of control)
-11 -10 -9 -8 -7 -6 -5 -4
-13 -12 -11 -10 -9 -8 -7 -6 -5
50
-11 -10 -9 -8 -7 -6
-9 -8 -7 -6 -5
-10 -4
-12 -11 -10 -9 -8 -7 -6
-12 -11
100
-100
-9 -8 -7 -6 -5
-12 -11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
LTC4
LTD4
-12 -11 -10 -9 -8
-7 LTB -6 -5 -4 -3
4
MK 571
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Assay developed in 2010 New assay conditions Human Q Standard turnaround time

45
leukotrienes ❚
CysLT 2 (LTC 4 )
cellul ar
Ref. 2051 Agonist effect
Ref. 2052 Antagonist effect
Q 3 weeks
Source
human recombinant (HEK-293 cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control LTC 4 (300 nM)
Reference LTC 4 (EC 50 : 18 nM)
Antagonist effect Stimulant LTC 4 (100 nM)
Reference unavailable
Takasaki, J. et al. (2000) Biochem. Biophys. Res. Commun., 274: 316-322.
Ca 2+ mobilization (% of control)
100
50
0
-11 -10
LTC4
LTD4
LTB4
-9 -8 -7 -6
log [agonist] (M)
[Solvent] must be kept ≤ 0.1%
antagonist effect:
no graph available
Cerep
services
Receptors
[GPCRs]
-11 -10
-9 -8 -7 -6 -5 -4
-12 -11
-10 -9 -8 -7
-11 -10
-9 -8 -7 -6 -5 -4
-12 -11 -10 -9 -8 -7 -6 -5 -4 -3
-12 -11
-12 -11
-10 -9 -8 -7
-10 -9 -8 -7 -6 -5
Ion
channels
-9 -8 -7 -6 -5
-10 -4
❚ Lysophospholipid
Transporters
LPA 1 - agonist radioligand
Source
human recombinant (CHO cells)
❚ lysophosphatidic acid
Ligand
[ 3 H]LPA (2 nM)
binding
Kd
19 nM
Ref. 1468
Non specific LPA (10 µM)
Q 3 weeks
Reference LPA (IC 50 : 42.5 nM)
Included in:
Organ safety profile
An, S. et al. (1997) Biochem. Biophys. Res. Commun., 231: 619-622.
specific binding (% of control)
100
50
0
LPA
phosphatidic acid
SEW 2871
S 1P
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
Kinases
Epigenetic &
DNA-related
enzymes
LPA 2
❚ lysophosphatidic acid
cellul ar
Ref. 3171 Agonist effect
Ref. 3172 Antagonist effect
Q 3 weeks
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control LPA (1 µM)
Reference LPA (EC 50 : 3.5 nM)
Antagonist effect Stimulant LPA (30 nM)
Reference unavailable
Heise, C.E. et al. (2001) Mol. Pharmacol., 60: 1173-1180.
1
[Solvent] must be kept 0.3%
Other
enzymes
Specialized
cellular
assays
LPA 3
❚ lysophosphatidic acid
cellul ar
Ref. 3158 Agonist effect
Ref. 3170 Antagonist effect
Q 3 weeks
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control LPA (1 µM)
Reference LPA (EC 50 : 6.4 nM)
Antagonist effect Stimulant LPA (30 nM)
Reference VPC 32183 (IC 50 : 3.9 µM)
Heise, C.E. et al. (2001) Mol. Pharmacol., 60: 1173-1180.
1
[Solvent] must be kept 0.3%
Standard
profiles
Testing
conditions
S 1 P 1
❚ sphingosine 1-phosphate
cellul ar
Ref. 3269 Agonist effect
Ref. 3271 Antagonist effect
Q 3 weeks
Source
human recombinant (CHO cells)
Measured product impedance
Detection method cellular dielectric spectroscopy
Agonist effect Control S 1 P (300 nM)
Reference S 1 P (EC 50 : 4 nM)
Antagonist effect Stimulant S 1 P (10 nM)
Reference VPC 23019 (IC 50 : 150 nM)
Davis, M.D., et al. (2005) J. Biol. Chem., 11: 9833-9841.
[Solvent] must be kept 0.1%
Ordering
information
Assay list
& index

46 in vitro pharmacology 2011 catalog
❚ lysophospholipid
S 1 P 2
❚ sphingosine 1-phosphate
cellul ar
Ref. 2133 Agonist effect
Ref. 2135 Antagonist effect
Q 3 weeks
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control S 1 P (300 nM)
Reference S 1 P (EC 50 : 6.3 nM)
Antagonist effect Stimulant S 1 P (30 nM)
Reference JTE 013 (IC 50 : 27 nM)
Siehler S. and Guerini, D. (2006) J. Rec. Sign. Transd., 26: 549-575.
Ca 2+ mobilization (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5
-10 -9 -8 -7 -6 -5
log [agonist] (M)
S 1 P
SEW 2871
phytosphingosine
100
[Solvent] must be kept ≤ 0.1%
50
0
log [antagonist] (M)
JTE 013
VPC 23019
CAY 10444
S 1 P 3
❚ sphingosine 1-phosphate
cellul ar
Ref. 2143 Agonist effect
Ref. 2145 Antagonist effect
Q 3 weeks
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control S 1 P (30 nM)
Reference S 1 P (EC 50 : 1.56 nM)
Antagonist effect Stimulant S 1 P (3 nM)
Reference unavailable
Siehler S. and Guerini, D. (2006) J. Rec. Sign. Transd., 26: 549-575.
Ca 2+ mobilization (% of control)
-12 -11
-12 -11
-11 -10
-12 -11
100
50
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7
-10 -9 -8 -7
-10 -9 -8 -7 -6 -5
0
-11 -10
-9 -8 -12 -11 -7 -10 -6 -9-5
-10 -4-7 -8 -6 -5 -4
log [agonist] (M)
S 1 P
SEW 2871
phytosphingosine
[Solvent] must be kept ≤ 0.1%
-9 -8 -7 -6 -5 -4
antagonist effect:
no graph available
-11 -10
-9 -8 -7 -6 -5 -4
-12 -11
-10 -9 -8 -7
-11 -10
-9 -8 -7 -6 -5 -4
-12 -11 -10 -9 -8 -7 -6 -5 -4 -3
-12 -11
-10 -9 -8 -7
-12 -11
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
❚ melanin concentrating hormone
MCH 1 - agonist radioligand
binding
Ref. 1115
Q 3 weeks
Included in:
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 125 I][Phe 13 ,Tyr 19 ]-MCH (0.1 nM)
1 nM
human MCH (0.1 µM)
human MCH (IC 50 : 0.092 nM)
Mac Donald, D. et al. (2000) Mol. Pharmacol., 58: 217-225.
specific binding (% of control)
100
50
human MCH
0
[Phe 13 -Tyr 19 ]-MCH
salmon MCH
-12 -11 -10 -9 -8 -7 -6
log [drug] (M)
MCH 1
cellul ar
Ref. 1035
Ref. 1036
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control human MCH (300 nM)
Reference human MCH (EC 50 : 2.9 nM)
Antagonist effect Stimulant human MCH (30 nM)
Reference unavailable
Wang, S. et al. (2001) J. Biol. Chem., 276: 34664-34670.
Ca 2+ mobilization (% of control)
100
50
0
-11 -10
log [agonist] (M)
human MCH
[Phe 13 ,Tyr 19 ]-MCH
salmon MCH
-9 -8 -7 -6
[Solvent] must be kept ≤ 0.1%
antagonist effect:
no graph available
MCH 2 - agonist radioligand
Source
human recombinant (CHO cells)
Ligand
[ 125 I]S36057 (0.05 nM)
binding
Kd
0.08 nM
Ref. 1190
Non specific human MCH (3 µM)
Q 3 weeks
Reference human MCH (IC 50 : 44 nM)
Included in:
Organ safety profile
Audinot, V. et al. (2001) Brit. J. Pharmacol., 133: 371-378.
specific binding (% of control)
-12 -11
-11 -10
100-12 -11
-12 -11
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7
-10 -9 -8 -7
50
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
0
-11 -10
-9 -8 -7 -6 -5 -4
-12 -11 -10 -9 -8 -7 -6 -5 -4 -3
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
human MCH
[Phe 13 ,Tyr 19 ]-MCH
salmon MCH

melanin concentrating hormone ❚
47
MCH 2
cellul ar
Ref. 1106
Ref. 1107
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control human MCH (100 nM)
Reference human MCH (EC 50 : 4.2 nM)
Antagonist effect Stimulant human MCH (30 nM)
Reference unavailable
Wang, S. et al. (2001) J. Biol. Chem., 276: 34664-34670.
Ca 2+ mobilization (% of control)
100
50
0
-11 -10
-9 -8 -7 -6
log [agonist] (M)
human MCH
[Phe 13 ,Tyr 19 ]-MCH
salmon MCH
[Solvent] must be kept ≤ 0.1%
antagonist effect:
no graph available
Cerep
services
Receptors
[GPCRs]
-11 -10
-9 -8 -7 -6 -5 -4
-12 -11
-10 -9 -8 -7
-11 -10
-9 -8 -7 -6 -5 -4
-12 -11 -10 -9 -8 -7 -6 -5 -4 -3
-12 -11
-12 -11
-10 -9 -8 -7
-10 -9 -8 -7 -6 -5
Ion
channels
-9 -8 -7 -6 -5
-10 -4
❚ melanocortin
MC 1 - agonist radioligand
binding
Ref. 0644
Q 3 weeks
Included in:
BioPrint ® profile
Source
Ligand
Kd
Non specific
Reference
B16-F1 cells (endogenous)
[ 125 I]NDP-a-MSH (0.05 nM)
0.05 nM
NDP-a-MSH (1 µM)
NDP-a-MSH (IC 50 : 0.18 nM)
Siegrist, W. et al. (1988) J. Recep. Res., 8: 323-343.
specific binding (% of control)
100
50
NDP-α-MSH
α-MSH
MT-II
0
ACTH
-12 -11 -10 -9 -8 -7 -6
log [drug] (M)
Transporters
Kinases
Epigenetic &
DNA-related
enzymes
MC 1
cellul ar
Ref. 2147
Ref. 2148
Q 3 weeks
Agonist effect
Antagonist effect
Source
B16-F1 cells (endogenous)
Measured product cAMP
Detection method HTRF
Agonist effect Control NDP-a-MSH (1 µM)
Reference NDP-a-MSH (EC 50 : 1.2 nM)
Antagonist effect Stimulant NDP-a-MSH (10 nM)
Reference AGRP (83-132) (IC 50 : 248 nM)
Tatro, J.B. et al. (1990) Cancer Research., 50: 1237-1242.
cAMP modulation (% of control)
100
50
0
-12 -11
-10 -9 -8 -7 -6 -5
log [agonist] (M)
NDP-α-MSH
α-MSH
ACTH (1-39)
MT-II
100
[Solvent] must be kept ≤ 0.3%
50
0
-12 -11
-10 -9 -8 -7 -6 -5
log [antagonist] (M)
AGRP (83-132)
SHU 9119
HS 024
Other
enzymes
Specialized
cellular
assays
MC 2
cellul ar
Ref. 2240
Ref. 2241
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (Cloudman M3 cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control ACTH (1-39) (1 µM)
Reference ACTH (1-39) (EC 50 : 14 nM)
Antagonist effect Stimulant ACTH (1-39) (30 nM)
Reference unavailable
Kapas, S. et al. (1996) Endocrinol., 137: 3291-3294.
-12 -11
-12 -11
-12 -11
-10 -9 -8 -7
-10 -9 -8 -7
-10 -9 -8 -7 -6 -5
-11 -10
-9 -8 -7
-6 -5 -10 -4
α
α
[Solvent] must be kept 0.3%
-9 -8 -7 -6 -5 -4
-13 -12 -11 -10
-9 -8 -7 -6
-12 -11 -10 -9 -8 -7 -6 -5 -4
Standard
profiles
Testing
conditions
-11 -10
-9 -8 -7 -6 -5 -4
MC 3 - agonist radioligand
binding
Ref. 0447
Q 3 weeks
Included in:
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 125 I]NDP-a-MSH (0.075 nM)
0.4 nM
NDP-a-MSH (1 µM)
NDP-a-MSH (IC 50 : 0.23 nM)
Schioth, H.B. et al. (1997) Neuropeptides, 31: 565-571.
α
α
Ordering
information
Assay list
& index

48 in vitro pharmacology 2011 catalog
❚ melanocortin
MC 3
cellul ar
Ref. 0959
Ref. 1755
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control NDP-a-MSH (1 µM)
Reference NDP-a-MSH (EC 50 : 2.2 nM)
Antagonist effect Stimulant NDP-a-MSH (30 nM)
Reference SHU 9119 (IC 50 : 39 nM)
Schioth, H.B. et al. (1997) Neuropeptides, 31: 565-571.
cAMP modulation (% of control)
100
100
50
50
0
0
-11 -10 -9 -8 -7 -6 -10 -9 -8 -7 -6 -5
log [agonist] (M)
log [antagonist] (M)
NDP-α-MSH
SHU 9119
α-MSH
AGRP (83-132)
MT-II
ACTH
[Solvent] must be kept ≤ 0.3%
MC 4 - agonist radioligand
binding
Ref. 0420
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 125 I]NDP-a-MSH (0.05 nM)
0.54 nM
NDP-a-MSH (1 µM)
NDP-a-MSH (IC 50 : 0.23 nM)
Schioth, H.B. et al. (1997) Neuropeptides, 31: 565-571.
specific binding (% of control)
-12 -11
-12 -11
-11 -10
100
-12 -11
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7
-10 -9 -8 -7
50 -10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
0
-11 -10
-9 -8 -7 -6 -5 -4
-13 -12 -11 -10 -9 -8 -7 -6
log [drug] (M)
-12 -11 -10 -9 -8 -7 -6 -5 -4
-13 -12 -11 -10 -9 -8 -7 -6 -5 -4
NDP-α-MSH
α-MSH
AGRP
SHU 9119
MC 4
cellul ar
Ref. 0699
Ref. 0700
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control NDP-a-MSH (30 nM)
Reference NDP-a-MSH (EC 50 : 0.4 nM)
Antagonist effect Stimulant NDP-a-MSH (1 nM)
Reference SHU 9119 (IC 50 : 0.5 nM)
Vanleeuween, D. et al. (2003) J. Biol. Chem., 278: 15935-15940.
cAMP modulation (% of control)
100
50
0
-10 -9 -8 -7 -6 -12 -11
-12 -11 -10 -9 -8 -7
log [agonist] (M)
NDP-α-MSH
α-MSH
MT-II
100
[Solvent] must be kept ≤ 0.3%
50
0
log [antagonist] (M)
SHU 9119
AGRP (83-132)
MC 4 - inverse agonist effect
cellul ar
Ref. 2423
Q 3 weeks
Source
Measured product cAMP
Detection method HTRF
Control
Reference
[Solvent] must be kept ≤ 0.3%
human recombinant (CHO cells)
AGRP (83-132) (1 µM)
AGRP (83-132) (IC 50 : 3.13 nM)
Adan, R.A.H. and Kas, M.J.H. (2003) Trends Pharmacol. Sci., 24: 315-321.
-12 -11
-11 -10
-12 -11
-12 -11
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7
-10 -9 -8 -7
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
-11 -10
-9 -8 -7 -6 -5 -4
-13 -12 -11 -10 -9 -8 -7 -6
-12 -11 -10 -9 -8 -7 -6 -5 -4
MC 5 - agonist radioligand
Source
human recombinant (CHO cells)
Ligand
[ 125 I]NDP-a-MSH (0.05 nM)
Kd
0.7 nM
Non specific NDP-a-MSH (1 µM)
binding
Reference NDP-a-MSH (IC 50 : 0.68 nM)
Ref. 0448
Q 4 weeks
Schioth, H.B. et al. (1997) Neuropeptides, 31: 565-571.
α
α
MC 5
cellul ar
Ref. 1869
Ref. 1870
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control a-MSH (10 µM)
Reference a-MSH (EC 50 : 380 nM)
Antagonist effect Stimulant a-MSH (1 µM)
Reference AGRP (83-132) (IC 50 : 120 nM)
Fathi, Z. et al. (1995) Neurochem. Res., 20: 107-113.
cAMP modulation (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5 -10 -9 -8 -7 -6
log [agonist] (M)
α-MSH
ACTH
SHU 9119
NDP-α-MSH
100
[Solvent] must be kept ≤ 0.3%
50
0
log [antagonist] (M)
AGRP (83-132)
-11 -10
-9 -8 -7 -6 -5 -4
-12 -11
-10 -9 -8 -7
-11 -10
-9 -8 -7 -6 -5 -4

49
❚ melatonin
Cerep
services
MT 1 (ML 1A ) - agonist radioligand
binding
Ref. 1538
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 125 I]2-iodomelatonin (0.01 nM)
0.04 nM
melatonin (1 µM)
melatonin (IC 50 : 0.16 nM)
Witt-Enderby, P.A. and Dubocovitch, M.L. (1996) Mol. Pharm., 50: 166-174.
specific binding (% of control)
100
50
0
-13 -12 -11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
melatonin
2-iodomelatonin
6-chloromelatonin
luzindole
Receptors
[GPCRs]
Ion
channels
MT 1 (ML 1A )
cellul ar
Ref. 2498 Agonist effect
Ref. 2500 Antagonist effect
Q 3 weeks
Source
human recombinant (CHO cells)
Measured product impedance
Detection method cellular dielectric spectroscopy
Agonist effect Control melatonin (10 nM)
Reference melatonin (EC 50 : 0.22 nM)
Antagonist effect Stimulant melatonin (1 nM)
Reference luzindole (IC 50 : 680 nM)
Browning, C. et al. (2000) Br. J. Pharmacol., 129: 877-886.
[Solvent] must be kept 0.1%
Transporters
Kinases
MT 2 (ML 1B ) - agonist radioligand
Source
human recombinant (CHO cells)
Ligand
[ 125 I]2-iodomelatonin (0.05 nM)
binding
Kd
0.085 nM
Ref. 1687
Non specific melatonin (1 µM)
Q 3 weeks
Reference melatonin (IC 50 : 0.18 nM)
Included in:
Organ safety profile
Beresford, I.J.M. et al. (1998) J. Pharmacol. Exp. Ther., 285: 1239-1245.
specific binding (% of control)
100
50
melatonin
2-iodomelatonin
4-P-PDOT
0
luzindole
-13 -12 -11 -10 -9 -8 -7 -6
log [drug] (M)
Epigenetic &
DNA-related
enzymes
Other
enzymes
MT 2 (ML 1B )
cellul ar
Ref. 2092 Agonist effect
Ref. 2100 Antagonist effect
Q 3 weeks
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control melatonin (1 µM)
Reference melatonin (EC 50 : 0.25 nM)
Antagonist effect Stimulant melatonin (10 nM)
Reference unavailable
Beresford, I.J.M. et al. (1998) J. Pharmacol. Exp. Ther., 285: 1239-1245.
cAMP modulation (% of control)
100
50
0
log [agonist] (M)
melatonin
2-iodomelatonin
GR 135531
IIK7
[Solvent] must be kept ≤ 0.3%
-11 -10
-12 -11
-10 -9 -8 -7 -6
-9 -8 -7 -6 -5 -4
antagonist effect:
no graph available
❚ See other Melatonin assays, page 89
Specialized
cellular
assays
Standard
profiles
-12 -11
-10 -9 -8 -7
❚ motilin
-12 -11
-12 -11
-10 -9 -8 -7
-10 -9 -8 -7 -6 -5
-11 -10
-9 -8 -7 -6 -5 -4
Testing
conditions
motilin - agonist radioligand
binding
Ref. 0470
Q 3 weeks
Included in:
BioPrint ® profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 125 I]motilin (0.05 nM)
0.26 nM
[Nleu 13 ]-motilin (1 µM)
[Nleu 13 ]-motilin (IC 50 : 1.4 nM)
Feighner, S.D. et al. (1999) Science, 284: 2184-2188.
-9 -8 -7 -6 -5
-10 -4
specific binding (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5 -4 -3 -2
log [drug] (M)
● [Nleu 13 ]-motilin
■ motilin
▲ erythromicin
Ordering
information
Assay list
& index

50 in vitro pharmacology 2011 catalog
❚ motilin
motilin
cellul ar
Ref. 1321 Agonist effect
Ref. 1894 Antagonist effect
Q 3 weeks
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control motilin (3 nM)
Reference motilin (EC 50 : 0.011 nM)
Antagonist effect Stimulant motilin (0.3 nM)
Reference unavailable
Dass, N.B. et al. (2003) Brit. J. Pharmacol. 140: 948-954.
Ca 2+ mobilization (% of control)
100
50
0
-13
-12 -11
log [agonist] (M)
motilin
[Nleu 13 ]-motilin
erythromycin
-10 -9 -8 -7 -6 -5
[Solvent] must be kept ≤ 0.1%
antagonist effect:
no graph available
-11 -10
-9 -8 -7 -6 -5 -4
❚ muscarinic
-12 -11
-12 -11
-12 -11
-10 -9 -8 -7
-10 -9 -8 -7
-10 -9 -8 -7 -6 -5
-11 -10
-9 -8 -7 -6 -5 -4
-12 -11 -10 -9 -8 -7 -6 -5 -4 -3
M (non-selective) - antagonist radioligand
binding
Ref. 0089
Q 3 weeks
Included in:
Diversity profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]QNB (0.05 nM)
0.01 nM
atropine (1 µM)
atropine (IC 50 : 0.45 nM)
Richards, M.H. (1990) Brit. J. Pharmacol., 99: 753-761.
-9 -8 -7 -6 -5
-10 -4
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5
log [drug] (M)
atropine
4-DAMP
methoctramine
pirenzepine
M 1 - antagonist radioligand
binding
Ref. 0091
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]pirenzepine (2 nM)
13 nM
atropine (1 µM)
pirenzepine (IC 50 : 22 nM)
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5
-12 -4
log [drug] (M)
Dorje, F. et al. (1991) J. Pharmacol. Exp. Ther., 256: 727-733.
[Custom offer] rat brain model (Ref. 0090), please contact us at customresearch@cerep.com
pirenzepine
methoctramine
atropine
4-DAMP
M 1
cellul ar
Ref. 1262
Ref. 1474
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control acetylcholine (100 nM)
Reference acetylcholine (EC 50 : 0.76 nM)
Antagonist effect Stimulant acetylcholine (3 nM)
Reference pirenzepine (IC 50 : 96 nM)
Sur, C. et al. (2003) Proc. Natl. Acad. Sci. USA, 100: 13674-13679.
Ca 2+ mobilization (% of control)
100
100
50
50
0
0
-11 -10 -9 -8 -7 -6 -5 -11 -10 -9 -8 -7 -6 -5 -4
log [agonist] (M)
log [antagonist] (M)
acetylcholine
pirenzepine
carbachol
atropine
4-DAMP
methoctramine
[Solvent] must be kept ≤ 0.1%
M 1
tissue
Ref. 0318
Q 4 weeks
Source
rabbit vas deferens (field-stimulated)
Agonist McN-A-343 (pD 2 = 6.4)
Antagonist pirenzepine (pA 2 = 8.2)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Eltze, M. (1988) Eur. J. Pharmacol., 151: 205-221.
tension (% of control)
100
-11 -10 -9 -8 -7 -6 -5 -4
-1350
-12 -11 -10 -9 -8 -7 -6 -5
-11 -10 -9 -8 -7 -6
-9 -8 -7 -6 -5
-10 -4
-12 -11 -10 -9 -8 -7 -6
0
-12 -11 -10 -9 -8 -7 -6 -5
-8 -7 -6 -5 -4
log [agonist] (M)
pirenzepine
none
10 nM
-12 -11 -10 -9 -8 -7 30 -6nM-5 -4 -3
100 nM
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
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Assay developed in 2010 New assay conditions Human Q Standard turnaround time

51
M 2 - antagonist radioligand
binding
Ref. 0093
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
BioPrint ® profile
M 2 - agonist radioligand
binding
Ref. 1626
Q 3 weeks
Included in:
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]AF-DX 384 (2 nM)
4.6 nM
atropine (1 µM)
methoctramine (IC 50 : 32 nM)
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
Dorje, F. et al. (1991) J. Pharmacol. Exp. Ther., 256: 727-733.
[Custom offer] rat heart model (Ref. 0092), please contact us at customresearch@cerep.com
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]oxotremorine-M (1.5 nM)
1.4 nM
atropine (1 µM)
acetylcholine (IC 50 : 3 nM)
Van den Beukel, I. et al. (1997) J. Pharmacol. Exp. Ther., 281: 1113-1119.
muscarinic ❚
methoctramine
atropine
4-DAMP
pirenzepine
Cerep
services
Receptors
[GPCRs]
Ion
channels
Transporters
M 2
cellul ar
Ref. 1658
Ref. 1659
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control acetylcholine (10 µM)
Reference acetylcholine (EC 50 : 107 nM)
Antagonist effect Stimulant acetylcholine (1 µM)
Reference methoctramine (IC 50 : 197 nM)
Michal, P. et al. (2001) Brit. J. Pharmacol., 132: 1217-1228.
cAMP modulation (% of control)
100
50
0
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-12 -11 -4 -10 -4
log [agonist] (M)
acetylcholine
oxotremorine
metoclopramide
carbachol
100
50
0
log [antagonist] (M)
methoctramine
atropine
4-DAMP
pirenzepine
Kinases
Epigenetic &
DNA-related
enzymes
M 2 - inverse agonist effect
cellul ar
Ref. 2411
Q 3 weeks
Source
Measured product cAMP
Detection method HTRF
Control
Reference
[Solvent] must be kept ≤ 0.3%
human recombinant (CHO cells)
tropicamide (10 µM)
tropicamide (EC 50 : 210 nM)
Nelson, C.P. et al. (2006) J. Pharmacol. Exp. Ther, 316: 279-288.
-12 -11
-12 -11
-11 -10
-12 -11
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7
-10 -9 -8 -7
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
-11 -10
-9 -8 -7 -6 -5 -4
Other
enzymes
Specialized
cellular
assays
M 2
tissue
Ref. 0319
Q 4 weeks
Source
guinea-pig left atrium (electrically paced)
Agonist carbachol (pD 2 = 6.4)
Antagonist methoctramine (pA 2 = 6.7)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Eglen, R.M. et al. (1988) Brit. J. Pharmacol., 95: 1031-1038.
tension (% of control)
100
50
0
-8 -6 -7 -5
log [agonist] (M)
methoctramine
none
0.1 µM
0.3 µM
1 µM
Standard
profiles
Testing
conditions
M 3 - antagonist radioligand
binding
Ref. 0095
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]4-DAMP (0.2 nM)
0.5 nM
atropine (1 µM)
4-DAMP (IC 50 : 0.46 nM)
Peralta, E.G. et al. (1987) Embo. J., 6: 3923-3929.
specific binding (% of control)
100
50
0
-12
-11
-10 -9 -8 -7 -6 -5
log [drug] (M)
4-DAMP
atropine
pirenzepine
methoctramine
Ordering
information
Assay list
& index

52 in vitro pharmacology 2011 catalog
❚ muscarinic
M 3
cellul ar
Ref. 1243
Ref. 1244
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control acetylcholine (1 µM)
Reference acetylcholine (EC 50 : 10 nM)
Antagonist effect Stimulant acetylcholine (10 nM)
Reference 4-DAMP (IC 50 : 3.6 nM)
Sur, C. et al. (2003) Proc. Natl. Acad. Sci. USA, 100: 13674-13679.
Ca 2+ mobilization (% of control)
100
50
0
log [agonist] (M)
acetylcholine
oxotremorine-M
carbachol
100
-11 -10 -9 -8 -7 -6 -5 -11 -10 -9 -8 -7 -6 -5 -4
[Solvent] must be kept ≤ 0.1%
50
0
log [antagonist] (M)
4-DAMP
atropine
pirenzepine
M 3
tissue
Ref. 0320
Q 4 weeks
Source
guinea-pig ileum
Agonist carbachol (pD 2 = 6.6)
Antagonist 4-DAMP (pA 2 = 9.2)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Clague, R.U. et al. (1985) Brit. J. Pharmacol., 86: 163-170.
tension (% of max.)
100
50
0
-9 -8 -7 -6 -5 -4
log [agonist] (M)
4-DAMP
none
3 nM
10 nM
30 nM
M 4 - antagonist radioligand
binding
Ref. 0096
Q 3 weeks
Included in:
High-throughput profile
BioPrint ® profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]4-DAMP (0.2 nM)
0.32 nM
atropine (1 µM)
4-DAMP (IC 50 : 0.53 nM)
Dorje, F. et al. (1991) J. Pharmacol. Exp. Ther., 256: 727-733.
specific binding (% of control)
100
50
0
-12
-11
4-DAMP
atropine
pirenzepine
methoctramine
-10 -9 -8 -7 -6 -5
log [drug] (M)
M 4 - agonist radioligand
Source
human recombinant (CHO cells)
Ligand
[ 3 H]oxotremorine-M (6 nM)
binding
Kd
4.6 nM
Ref. 1619
Non specific atropine (1 µM)
Q 3 weeks
Reference acetylcholine (IC 50 : 20 nM)
Included in:
Organ safety profile
Van den Beukel, I. et al. (1997) J. Pharmacol. Exp. Ther., 281: 1113-1119.
specific binding (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5
log [drug] (M)
acetylcholine
oxotremorine
carbachol
atropine
M 4
cellul ar
Ref. 1670
Ref. 1671
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control acetylcholine (10 µM)
Reference acetylcholine (EC 50 : 33 nM)
Antagonist effect Stimulant acetylcholine (300 nM)
Reference PD 102807 (IC 50 : 280 nM)
Olianas, M.C. and Onali, P. (1999) Life Sc., 65: 2233-2240.
[Solvent] must be kept 0.3%
M 4 - inverse agonist effect
cellul ar
Ref. 2412
Q 3 weeks
Source
Measured product cAMP
Detection method HTRF
Control
Reference
[Solvent] must be kept ≤ 0.3%
human recombinant (CHO cells)
tropicamide (10 µM)
tropicamide (EC 50 : 122 nM)
Jakubik, J. et al. (1995) FEBS Lett., 377: 275-279.

53
muscarinic ❚
M 5 - antagonist radioligand
Source
human recombinant (CHO cells)
Ligand
[ 3 H]4-DAMP (0.3 nM)
binding
Kd
0.3 nM
Ref. 0097
Non specific atropine (1 µM)
Q 3 weeks
Reference 4-DAMP (IC 50 : 0.52 nM)
Included in:
High-throughput profile
Dorje, F. et al. (1991) J. Pharmacol. Exp. Ther., 256: 727-733.
specific binding (% of control)
100
50
0
4-DAMP
atropine
pirenzepine
methoctramine
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
Cerep
services
Receptors
[GPCRs]
M 5 - agonist radioligand
Source
human recombinant (CHO cells)
Ligand
[ 3 H]oxotremorine-M (6 nM)
binding
Kd
11 nM
Non specific atropine (1 µM)
Ref. 1620
Q 3 weeks
Reference acetylcholine (IC 50 : 17 nM)
Included in:
Organ safety profile
Loudon, J.M. et al. (1997) J. Pharmacol. Exp. Ther., 283: 1059-1068.
specific binding (% of control)
100
50
acetylcholine
atropine
0
oxotremorine-M
4-DAMP
-12 -11 -10 -9 -8 -7 -6 -5
log [drug] (M)
Ion
channels
Transporters
M 5
cellul ar
Ref. 1320
Ref. 1652
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control acetylcholine (1 µM)
Reference acetylcholine (EC 50 : 0.5 nM)
Antagonist effect Stimulant acetylcholine (10 nM)
Reference atropine (IC 50 : 55 nM)
Kukkonen, J.P. et al. (1996) J. Pharmacol. Exp. Ther., 279: 593-601.
Ca 2+ mobilization (% of control)
100
100
50
50
0
0
-11 -10 -9 -8 -7 -6 -5 -4 -10 -9 -8 -7 -6 -5 -4
log [agonist] (M)
log [antagonist] (M)
acetylcholine
atropine
oxotremorine-M
4-DAMP
carbachol
pirenzepine
[Solvent] must be kept ≤ 0.1%
Kinases
Epigenetic &
DNA-related
enzymes
❚ neurokinin
-12 -11
-10 -9 -8 -7 -6 -5
Other
enzymes
NK 1 - agonist radioligand
binding
Ref. 0100
Q 3 weeks
Included in:
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
U-373MG cells (endogenous)
[ 125 I]BH-SP (0.15 nM)
0.12 nM
[Sar 9 ,Met(O 2 ) 11 ]-SP (1 µM)
[Sar 9 ,Met(O 2 ) 11 ]-SP (IC 50 : 0.29 nM)
-9 -8 -7 -6 -5
-10 -4
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
Heuillet, E. et al. (1993) J. Neurochem., 60: 868-876.
[Custom offer] rat brain model (Ref. 0099), please contact us at customresearch@cerep.com
[Sar 9 ,Met(O 2 ) 11 ]-SP
[Nle 10 ]-NKA (4-10)
[MePhe 7 ]-NKB
Specialized
cellular
assays
Standard
profiles
NK 1
cellul ar
Ref. 2190
Ref. 2192
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
U-373MG cells (endogenous)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control [Sar 9 ,Met(O 2 ) 11 ]-SP (100 nM)
Reference [Sar 9 ,Met(O 2 ) 11 ]-SP
(EC 50 : 0.17 nM)
Antagonist effect Stimulant [Sar 9 ,Met(O 2 ) 11 ]-SP (3 nM)
Reference L 733,060 (IC 50 : 10 nM)
Eistetter, H.R. et al. (1992) Glia, 6: 89-95.
Ca 2+ mobilization (% of control)
100
50
0
-13 -12 -11 -10 -9 -8 -7 -6 -5 -4 -13 -12-11 -10 -9 -8 -7 -6 -5 -4
log [agonist] (M)
[Sar 9 ,Met(O 2 ) 11 ]-SP
[Nleu 10 ]-NKA (4-10)
[MePhe 7 ]-NKB
substance P
100
[Solvent] must be kept ≤ 0.1%
50
0
log [antagonist] (M)
L 733,060
GR 159897
SB 222200
spantide II
Testing
conditions
Ordering
information
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
-12 -11
-12 -11
-11 -10
-12 -11
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Assay developed in 2010 New assay conditions Human Q Standard turnaround time
-10 -9 -8 -7
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
-11 -10
-9 -8 -7 -6 -5 -4
Assay list
& index

54 in vitro pharmacology 2011 catalog
❚ neurokinin
NK 1
tissue
Ref. 0321
Q 4 weeks
Source
rabbit pulmonary artery
(precontracted with 0.1 µM norepinephrine)
Agonist [Sar 9 ,Met(O 2 ) 11 ]-SP (pD 2 = 9.8)
Antagonist spantide II
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Emonds-Alt, X. et al. (1993) Eur. J. Pharmacol., 250: 403-413.
tension (% of control)
100
50
0
-12 -11 -10 -9
log [agonist] (M)
NK 1
tissue gpcr
Ref. 0624
Q 4 weeks
Source
guinea-pig ileum
Agonist [Sar 9 ,Met(O 2 ) 11 ]-SP (pD 2 = 8.5)
Antagonist spantide II
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Emonds-Alt, X. et al. (1993) Eur. J. Pharmacol., 250: 403-413.
tension (% of max.)
100
50
0
-11 -10 -9 -8 -7 -6
log [agonist] (M)
NK 2 - agonist radioligand
binding
Ref. 0102
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 125 I]NKA (0.1 nM)
0.12 nM
[Nleu 10 ]-NKA (4-10) (300 nM)
[Nleu 10 ]-NKA (4-10) (IC 50 : 2.7 nM)
Aharony, D. et al. (1993) Mol. Pharmacol, 44: 356-363.
NK 2
cellul ar
Ref. 1251
Ref. 1765
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control [Nleu 10 ]-NKA (4-10) (1 µM)
Reference [Nleu 10 ]-NKA(4-10)(EC 50 : 1.5 nM)
Antagonist effect Stimulant [Nleu 10 ]-NKA (4-10) (10 nM)
Reference GR 159897 (IC 50 : 15.7 nM)
Subramamian, N. et al. (1994) Biochem. Biophys. Res. Commun., 200: 1512-1520.
Ca 2+ mobilization (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -11 -10 -9 -8 -7 -6 -5 -4
log [agonist] (M)
[Nleu 10 ]-NKA (4-10)
NKB
[Sar 9 ,Met(O 2 ) 11 ]-SP
senktide
100
[Solvent] must be kept ≤ 0.1%
50
0
log [antagonist] (M)
GR 159897
SR 48968
SB 222200
spantide II
NK 2
tissue
Ref. 0322
Q 4 weeks
Source
rabbit pulmonary artery
(endothelium-denuded)
Agonist [bAla 8 ]-NKA (4-10) (pD 2 = 8.2)
Antagonist SR 48968 (pA 2 = 10.3)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Emonds-Alt, X. et al. (1993) Regul. Peptides, 46: 31-36.
tension (% of max.)
-12 -11
-12 -11
-11 -10 -9 -8 -7 -6 -5 -4
100-12 -11 -10 -9 -8 -7
-11 -10 -9 -8 -7 -6 -5 -4
-10 -9 -8 -7
50
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
0
-10 -9 -8 -7 -6
log [agonist] (M)
SR 48968
none
0.1 nM
0.3 nM
1 nM
NK 3 - antagonist radioligand
binding
Ref. 0104
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]SR 142801 (0.4 nM)
0.47 nM
SB 222200 (10 µM)
SB 222200 (IC 50 : 8.8 nM)
Sarau, H.M. et al. (1997) J. Pharmacol. Exp. Ther., 281: 1303-1311.
specific binding (% of control)
100
50
0
SB 222200
senktide
[Sar 9 ,Met (O 2
) 11 ]-SP
SR 48968
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
-10 -9 -8 -7 -6 -5 -4 -3
-12 -11 -10 -9 -8 -7 -6 -5 -4

55
NK 3 - agonist radioligand
binding
Ref. 1240
Q 3 weeks
Included in:
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 125 I][MePhe 7 ]-NKB (0.025 nM)
4.5 nM
SB 222200 (1 µM)
[MePhe 7 ]-NKB (IC 50 : 1.4 nM)
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
neurokinin ❚
[MePhe 7 ]-NKB
SR 48968
senktide
SB 222200
Anthes, J.C. et al. (2002) Eur. J. Pharmacol., 450: 191-202.
[Custom offer] guinea-pig brain model (Ref. 0103), please contact us at customresearch@cerep.com
Cerep
services
Receptors
[GPCRs]
NK 3
cellul ar
Ref. 1312
Ref. 1766
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control [MePhe 7 ]-NKB (10 nM)
Reference [MePhe 7 ]-NKB (EC 50 : 0.48 nM)
Antagonist effect Stimulant [MePhe 7 ]-NKB (1 nM)
Reference SB 222200 (IC 50 : 300 nM)
Medhurst, A.D. et al. (1999) Brit. J. Pharmacol., 128: 627-636.
Ca 2+ mobilization (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5 -9 -8 -7 -6 -5 -4
log [agonist] (M)
[MePhe 7 ]-NKB
senktide
[Sar 9 ,Met(O 2 ) 11 ]-SP
[Nleu 10 ]-NKA (4-10)
100
[Solvent] must be kept ≤ 0.1%
50
0
log [antagonist] (M)
SB 222200
SR 48968
spantide II
Ion
channels
Transporters
NK 3
tissue
Ref. 0323
Q 4 weeks
Source
rat portal vein
Agonist [MePhe 7 ]-NKB (pD 2 = 9.6)
Antagonist SB 222200
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Emonds-Alt, X. et al. (1995) Life Sci., 56: 27-32.
tension (% of max.)
-12 -11
-12 -11
100-12 -11 -10 -9 -8 -7
-11 -10 -9 -8 -7 -6 -5 -4
-10 -9 -8 -7
50
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
0
-11 -10 -9 -8
log [agonist] (M)
Kinases
Epigenetic &
DNA-related
enzymes
-11 -10 -9 -8 -7 -6 -5 -4
NK 3
tissue
Ref. 0625
Q 4 weeks
Source
guinea-pig ileum
Agonist [MePhe 7 ]-NKB (pD 2 = 8)
Antagonist SB 222200
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Emonds-Alt, X. et al. (1995) Life Sci., 56: 27-32.
tension (% of max.)
100
50
0
-11 -10 -9 -8 -7 -6
log [agonist] (M)
Other
enzymes
Specialized
cellular
assays
❚ neuromedin u
Standard
profiles
NMU1
cellul ar
Ref. 3310 Agonist effect
Ref. 3312 Antagonist effect
Q 3 weeks
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control NMU-25 (10 nM)
Reference NMU-25 (EC 50 : 0.13 nM)
Antagonist effect Stimulant NMU-25 (0.3 nM)
Reference unavailable
Meng, T., et al. (2008) Acta. Pharmacol. Sin., 29: 517-527.
Ca 2+ mobilization (% of control)
100
50
0
-12 -11 -10 -9 -8 -7
log [agonist] (M)
NMU-25 (human)
NMU-8 (porcine)
NMU-23 (rat)
NMS (human)
antagonist effect:
no graph available
Testing
conditions
-9 -8 -7 -6 -5
log [antagonist] (M)
SB 222200
SR 48968
spantide II
Ordering
information
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
-12 -11
-12 -11
-11 -10
-12 -11
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Assay developed in 2010 New assay conditions Human Q Standard turnaround time
-10 -9 -8 -7
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
-11 -10
-9 -8 -7 -6 -5 -4
Assay list
& index

56 in vitro pharmacology 2011 catalog
❚ neuromedin U
NMU2 - agonist radioligand
Source
human recombinant (HEK-293 cells)
Ligand
[ 125 I]NMU-8 (porcine) (0.05 nM)
binding
Kd
0.057 nM
Ref. 0991
Non specific NMU-8 (porcine) (100 nM)
Q 3 weeks
Reference NMU-8 (porcine) (IC 50 : 0.22 nM)
Included in:
Organ safety profile
Funes, S. et al. (2002) Peptides, 23: 1607-1615.
❚ neuropeptide s
NPS
cellul ar
Ref. 3291
Ref. 3292
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (HEK-293 cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control NPS (1 µM)
Reference NPS (EC 50 : 3.7 nM)
Antagonist effect Stimulant NPS (300 nM)
Reference unavailable
Xu, Y.L., et al. (2004) Neuron., 43: 487-497.
[Solvent] must be kept 0.1%
❚ neuropeptide w / neuropeptide B
NPBW1
cellul ar
Ref. 2845
Ref. 2851
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control NPB29 (100 nM)
Reference NPB29 (EC 50 : 0.08 nM)
Antagonist effect Stimulant NPB29 (1 nM)
Reference unavailable
Shimomura, Y., (2002) J. Biol. Chem., 277: 35826-35832.
❚ neuropeptide y
Y (non-selective) - agonist radioligand
binding
Ref. 0105
Q 3 weeks
Included in:
Diversity profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 125 I]peptide YY (0.05 nM)
0.1 nM
NPY (1 µM)
NPY (IC 50 : 0.46 nM)
Goldstein, M. et al. (1986) Progr. Brain Res., 68: 331-335.
Y 1 - agonist radioligand
binding
Ref. 0106
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
SK-N-MC cells (endogenous)
[ 125 I]peptide YY (0.025 nM)
0.06 nM
NPY (1 µM)
NPY (IC 50 : 0.079 nM)
Wieland, H. A. et al. (1995) J. Pharmacol. Exp. Ther., 275: 143-149.
specific binding (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5
log [drug] (M)
NPY
[Leu 31 , Pro 34 ]-NPY
BIBP 3226

neuropeptide y ❚
57
Y 1
cellul ar
Ref. 2206
Ref. 2207
Q 3 weeks
Agonist effect
Antagonist effect
Source
SK-N-MC cells (endogenous)
Measured product cAMP
Detection method HTRF
Agonist effect Control NPY (10 nM)
Reference NPY (EC 50 : 0.25 nM)
Antagonist effect Stimulant NPY (1 nM)
Reference BIBP 3226 (IC 50 : 125 nM)
Wieland, H.A. et al. (1995) J. Pharmacol. Exp. Ther., 275: 143-149.
[Solvent] must be kept 0.3%
Cerep
services
Receptors
[GPCRs]
Y 1
tissue
Ref. 0324
Q 4 weeks
Source
rabbit vas deferens (field-stimulated)
Agonist [Leu 31 ,Pro 34 ]-NPY (pD 2 = 8.1)
Antagonist BIBP 3226
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Doods, H. and Krause, J. (1991) Eur. J. Pharmacol., 204: 101-103.
tension (% of control)
100
50
[Leu 31 ,Pro 34 ]-NPY
0
NPY-(13-36)
-11 -10 -9 -8 -7 -6
log [agonist] (M)
Ion
channels
Transporters
Y 2 - agonist radioligand
binding
Ref. 0107
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
KAN-TS cells
[ 125 I]peptide YY (0.015 nM)
0.01 nM
NPY (1 µM)
NPY (IC 50 : 0.08 nM)
Fuhlendorff, J. et al. (1990) Proc. Natl. Acad. Sci. USA, 87: 182-186.
Kinases
Epigenetic &
DNA-related
enzymes
Y 2
tissue
Ref. 0325
Q 4 weeks
Source
rat vas deferens (field-stimulated)
Agonist NPY-(13-36) (pD 2 = 7.7)
Antagonist BIIE 0246
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Doods, H. and Krause, J. (1991) Eur. J. Pharmacol., 204: 101-103.
tension (% of control)
100
50
0
-10 -9 -8 -7 -6
log [agonist] (M)
NPY-(13-36)
[Leu 31 ,Pro 34 ]-NPY
Other
enzymes
Specialized
cellular
assays
Y 3
tissue
Ref. 0326
Q 4 weeks
Source
rat colon
Agonist NPY (pD 2 = 7)
Antagonist not available
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Dumont, Y. et al. (1993) Eur. J. Pharmacol., 238: 37-45.
tension (% of max.)
100
50
0
-9 -8 -7 -6
log [agonist] (M)
Standard
profiles
Testing
conditions
❚ For radioligand binding assays, how should I choose between the agonist and the antagonist models when both are
available?
For some binding assays two models are available using either agonist or antagonist as radioligand.
G-protein-coupled receptors have both high-affinity and low-affinity states that are bound differently by agonists and antagonists. Whereas
the antagonists bind with an equal affinity to both affinity states, agonists bind poorly to the low affinity state of the receptor. Therefore,
it is advisable to use an antagonist radioligand to evaluate the binding of antagonists knowing that this may fail to reveal the binding
of agonists. On the other hand, an assay using an agonist radioligand is suitable to evaluate both agonists and antagonists.
The testing of a compound in both assays and the comparison of its competition curves against each radioligand may provide information
about its functional activity at the receptor.
Ordering
information
Assay list
& index

58 in vitro pharmacology 2011 catalog
❚ neurotensin
NT (non-selective) - agonist radioligand
Source
rat brain
Ligand
[ 125 I]Tyr 3 -neurotensin (0.05 nM)
Kd
0.67 nM
Non specific neurotensin (1 µM)
binding
Reference neurotensin (IC 50 : 4 nM)
Ref. 0465
Q 4 weeks
Schotte, A. et al. (1986) Naun.-Sch. Arch. Pharm., 333: 400-405.
specific binding (% of control)
100
50
0
-10 -9 -8 -7 -6 -5
log [drug] (M)
neurotensin
levocabastine
NT (non-selective)
Source
rat stomach fundus
100
tissue
Ref. 0327
Q 4 weeks
Agonist neurotensin (pD 2 = 9)
Antagonist SR 142948
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Quirion, R. et al. (1980) Brit. J. Pharmacol., 68: 83-91.
tension (% of max.)
50
0
-11 -10 -9 -8
log [agonist] (M)
NTS 1 (NT 1 ) - agonist radioligand
binding
Ref. 0109
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 125 I]Tyr 3 -neurotensin (0.05 nM)
0.22 nM
neurotensin (1 µM)
neurotensin (IC 50 : 0.3 nM)
Vita, N. et al. (1993) FEBS Lett., 317: 139-142.
NTS 1 (NT 1 )
cellul ar
Ref. 1612 Agonist effect
Ref. 1634 Antagonist effect
Q 3 weeks
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control neurotensin (1 µM)
Reference neurotensin (EC 50 : 8.7 nM)
Antagonist effect Stimulant neurotensin (100 nM)
Reference SR142948 (IC 50 : 720 nM)
Gully, D. et al. (1997) J. Pharmacol. Exp. Ther., 280: 802-812.
[Solvent] must be kept 0.1%
NTS 2
cellul ar
Ref. 1919 Agonist effect
Ref. 1920 Antagonist effect
Q 3 weeks
Source
human recombinant (HEK-293 cells)
Measured product impedance
Detection method cellular dielectric spectroscopy
Agonist effect Control SR142948 (300 nM)
Reference SR142948 (EC 50 : 15 nM)
Antagonist effect Stimulant SR142948 (50 nM)
Reference neurotensin (IC 50 : 99 nM)
Davisvita, N., (1998) Eur. J. Pharmacol., 360: 265-272.
[Solvent] must be kept 0.1%
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ For nicotinic assays, see "Other receptors",
page 89
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Assay developed in 2010 New assay conditions Human Q Standard turnaround time

59
Cerep
services
❚ opioid and opioid-like
Receptors
[GPCRs]
opioid (non-selective) - antagonist radioligand
binding
Ref. 0112
Q 3 weeks
Included in:
Diversity profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]naloxone (1 nM)
2.6 nM
naloxone (1 µM)
naloxone (IC 50 : 1.5 nM)
Childers, S.R. et al. (1979) Eur. J. Pharmacol., 55: 11-18.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6
log [drug] (M)
naloxone
DAMGO
U 50488
DPDPE
Ion
channels
Transporters
delta 2 (DOP) - agonist radioligand
binding
Ref. 0114
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]DADLE (0.5 nM)
0.73 nM
naltrexone (10 µM)
DPDPE (IC 50 : 1.8 nM)
Simonin, F. et al. (1994) Mol. Pharmacol., 46: 1015-1021.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
DPDPE
naloxone
DAMGO
U 50488
Kinases
Epigenetic &
DNA-related
enzymes
delta 2 (DOP)
cellul ar
Ref. 2568
Ref. 2571
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
NG-10815 cells (endogenous)
Measured product impedance
Detection method cellular dielectric spectroscopy
Agonist effect Control DPDPE (1 µM)
Reference DPDPE (EC 50 : 1.36 nM)
Antagonist effect Stimulant DPDPE (30 nM)
Reference naltrindole (IC 50 : 0.32 nM)
Law, P.Y. and Loh, H.H. (1993) Mol. Pharmacol., 43: 684-693.
[Solvent] must be kept 0.1%
Other
enzymes
Specialized
cellular
assays
delta 2 (DOP)
tissue
Ref. 0328
Q 4 weeks
Source
hamster vas deferens (field-stimulated)
Agonist DPDPE (pD 2 = 7.7)
Antagonist naltrindole (pA 2 = 9.7)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
McKnight, A.T. et al. (1985) Neuropharmacol., 24: 1011-1017.
tension (% of control)
100
50
0
-10 -9 -8 -7 -6
log [agonist] (M)
naltrindole
none
0.3 nM
1 nM
3 nM
Standard
profiles
Testing
conditions
kappa (KOP) - agonist radioligand
binding
Ref. 1971
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat recombinant (CHO cells)
[ 3 H]U 69593 (1 nM)
2 nM
naloxone (10 µM)
U 50488 (IC 50 : 0.84 nM)
Meng, F. et al. (1993) Proc. Natl. Acad. Sci. USA, 90: 9954-9958.
specific binding (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
U 50488
naloxone
DPDPE
DAMGO
Ordering
information
Assay list
& index

60 in vitro pharmacology 2011 catalog
❚ opioid and opioid-like
kappa (KOP)
cellul ar
Ref. 2071
Ref. 2072
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
rat recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control U 50488 (1 µM)
Reference U 50488 (EC 50 : 1.1 nM)
Antagonist effect Stimulant U 50488 (100 nM)
Reference nor-BNI (IC 50 : 9.2 nM)
Avidor-Reiss, T. et al. (1995) FEBS Lett., 361: 70-74.
cAMP modulation (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5 -4 -11 -10 -9 -8 -7 -6 -5
log [agonist] (M)
U 50488
U 69593
DAMGO
DPDPE
100
50
0
log [antagonist] (M)
nor-BNI
naloxone
naltrexone
DGNTI
kappa (KOP)
tissue
Ref. 0329
Q 4 weeks
Source
rabbit vas deferens (field-stimulated)
Agonist U 69593 (pD 2 = 7.8)
Antagonist nor-BNI (pA 2 = 10.8)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Oka, T. et al. (1980) Eur. J. Pharmacol., 73: 235-236.
tension (% of control)
-12 -11
-12 -11
-11 -10
100-12 -11
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7
-10 -9 -8 -7
50
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
0
-11 -10
-9 -8 -7 -6 -5 -4
-13 -12 -11 -10 -9 -8 -7 -6
-10 -9 -8 -7 -6
log [agonist] (M)
-12 -11 -10 -9 -8 -7 -6 -5 -4
nor-BNI
none
0.1 nM
0.3 nM
1 nM
mu (MOP) - antagonist radioligand
Source
human recombinant (HEK-293 cells)
Ligand
[ 3 H]diprenorphine (0.4 nM)
Kd
0.14 nM
Non specific naltrexone (1 µM)
binding
Reference naltrexone (IC 50 : 1.1 nM)
Ref. 1666
Q 3 weeks
Zhang, S. et al. (1998) J. Pharmacol. Exp. Ther., 286: 136-141.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
naltrexone
DAMGO
U 50488
DPDPE
mu (MOP) - agonist radioligand
binding
Ref. 0118
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
BioPrint ® profile
Organ safety profile
mu (MOP)
cellul ar
Ref. 1392
Ref. 1393
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (HEK-293 cells)
[ 3 H]DAMGO (0.5 nM)
0.35 nM
naloxone (10 µM)
DAMGO (IC 50 : 0.537 nM)
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5
log [drug] (M)
Wang, J.-B. et al. (1994) FEBS Lett., 338: 217-222.
[Custom offer] rat brain model (Ref. 0117), please contact us at customresearch@cerep.com
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control DAMGO (1 µM)
Reference DAMGO (EC 50 : 2.8 nM)
Antagonist effect Stimulant DAMGO (30 nM)
Reference CTOP (IC 50 : 335 nM)
Wang, J.B. et al. (1994) FEBS Lett., 338: 217-222.
cAMP modulation (% of control)
100
50
0
log [agonist] (M)
DAMGO
DPDPE
fentanyl
morphine
100
[Solvent] must be kept ≤ 0.3%
DAMGO
naloxone
U 50488
DPDPE
-12 -11 -10 -9 -8 -7 -6 -5 -10 -9 -8 -7 -6 -5
50
0
log [antagonist] (M)
CTOP
naltrexone
naltrindole
naloxone
mu (MOP)
tissue
Ref. 0330
Q 4 weeks
Source
guinea-pig ileum (field-stimulated)
Agonist DAMGO (pD 2 = 8.3)
Antagonist naloxone (pA 2 = 8.8)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Hutchinson, M. et al. (1975) Brit. J. Pharmacol., 55: 541-546.
tension (% of control)
-12 -11
-12 -11
-11 -10
100-12 -11
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7
-10 -9 -8 -7
50 -10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
0
-11 -10
-9 -8 -7 -6 -5 -4
-13 -12 -11 -10 -9 -8 -7 -6
log [agonist] (M)
-12 -11 -10 -9 -8 -7 -6 -5 -4
-10 -9 -8 -7 -6
naloxone
none
3 nM
10 nM
30 nM

61
NOP (ORL1) - agonist radioligand
binding
Ref. 0358
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (HEK-293 cells)
[ 3 H]nociceptin (0.2 nM)
0.4 nM
nociceptin (1 µM)
nociceptin (IC 50 : 1.1 nM)
Ardati, A. et al. (1997) Mol. Pharmacol., 51: 816-824.
specific binding (% of control)
opioid and opioid-like ❚
100
50
nociceptin
DAMGO
0
DPDPE
U 50488
-12 -11 -10 -9 -8 -7 -6 -5
log [drug] (M)
Cerep
services
Receptors
[GPCRs]
NOP (ORL1)
cellul ar
Ref. 2381 Agonist effect
Ref. 2382 Antagonist effect
Q 3 weeks
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control nociceptin (10 nM)
Reference nociceptin (EC 50 : 0.1 nM)
Antagonist effect Stimulant nociceptin (1 nM)
Reference UFP-101 (IC 50 : 64 nM)
New, D.C. and Wong, Y.H. (2002) Neurosign., 11: 197-212.
[Solvent] must be kept 0.3%
Ion
channels
Transporters
NOP (ORL1)
tissue
Ref. 1226
Q 4 weeks
Source
mouse vas deferens (field-stimulated)
Agonist nociceptin (pD 2 = 7.9)
Antagonist UFP-101
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Calo, G. et al. (2002) Brit. J. Pharmacol., 136: 303-311.
tension (% of control)
100
50
0
log [agonist] (M)
-11 -10 -9 -8 -7 -6
Kinases
Epigenetic &
DNA-related
enzymes
❚ Orexin
Other
enzymes
OX 1 - agonist radioligand
Source
human recombinant (CHO cells)
Ligand
[ 125 I]orexin-A (0.1 nM)
binding
Kd
10 nM
Ref. 1987
Non specific SB 334867 (1 µM)
Q 3 weeks
Reference orexin-A (IC 50 : 0.49 nM)
Included in:
Organ safety profile
Langmead, C.J. et al. (2004) Brit. J. Pharmacol., 141: 340-346.
Specialized
cellular
assays
Standard
profiles
OX 1
cellul ar
Ref. 2234
Ref. 2235
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control orexin-A (10 nM)
Reference orexin-A (EC 50 : 0.8 nM)
Antagonist effect Stimulant orexin-A (3 nM)
Reference SB 334867 (IC 50 : 210 nM)
Smart, D. et al. (2001) Brit. J. Pharmacol., 132: 1179-1182.
Ca 2+ mobilization (% of control)
100
100
50
50
0
0
-9 -8 -7 -6 -8 -11 -10 -7 -6 -5
log [agonist] (M)
log [antagonist] (M)
orexin-A
SB 334867
orexin-B
SB 408124
[Ala 11 ,D-Leu 15 ]-orexin-B
[Solvent] must be kept ≤ 0.3%
Testing
conditions
Ordering
information
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
-12 -11
-11 -10 -9 -8 -7 -6 -5 -4
-12 -11
-10 -9 -8 -7
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: -12 -11+86 -10 -921 -8 5132 -7 0568
Assay developed in 2010 New assay conditions Human Q Standard turnaround time
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
-11 -10
-9 -8 -7 -6 -5 -4
Assay list
& index

62 in vitro pharmacology 2011 catalog
❚ orexin
OX 2 - agonist radioligand
Source
human recombinant (HEK-293 cells)
Ligand
[ 125 I]orexin-A (0.04 nM)
binding
Kd
0.2 nM
Ref. 1988
Non specific orexin-B (1 µM)
Q 3 weeks
Reference orexin-B (IC 50 : 0.21 nM)
Included in:
Organ safety profile
Wieland, H.A. et al. (2002) Eur. J. Biochem., 269: 1128-1135.
OX 2
cellul ar
Ref. 2349
Ref. 2350
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (HEK-293 cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control orexin-B (1 µM)
Reference orexin-B (EC 50 : 3.7 nM)
Antagonist effect Stimulant orexin-B (10 nM)
Reference unavailable
Ammoun, S. et al. (2003) J. Pharmacol. Exp. Ther., 305: 507-514.
Ca 2+ mobilization (% of control)
100
antagonist effect:
50
no graph available
0
-9 -8 -7 -6
-11 -10
log [agonist] (M)
orexin-B
orexin-A
[Ala 11 ,D-Leu 15 ]-orexin-B
[Solvent] must be kept ≤ 0.3%
❚ orphans (class a)
GPR119
cellul ar
Ref. 3297
Ref. 3299
Q 3 weeks
Agonist effect
Antagonist effect
Source
HIT-T15 cells (endogenous)
Measured product cAMP
Detection method HTRF
Agonist effect Control AR231453 (10 µM)
Reference AR231453 (EC 50 : 71 nM)
Antagonist effect Stimulant AR231453 (300 nM)
Reference unavailable
Chu, Z.L et al.(2008) Endocrinology, 149: 2038-2047.
-12 -11
-12 -11
-11 -10 -9 -8 -7 -6 -5 -4
-12 -11
-10 -9 -8 -7
-10 -9 -8 -7
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
-11 -10
-9 -8 -7 -6 -5 -4
-12 -11 -10 -9 -8 -7 -6 -5 -4 -3
❚ parathyroid hormone
PTH1
cellul ar
Ref. 2660
Ref. 2661
Q 3 weeks
Agonist effect
Antagonist effect
Source
SaOS2 cells (endogenous)
Measured product cAMP
Detection method HTRF
Agonist effect Control PTHrP (1-34) (1 µM)
Reference PTHrP (1-34) (EC 50 : 1.7 nM)
Antagonist effect Stimulant PTHrP (1-34) (10 nM)
Reference PTHrP (7-34) (IC 50 : 84 nM)
Orloff, J.J. et al. (1992) Endocrinol., 131: 1603-1611.
[Solvent] must be kept 0.3%
❚ platelet activating factor
PAF - agonist radioligand
binding
Ref. 0915
Q 3 weeks
Included in:
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]C 16 -PAF (1.5 nM)
1.5 nM
WEB 2086 (10 µM)
C 16 -PAF (IC 50 : 2.4 nM)
Fukunaga, K. et al. (2001) J.Biol.Chem., 276: 43025-43030.
specific binding (% of control)
100
50
0
C 16-PAF
WEB 2086
-12 -11 -10 -9 -8 -7 -6 -5
log [drug] (M)

63
platelet activating factor ❚
PAF
cellul ar
Ref. 1610
Ref. 1611
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control C 16 -PAF (100 nM)
Reference C 16 -PAF (EC 50 : 0.36 nM)
Antagonist effect Stimulant C 16 -PAF (1 nM)
Reference WEB 2086 (IC 50 : 3 µM)
Fukunaga, K. et al. (2001) J. Biol. Chem., 276: 43025-43030.
Ca 2+ mobilization (% of control)
100
100
50
50
0
0
-10 -9 -8 -7 -6 -8 -7 -6 -5 -4
log [agonist] (M)
log [antagonist] (M)
C 16-PAF WEB 2086
[Solvent] must be kept ≤ 0.1%
Cerep
services
Receptors
[GPCRs]
❚ prokineticin
-12 -11
-10 -9 -8 -7 -6 -5
Ion
channels
-9 -8 -7 -6 -5
-10 -4
PK 1
cellul ar
Ref. 2449
Ref. 2451
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (HEK-293 cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control PK1 (30 nM)
Reference PK1 (EC 50 : 0.82 nM)
Antagonist effect Stimulant PK1 (3 nM)
Reference unavailable
Chen, J. et al. (2005) Mol. Pharmacol., 67: 2070-2076.
[Solvent] must be kept 0.1%
Transporters
Kinases
PK 2
cellul ar
Ref. 2450
Ref. 2452
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (HEK-293 cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control PK2 (10 nM)
Reference PK2 (EC 50 : 1.1 nM)
Antagonist effect Stimulant PK2 (2 nM)
Reference unavailable
Chen, J. et al. (2005) Mol. Pharmacol., 67: 2070-2076.
[Solvent] must be kept 0.1%
Epigenetic &
DNA-related
enzymes
Other
enzymes
❚ prostanoid
Specialized
cellular
assays
DP 1 - agonist radioligand
Source
human recombinant (1321N1 cells)
Ligand
[ 3 H]PGD 2 (1.5 nM)
Kd
1.2 nM
Non specific BW245C (1 µM)
binding
Reference BW245C (IC 50 : 2.3 nM)
Ref. 2517
Q 3 weeks
Wright, D.H. et al.(1998) Br. J. Pharmacol., 123: 1317-1324.
Standard
profiles
Testing
conditions
DP 1
cellul ar
Ref. 2484
Ref. 2486
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control BW 245C (1 µM)
Reference BW 245C (EC 50 : 2.4 nM)
Antagonist effect Stimulant BW 245C (30 nM)
Reference MK 0524 (IC 50 : 3.4 nM)
Wright, D.H. et al. (1998) Brit. J. Pharmacol., 123: 1317-1324.
α
[Solvent] must be kept 0.3%
Ordering
information
Assay list
& index

64 in vitro pharmacology 2011 catalog
❚ prostanoid
EP 1 - agonist radioligand
Source
human recombinant (HEK-293 cells)
Ligand
[ 3 H]PGE 2 (1.5 nM)
Kd
1.5 nM
Non specific PGE 2 (10 µM)
binding
Reference PGE 2 (IC 50 : 1.4 nM)
Ref. 0440
Q 3 weeks
Sharif, N.A. and Davis, T.L. (2002) J. Pharm. Pharmacol., 54: 539-547.
specific binding (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
PGE2
AH 6809
butaprost
AH 23848
EP 1
cellul ar
Ref. 2053
Ref. 2054
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (HEK-293 cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control PGE 2 (100 nM)
Reference PGE 2 (EC 50 : 0.88 nM)
Antagonist effect Stimulant PGE 2 (3 nM)
Reference SC 51322 (IC 50 : 53.7 nM)
Ungrin, M.D. et al. (1999) Analytical Biochem., 272: 34-42.
Ca 2+ mobilization (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5 -4
log [agonist] (M)
PGE2
17-phenyl PGE2
PGF2α
U 44069
100
[Solvent] must be kept ≤ 0.1%
50
0
-9 -8 -7 -6 -5
log [antagonist] (M)
SC 51322
AL 8810
AH 23848
AH 6809
EP 2 - agonist radioligand
binding
Ref. 1955
Q 3 weeks
Included in:
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (HEK-293 cells)
[ 3 H]PGE 2 (3 nM)
3 nM
PGE 2 (10 µM)
PGE 2 (IC 50 : 1.7 nM)
Abramovitz, M. et al. (2000) Biochem. Biophys. Acta., 1483: 285-293.
-12 -11
-12 -11
-11 -10
-12 -11
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7
-10 -9 -8 -7
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
-11 -10
-9 -8 -7 -6 -5 -4
EP 2
cellul ar
Ref. 1956
Ref. 1957
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control PGE 2 (10 µM)
Reference PGE 2 (EC 50 : 100 nM)
Antagonist effect Stimulant PGE 2 (300 nM)
Reference AH 6809 (IC 50 : 3.9 µM)
Wilson, R.J. et al. (2004) Eur. J. Pharmacol., 501: 49-58.
cAMP modulation (% of control)
100
100
50
50
0
0
-9 -8 -7 -6 -5
-8 -7 -6 -5 -4
log [agonist] (M)
log [antagonist] (M)
PGE2
AH 6809
butaprost
AH 23848
AH 13205
U 44069
[Solvent] must be kept ≤ 0.3%
EP 3 - agonist radioligand
Source
human recombinant (HEK-293 cells)
Ligand
[ 3 H]PGE 2 (0.5 nM)
Kd
0.8 nM
Non specific PGE 2 (1 µM)
binding
Reference sulprostone (IC 50 : 2.9 nM)
Ref. 2774
Q 3 weeks
Abramovitz, M. et al. (2000) Biochem. Biophys. Acta., 1483: 285-293.
-12 -11
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
EP 3
cellul ar
Ref. 2577
Ref. 2578
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (HEK-293 cells)
Measured product impedance
Detection method cellular dielectric spectroscopy
Agonist effect Control sulprostone (10 nM)
Reference sulprostone (EC 50 : 0.058 nM)
Antagonist effect Stimulant sulprostone (0.1 nM)
Reference unavailable
Asboth, G. et al. (1996) Endocrinol., 137: 2572-2579.
[Solvent] must be kept 0.1%

65
prostanoid ❚
EP 4 - agonist radioligand
Source
human recombinant (HEK-293 cells)
Ligand
[ 3 H]PGE 2 (0.5 nM)
Kd
0.3 nM
Non specific PGE 2 (10 µM)
binding
Reference PGE 2 (IC 50 : 1.9 nM)
Ref. 0441
Q 3 weeks
Abramovitz, M. et al. (2000) Biochem. Biophys. Acta., 1483: 285-293.
α
Cerep
services
Receptors
[GPCRs]
EP 4
cellul ar
Ref. 1871
Ref. 1872
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control PGE 2 (1 µM)
Reference PGE 2 (EC 50 : 7.1 nM)
Antagonist effect Stimulant PGE 2 (30 nM)
Reference unavailable
Wilson, R.J. et al. (2004) Eur. J. Pharmacol., 501: 49-58.
cAMP modulation (% of control)
100
50
0
-12 -11
-10 -9 -8 -7 -6 -5
log [agonist] (M)
PGE2
thromboxane
17-phenyl PGE2
[Solvent] must be kept ≤ 0.3%
-4
antagonist effect:
no graph available
Ion
channels
Transporters
FP - agonist radioligand
binding
Ref. 1979
Q 3 weeks
Included in:
BioPrint ® profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (HEK-293 cells)
[ 3 H]PGF 2a (2 nM)
3.83 nM
cloprostenol (10 µM)
PGF 2a (IC 50 : 2.02 nM)
Abramovitz, M. et al. (2000) Biochem. Biophys. Acta., 1483: 285-293.
specific binding (% of control)
100
50
-9 -8 -7 -6 -5
-10 -4
0
-12 -11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
PGF2α
cloprostenol
latanoprost
AH 23848
Kinases
Epigenetic &
DNA-related
enzymes
FP
cellul ar
Ref. 2011
Ref. 2013
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (HEK-293 cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control PGF 2a (1 µM)
Reference PGE 2a (EC 50 : 1.9 nM)
Antagonist effect Stimulant PGF 2a (10 nM)
Reference unavailable
Sharif, N.A. et al. (2003) Prost. Leuk. Ess. Fatty Acids, 68: 27-33.
Ca 2+ mobilization (% of control)
100
50
0
-11 -10
log [agonist] (M)
PGF2α
cloprostenol
latanoprost
PGE2
-9 -8 -7 -6
[Solvent] must be kept ≤ 0.1%
antagonist effect:
no graph available
Other
enzymes
Specialized
cellular
assays
IP (PGI 2 ) - agonist radioligand
binding
Ref. 2230
Q 3 weeks
Included in:
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (HEK-293 cells)
[ 3 H]iloprost (10 nM)
8 nM
iloprost (10 µM)
iloprost (IC 50 : 22 nM)
Abramovitz, M. et al. (2000) Biochem. Biophys. Acta., 1483: 285-293.
specific binding (% of control)
-12 -11
-12 -11
-11 -10
100
-12 -11
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7
-10 -9 -8 -7
50 -10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
0
-11 -10
-9 -8 -7 -6 -5 -4
-12 -11 -10 -9 -8 -7 -6 -5 -4 -3
-12 -11 -10 -9 -8 -7 -6 -5
log [drug] (M)
iloprost
PGF2α
U 46619
U 44069
Standard
profiles
Testing
conditions
IP (PGI 2 )
cellul ar
Ref. 2228 Agonist effect
Ref. 2229 Antagonist effect
Q 3 weeks
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control iloprost (100 nM)
Reference iloprost (EC 50 : 0.68 nM)
Antagonist effect Stimulant iloprost (5 nM)
Reference unavailable
Boie, Y. et al. (1994) J. Biol. Chem., 269: 12173-12178.
cAMP modulation (% of control)
100
50
0
-13
-12 -11
iloprost
PGI2
PGE2
PGF2α
-10 -9 -8 -7 -6
log [agonist] (M)
[Solvent] must be kept ≤ 0.3%
antagonist effect:
no graph available
Ordering
information
Assay list
& index
-11 -10
-9 -8 -7 -6 -5 -4
-12 -11
-10 -9 -8 -7

66 in vitro pharmacology 2011 catalog
❚ prostanoid
TP (TXA 2 /PGH 2 ) - antagonist radioligand
binding
Ref. 2048
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (HEK-293 cells)
[ 3 H]SQ 29548 (5 nM)
4 nM
U 44069 (10 µM)
U 44069 (IC 50 : 12 nM)
Abramovitz, M. et al. (2000) Biochem. Biophys. Acta., 1483: 285-293.
specific binding (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5 -4 -3
log [drug] (M)
U 44069
U 46619
PGF2α
PGE2
TP (TXA 2 /PGH 2 )
cellul ar
Ref. 2059 Agonist effect
Ref. 2060 Antagonist effect
Q 3 weeks
Source
human recombinant (HEK-293 cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control U 44069 (1 µM)
Reference U 44069 (EC 50 : 5 nM)
Antagonist effect Stimulant U 44069 (30 nM)
Reference L 670596 (IC 50 : 25 nM)
Elmhurst, J.L. et al. (1997) J. Pharmacol. Exp. Ther., 283: 1198-1205.
Ca 2+ mobilization (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4 -10 -9 -8 -7 -6 -5
log [agonist] (M)
U 44069
U 46619
PGE2
PGF2α
100
[Solvent] must be kept ≤ 0.1%
50
0
log [antagonist] (M)
L 670596
SQ 29548
AL 8810
AH 6809
-11 -10
-9 -8 -7 -6 -5 -4
-12 -11
-10 -9 -8 -7
-11 -10
-9 -8 -7 -6 -5 -4
-12 -11
-10 -9 -8 -7
-12 -11
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
❚ proteinase-activated
PAR1 - agonist radioligand
binding
Ref. 2592
Q 3 weeks
Included in:
Diversity profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (KNRK cells)
[ 3 H]ha-TRAP (0.5 nM)
0.25 nM
ha-TRAP (10 µM)
ha-TRAP (IC 50 : 1.3 nM)
Ahn, H.S. et al. (1997) Mol. Pharmacol., 51: 350-356.
PAR1
cellul ar
Ref. 2332
Ref. 2333
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (KNRK cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control TFLLR-NH 2 (100 µM)
Reference TFLLR-NH 2 (EC 50 : 3.6 µM)
Antagonist effect Stimulant TFLLR-NH 2 (10 µM)
Reference SCH 79797 (IC 50 : 935 nM)
Kawabata, A. et al. (1999) J. Pharmacol. Exp. Ther., 288: 358-370.
Ca 2+ mobilization (% of control)
100
100
50
50
0
0
-10 -9 -8 -7 -6 -5 -4 -9 -8 -7 -6 -5
-12 -11 -4
log [agonist] (M)
log [antagonist] (M)
TFLLR-NH 2
SCH 79797
SLIGRL-NH
2
FSLLRY-NH
2
thrombin
3-mercaptopropionyl-F-Cha-
trypsin
Cha-RKPBDK-NH 2
tcY-NH 2
[Solvent] must be kept ≤ 0.1%
PAR2 - agonist radioligand
Source
human recombinant (Hela cells)
Ligand
[ 3 H]2-fuoryl-LIGRL-NH 2 (2.5 nM)
binding
Kd
13 nM
Ref. 2424
Non specific 2-fuoryl-LIGRL-NH 2 (10 µM)
Q 3 weeks
Reference SLIGRL-NH 2 (IC 50 : 67 nM)
Included in:
Organ safety profile
Kanke, T. et al. (2005) Brit. J. Pharmacol., 145: 255-263.
-12 -11
-12 -11
-11 -10
-12 -11
-7 -6 -5 -9 -8 -4
-10 -9 -8 -7
-10 -9 -8 -7
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
-11 -10
-9 -8 -7 -6 -5 -4

67
proteinase-activated ❚
PAR2
cellul ar
Ref. 2323
Ref. 2324
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (Hela cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control trypsin (100 µM)
Reference trypsin (EC 50 : 169 nM)
Antagonist effect Stimulant trypsin (1 µM)
Reference unavailable
Kawabata, A. et al. (1999) J. Pharmacol. Exp. Ther., 288: 358-370.
[Solvent] must be kept 0.1%
Cerep
services
Receptors
[GPCRs]
❚ purinergic
Ion
channels
P2Y - agonist radioligand
binding
Ref. 0128
Q 3 weeks
Included in:
High-throughput profile
Diversity profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 35 S]dATPαS (10 nM)
10 nM
dATPαS (10 µM)
dATPαS (IC 50 : 20 nM)
Simon, J. et al. (1995) Pharmacol. Toxicol., 76: 302-307.
specific binding (% of control)
100
50
0
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
dATPαS
ADPβS
suramin
α,β-MeATP
Transporters
Kinases
P2Y 1
cellul ar
Ref. 2132
Ref. 2134
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (1321N1 cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control MRS 2365 (100 nM)
Reference MRS 2365 (EC 50 : 0.24 nM)
Antagonist effect Stimulant MRS 2365 (1 nM)
Reference MRS 2500 (IC 50 : 39.3 nM)
Chhatriwala, M. et al. (2004) J. Pharmacol. Exp. Ther., 311: 1038-1043.
[Solvent] must be kept 0.1%
Epigenetic &
DNA-related
enzymes
Other
enzymes
P2Y 2
cellul ar
Ref. 2164
Ref. 2167
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (1321N1 cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control UTP (3 µM)
Reference UTP (EC 50 : 60 nM)
Antagonist effect Stimulant UTP (300 nM)
Reference unavailable
Kassack, M.U. et al. (2002) J. Biomol. Screen., 7: 233-246.
Ca 2+ mobilization (% of control)
100
50
0
-9 -8 -7 -6 -5
-10 -4
log [agonist] (M)
UTP
UDP
MRS 2365
2MeSADP
[Solvent] must be kept ≤ 0.1%
antagonist effect:
no graph available
Specialized
cellular
assays
Standard
profiles
P2Y 4
cellul ar
Ref. 2165
Ref. 2168
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (1321N1 cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control UTP (100 nM)
Reference UTP (EC 50 : 1.9 nM)
Antagonist effect Stimulant UTP (10 nM)
Reference unavailable
Herold, C.L. et al. (2004) J. Biol. Chem., 279: 11456-11464.
Ca 2+ mobilization (% of control)
-12 -11
-12 -11
100 -12 -11
50
-10 -9 -8 -7
-10 -9 -8 -7 -6 -5
0
-11 -10
-9 -8-12 -7 -11 -10 -6 -9-5
-10 -8-4-7 -6 -5 -4
-9 -8 -7 -6 -5 -4
-12 -11 -10 -9 -8 -7 -6 -5 -4 -3
antagonist effect:
-10 -9 -8 -7
no graph available
log [agonist] (M)
UTP
UDP
MRS 2365
2MeSADP
[Solvent] must be kept ≤ 0.1%
Testing
conditions
Ordering
information
-11 -10
-9 -8 -7 -6 -5 -4
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
-12 -11
-11 -10
-12 -11
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
-11 -10
-9 -8 -7 -6 -5 -4
-12 -11 -10 -9 -8 -7 -6 -5 -4 -3
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: -12 -11+86 -10 -921 -8 5132 -7 0568
Assay developed in 2010 New assay conditions Human Q Standard turnaround time
-12 -11 -10 -9 -8 -7 -6 -5 -4
Assay list
& index

68 in vitro pharmacology 2011 catalog
❚ purinergic
P2Y 6
cellul ar
Ref. 2166
Ref. 2169
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (1321N1 cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control UDP (1 µM)
Reference UDP (EC 50 : 13 nM)
Antagonist effect Stimulant UDP (100 nM)
Reference unavailable
Li, Q. et al. (1998) Mol. Pharmacol., 54: 541-546.
Ca 2+ mobilization (% of control)
100
50
0
-9 -8 -7 -6 -5
-10 -4
log [agonist] (M)
UDP
2MeSADP
UTP
MRS 2365
[Solvent] must be kept ≤ 0.1%
antagonist effect:
no graph available
❚ See other Purinergic assays, pp. 90 and 101
-11 -10
-9 -8 -7 -6 -5 -4
❚ relaxin
-12 -11
-12 -11
-12 -11
-10 -9 -8 -7
-10 -9 -8 -7
-10 -9 -8 -7 -6 -5
-11 -10
-9 -8 -7 -6 -5 -4
-12 -11 -10 -9 -8 -7 -6 -5 -4 -3
RXFP1 - agonist radioligand
Source
human recombinant (HEK-293 cells)
Ligand
[ 125 I]H2 relaxin (0.02 nM)
Kd
0.23 nM
Non specific H2 relaxin (100 nM)
binding
Reference H2 relaxin (IC 50 : 1.1 nM)
Ref. 2058
Q 3 weeks
Halls, M.L. et al. (2005) J. Pharm. Exp. Ther., 313: 677-687.
-9 -8 -7 -6 -5
-10 -4
specific binding (% of control)
100
50
0
-13 -12 -11 -10 -9 -8 -7 -6 -5
log [drug] (M)
H2 relaxin
INSL3
INSL5
relaxin 3B chain
RXFP1
cellul ar
Ref. 2130
Ref. 2131
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (HEK-293 cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control H2 relaxin (100 nM)
Reference H2 relaxin (EC 50 : 3 nM)
Antagonist effect Stimulant H2 relaxin (10 nM)
Reference unavailable
Wilkinson, T.N. et al. (2005) BMC Evol. Biol., 5: 14.
[Solvent] must be kept 0.3%
❚ serotonin
5-HT (non-selective) - agonist radioligand
binding
Ref. 0129
Q 3 weeks
Included in:
Diversity profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]serotonin (2.5 nM)
2.5 nM
serotonin (10 µM)
serotonin (IC 50 : 1.3 nM)
Peroutka, S.J. and Snyder, S.H. (1979) Mol. Pharmacol., 16: 687-699.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5
log [drug] (M)
serotonin
8-OH-DPAT
ketanserin
MDL 72222
5-HT 1A - agonist radioligand
binding
Ref. 0131
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (HEK-293 cells)
[ 3 H]8-OH-DPAT (0.3 nM)
0.5 nM
8-OH-DPAT (10 µM)
8-OH-DPAT (IC 50 : 0.36 nM)
Mulheron, J.G. et al. (1994) J. Biol. Chem., 269: 12954-12962.
specific binding (% of control)
100
50
8-OH-DPAT
serotonin
ketanserin
0
MDL 72222
-11 -10 -9 -8 -7 -6 -5 -4 -3
log [drug] (M)

serotonin ❚
69
5-HT 1A
cellul ar
Ref. 2093
Ref. 2101
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control 8-OH-DPAT (100 nM)
Reference 8-OH-DPAT (EC 50 : 0.85 nM)
Antagonist effect Stimulant 8-OH-DPAT (10 nM)
Reference WAY 100635 (IC 50 : 20.5 nM)
Newman-Tancredi, A. et al. (2001) Brit. J. Pharmacol., 132: 518-524.
α
[Solvent] must be kept 0.3%
Cerep
services
Receptors
[GPCRs]
5-HT 1B - antagonist radioligand
binding
Ref. 0132
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 125 I]CYP (0.1 nM) (+ 30 µM (-)propranolol)
0.16 nM
serotonin (10 µM)
serotonin (IC 50 : 10 nM)
Hoyer, D. et al. (1985) Eur. J. Pharmacol., 118: 1-12.
specific binding (% of control)
100
50
serotonin
ketanserin
0
8-OH-DPAT
MDL 72222
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
Ion
channels
Transporters
5-HT 1B
cellul ar
Ref. 2600
Ref. 2604
Q 3 weeks
Agonist effect
Antagonist effect
Source
CHO cells (endogenous)
Measured product impedance
Detection method cellular dielectric spectroscopy
Agonist effect Control serotonin (1 µM)
Reference serotonin (EC 50 : 5.3 nM)
Antagonist effect Stimulant serotonin (30 nM)
Reference GR 127935 (IC 50 : 9.18 nM)
Giles, H. et al. (1996) Brit. J. Pharmacol., 117: 1119-1126.
[Solvent] must be kept 0.1%
Kinases
Epigenetic &
DNA-related
enzymes
5-HT 1D - agonist radioligand
binding
Ref. 1974
Q 3 weeks
Included in:
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat recombinant (CHO cells)
[ 3 H]serotonin (1 nM)
0.5 nM
serotonin (10 µM)
serotonin (IC 50 : 1.82 nM)
Wurch T. et al. (1997) J. Neurochem., 68: 410-418.
Other
enzymes
Specialized
cellular
assays
5-HT 1D
cellul ar
Ref. 2496
Ref. 2499
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
rat recombinant (CHO cells)
Measured product impedance
Detection method cellular dielectric spectroscopy
Agonist effect Control serotonin (100 nM)
Reference serotonin (EC 50 : 0.6 nM)
Antagonist effect Stimulant serotonin (3 nM)
Reference methiothepin (IC 50 : 408 nM)
Wurch, T. et al. (1997) J. Neurochem., 68: 410-418.
[Solvent] must be kept 0.1%
Standard
profiles
Testing
conditions
5-HT 2A - antagonist radioligand
binding
Ref. 0135
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (HEK-293 cells)
[ 3 H]ketanserin (0.5 nM)
0.6 nM
ketanserin (1 µM)
ketanserin (IC 50 : 0.73 nM)
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4 -3
log [drug] (M)
Bonhaus, D.W. et al. (1995) Brit. J. Pharmacol., 115: 622-628.
[Custom offer] rat brain model (Ref. 0134), please contact us at customresearch@cerep.com
ketanserin
serotonin
8-OH-DPAT
MDL 72222
Ordering
information
Assay list
& index

70 in vitro pharmacology 2011 catalog
❚ serotonin
5-HT 2A - agonist radioligand
binding
Ref. 0471
Q 3 weeks
Included in:
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (HEK-293 cells)
[ 125 I](±)DOI (0.1 nM)
0.3 nM
(±)DOI (1 µM)
(±)DOI (IC 50 : 0.27 nM)
Bryant, H.U. et al. (1996) Life Sci., 15: 1259-1268.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6
log [drug] (M)
(+)DOI -
serotonin
mesulergine
ketanserin
5-HT 2A
cellul ar
Ref. 3196
Ref. 3198
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
human recombinant (HEK-293 cells)
Measured product IP 1
Detection method HTRF
Agonist effect Control serotonin (10 µM)
Reference serotonin (EC 50 : 27 nM)
Antagonist effect Stimulant serotonin (100 nM)
Reference ketanserin (IC 50 : 24.2 nM)
Porter, R.H.P. et al.(1999) Brit. J. Pharmacol., 128: 13-20.
Ca 2+ mobilization (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5 -4
log [agonist] (M)
serotonin
(±)DOI
5-methoxytryptamine
BW 723C86
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5 -4
log [antagonist] (M)
ketanserin
mesulergine
SB 206553
SB 204741
5-HT 2A
tissue
Ref. 0334
Q 4 weeks
Source
rabbit aorta (endothelium-denuded)
Agonist serotonin (pD 2 = 6.5)
Antagonist ketanserin (pA 2 = 8.7)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Rinaldi-Carmona, M. et al. (1992) J. Pharmacol. Exp. Ther., 262: 759-768.
tension (% of max.)
-12 -11
100
50
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
0
-8 -7 -6 -5 -4 -3
log [agonist] (M)
ketanserin
none
3 nM
10 nM
30 nM
5-HT 2B - antagonist radioligand
Source
human recombinant (CHO cells)
Ligand
[ 3 H]mesulergine (2 nM)
Kd
2.4 nM
Non specific mesulergine (10 µM)
binding
Reference mesulergine (IC 50 : 2.35 nM)
Ref. 1609
Q 3 weeks
Kursar, J.D. et al. (1994) Mol. Pharmacol., 46: 227-234.
specific binding (% of control)
100
50
0
-11
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
mesulergine
SB 206553
SB 204741
ketanserin
selected cerep assays
❚ binding assays
-10 -9 -8 -7 -6 -5 -4 -3
-11
-10 -9 -8 -7 -6 -5 -4 -3
-12 -11 -10 -9 -8 -7 -6 -5 -4
Binding assays are developed according to the competition assay principle. There are three assay formats -13 -12 used: -11 -10filtration, -9 -8 -7 -6scintillation
-5
-10 -9 -8 -7 -6
proximity assay (SPA) and centrifugation. All formats utilize a radiolabeled ligand and a source of receptor (membranes, soluble/purified).
Large batches of cells, from which prepared membranes are frozen and stored, are produced in-house. Membrane preparations are
-10 -9 -8 -7 -6 -5 -4
quality controlled before use.
-12 -11 -10 -9 -8 -7 -6 -5 -4 -3
❚ cellular Functional GPCR assays
-12 -11 -10 -9 -8 -7 -6 -5
Functional GPCR assays are cell-based assays to measure agonist-like, inverse agonist, antagonist and modulator
-11 -10 -9
activity
-8 -7 -6of -5compounds.
-4
Various technologies are used: TR-FRET to determine cAMP concentration and IP1 levels, real time fluorescence to monitor calcium flux,
cellular dielectric spectroscopy to measure impedance modulation. Large batches of cells, from which whole cells are frozen and stored
for functional assays, are produced in-house. Cells are quality controlled before use. A novel patented host cell line was designed and
constructed for Gi protein coupled receptors.
❚ tissue bioassays
Tissue bioassays are functional assays designed to evaluate the agonist and antagonist activities of compounds at various receptors and
ion channels in whole tissues. The tissues used are isolated from contractile cardiac and smooth muscles of the cardiovascular, respiratory,
gastrointestinal and urogenital tracts of rodents, rabbit or human. The selected tissues are assayed in organ bath systems to record the
contractile activity in conditions as selective as possible to avoid any potential interaction with other receptors known to be present in the
tissue used.

71
serotonin ❚
5-HT 2B - agonist radioligand
binding
Ref. 1333
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 125 I](±)DOI (0.2 nM)
0.2 nM
(±)DOI (1 µM)
(±)DOI (IC 50 : 5 nM)
Choi, D.S. et al. (1994) FEBS Lett., 352: 393-399.
specific binding (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6
log [drug] (M)
(±)DOI
serotonin
5-methoxytryptamine
BW 723C86
Cerep
services
Receptors
[GPCRs]
5-HT 2B
cellul ar
Ref. 3344
Ref. 3345
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
human recombinant (CHO cells)
Measured product IP 1
Detection method HTRF
Agonist effect Control serotonin (1 µM)
Reference serotonin (EC 50 : 10.1 nM)
Antagonist effect Stimulant serotonin (30 nM)
Reference SB 206553 (IC 50 : 28.4 nM)
Porter, R.H.P. et al. (1999) Brit. J. Pharmacol., 128: 13-20.
-10 -9 -8 -7 -6 -5 -4 -3
-11 -10 -9 -8 -7 -6 -5 -4 -3
-12 -11 -10 -9 -8 -7 -6 -5 -4
-13 -12 -11 -10 -9 -8 -7 -6 -5
-6
-10 -9 -8 -7
-5 -4
-10 -9 -8 -7 -6
-6 -5 -4 -12 -11 -10 -9 -8 -7 -3
-11 -10 -9 -8 -7 -6 -5
-12
Ion
channels
Transporters
-11 -10 -9 -8 -7 -6 -5 -4
5-HT 2B
tissue
Ref. 0333
Q 4 weeks
Source
rat stomach fundus
Agonist 5-CT (pD 2 = 7.5)
Antagonist methiothepin (pA 2 = 8.4)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Baxter, G.S. et al. (1994) Brit. J. Pharmacol., 112: 323-331.
tension (% of max.)
100
50
methiothepin
none
0.1 µM
0
1 µM
10 µM
-9 -8 -7 -6 -5 -4
log [agonist] (M)
Kinases
Epigenetic &
DNA-related
enzymes
5-HT 2C - antagonist radioligand
Source
human recombinant (HEK-293 cells)
Ligand
[ 3 H]mesulergine (1 nM)
binding
Kd
0.5 nM
Ref. 0137
Non specific RS 102221 (10 µM)
Q 3 weeks
Reference RS 102221 (IC 50 : 3.1 nM)
Included in:
High-throughput profile
Stam, N.J. et al. (1994) Eur. J. Pharmacol., 269: 339-348.
specific binding (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5
log [drug] (M)
RS 102221
Ro 600175
serotonin
ketanserin
Other
enzymes
Specialized
cellular
assays
5-HT 2C - agonist radioligand
binding
Ref. 1003
Q 3 weeks
Included in:
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (HEK-293 cells)
[ 125 I](±)DOI (0.1 nM)
0.9 nM
(±)DOI (10 µM)
(±)DOI (IC 50 : 0.38 nM)
Bryant, H.U. et al. (1996) Life Sci., 15: 1259-1268.
specific binding (% of control)
100 -10 -9 -8 -7 -6 -5 -4 -3
-11 -10 -9 -8 -7 -6 -5 -4 -3
-12 -11 -10 -9 -8 -7 -6 -5 -4
50
-13 -12 -11 -10 -9 -8 -7 -6 -5
-9 -8 -7 -6
-10
(±)DOI
serotonin
RS 102221
-10 -9 -8 -7 -6 -5 -4
0
Ro 600175
-11 - 10 -9 -8 -7 -6
-11 -10 -8 -6 -5 -12 -9 -7 -4 -3
log [drug] (M)
-10 -9 -8 -7 -12 -11 -6 -5
-11 -10 -7 -6 -5 -4
-9 -8
Standard
profiles
Testing
conditions
5-HT 2C
cellul ar
Ref. 3197
Ref. 3199
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
human recombinant (HEK-293 cells)
Measured product IP 1
Detection method HTRF
Agonist effect Control serotonin (1 µM)
Reference serotonin (EC 50 : 1.81 nM)
Antagonist effect Stimulant serotonin (30 nM)
Reference SB 206553 (IC 50 : 20.2 nM)
Porter, R.H.P. et al. (1999) Brit. J. Pharmacol., 128: 13-20.
❚ For 5-HT 3 assays, see "OTHER RECEPTORS", page 90
Ordering
information
Assay list
& index

72 in vitro pharmacology 2011 catalog
❚ serotonin
5-HT 4e - antagonist radioligand
binding
Ref. 0501
Q 3 weeks
Included in:
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]GR 113808 (0.3 nM)
0.15 nM
serotonin (100 µM)
serotonin (IC 50 : 170 nM)
Mialet, J. et al. (2000) Brit. J. Pharmacol., 129: 771-781.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
serotonin
GR 113808
ketanserin
8-OH-DPAT
5-HT 4e
cellul ar
Ref. 1044
Ref. 1045
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control serotonin (1 µM)
Reference serotonin (EC 50 : 5.2 nM)
Antagonist effect Stimulant serotonin (30 nM)
Reference GR 113808 (IC 50 : 0.3 nM)
Mialet, J. et al. (2000) Brit. J. Pharmacol., 129: 771-781.
cAMP modulation (% of control)
100
100
50
50
0
0
-11 -10 -9 -8 -7 -6 -5 -4 -3 -12 -11 -10 -9 -8 -7 -6 -5 -4 -3
log [agonist] (M)
log [antagonist] (M)
serotonin
GR 113808
RS 67506
ketanserin
cisapride
5-CT
5-HT 4
tissue
Ref. 0336
Q 4 weeks
Source
guinea-pig colon
Agonist serotonin (pD 2 = 7.1)
Antagonist GR 113808 (pA 2 = 9.7)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Gale, J.D. et al. (1994) Brit. J. Pharmacol., 111: 332-338.
tension (% of max.)
-12 -11
-12 -11
-11 -10 -9 -8 -7 -6 -5 -4
-12 -11 -10 -9 -8 -7
100
-11 -10 -9 -8 -7 -6 -5 -4
-10 -9 -8 -7
50 -10 -9 -8 -7 -6 -5
-10 -9 -8 -7 -6 -5 -4
GR 113808
none
1 nM
3 nM
0
10 nM
-9 -8 -7 -6 -5 -4
log [agonist] (M)
5-HT 5a - agonist radioligand
binding
Ref. 0140
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (HEK-293 cells)
[ 3 H]LSD (1.5 nM)
1.5 nM
serotonin (100 µM)
serotonin (IC 50 : 120 nM)
Rees, S. et al. (1994) FEBS Lett., 355: 242-246.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4 -3
log [drug] (M)
serotonin
methiothepin
8-OH-DPAT
ketanserin
5-HT 6 - agonist radioligand
binding
Ref. 0142
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]LSD (2 nM)
1.8 nM
serotonin (100 µM)
serotonin (IC 50 : 150 nM)
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
Monsma, F.J. et al. (1993) Mol. Pharmacol., 43: 320-327.
[custom offer] rat cDNA model (Ref. 0141), please contact us at customresearch@cerep.com
serotonin
methiothepin
MDL 72222
8-OH-DPAT
5-HT 6
cellul ar
Ref. 1627
Ref. 1628
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control serotonin (10 µM)
Reference serotonin (EC 50 : 20 nM)
Antagonist effect Stimulant serotonin (100 nM)
Reference methiothepin (IC 50 : 65 nM)
Kohen, R. et al. (1996) J. Neurochem., 66: 47-56.
cAMP modulation (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4
log [agonist] (M)
serotonin
5-methoxytryptamine
5-CT
100
50
0
-10 -9 -8 -7 -6 -5
log [antagonist] (M)
methiothepin
SB 285585
Ro 046790
-11 -10
-9 -8 -7 -6 -5 -4
-12 -11
-10 -9 -8 -7

73
5-HT 7 - agonist radioligand
binding
Ref. 0144
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]LSD (4 nM)
2.3 nM
serotonin (10 µM)
serotonin (IC 50 : 0.45 nM)
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4
serotonin ❚
log [drug] (M)
Shen, Y. et al. (1993) J. Biol. Chem., 268: 18200-18204.
[custom offer] rat cDNA model (Ref. 0143), please contact us at customresearch@cerep.com
serotonin
8-OH-DPAT
ketanserin
MDL 72222
Cerep
services
Receptors
[GPCRs]
5-HT 7
cellul ar
Ref. 1661
Ref. 1662
Q 3 weeks
Included in:
Agonist effect
Antagonist effect
Cellular functional GPCR profile
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control serotonin (10 µM)
Reference serotonin (EC 50 : 25 nM)
Antagonist effect Stimulant serotonin (300 nM)
Reference mesulergine (IC 50 : 25 nM)
Adham, N. et al. (1998) J. Pharmacol. Exp. Ther., 287: 508-514.
❚ See other Serotonin assays pp. 91, 101 and 105
❚ For sigma assays, see "Other receptors",
page 91
Ion
channels
Transporters
❚ somatostatin
Kinases
sst (non-selective) - agonist radioligand
binding
Ref. 0149
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Source
Ligand
Kd
Non specific
Reference
AtT-20 cells
[ 125 I]Tyr 11 -somatostatin-14 (0.05 nM)
0.08 nM
somatostatin-14 (300 nM)
somatostatin-14 (IC 50 : 0.2 nM)
Brown, P.J. et al. (1990) J. Biol. Chem., 265: 17995-18004.
specific binding (% of control)
100
50
0
-12 -11 -10 -9 -8 -7
log [drug] (M)
somatostatin-14
[D-Trp 8 ]-
somatostatin
somatostatin-28
BIM 23056
Epigenetic &
DNA-related
enzymes
Other
enzymes
sst 1 - agonist radioligand
binding
Ref. 1940
Q 3 weeks
Included in:
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 125 I]Tyr 11 -somatostatin-14 (0.1 nM)
1nM
somatostatin-28 (1 µM)
somatostatin-28 (IC 50 : 0.5 nM)
Patel, C.Y. and Srikant, C.B. (1994) Endocrinology, 135: 2814-2817.
Specialized
cellular
assays
Standard
profiles
sst 1
cellul ar
Ref. 2253
Ref. 2254
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control somatostatin-28 (100 nM)
Reference somatostatin-28 (EC 50 : 0.37 nM)
Antagonist effect Stimulant somatostatin-28 (3 nM)
Reference unavailable
Patel, Y.C. and Srikant, C.B. (1994) Endocrinology, 135: 2814-2817.
[Solvent] must be kept 0.3%
Testing
conditions
Ordering
information
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Assay developed in 2010 New assay conditions Human Q Standard turnaround time
Assay list
& index

74 in vitro pharmacology 2011 catalog
❚ somatostatin
sst 2 - agonist radioligand
binding
Ref. 2339
Q 6 weeks
Source
Ligand
Kd
Non specific
Reference
IMR32 cells (endogenous)
[ 125 I]Tyr 11 -somatostatin-14 (0.04 nM)
0.2 nM
seglitide (1 µM)
seglitide (IC 50 : 0.2 nM)
O’Dorisio, M.S. et al. (1994) Cell Growth Differ., 5: 1-8.
specific binding (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5
log [drug] (M)
seglitide
somatostatin-14
CYN 154806
BIM 23027
sst 4 - agonist radioligand
binding
Ref. 0482
Q 3 weeks
Included in:
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 125 I]Tyr 11 -somatostatin-14 (0.1 nM)
5.9 nM
somatostatin-14 (1 µM)
somatostatin-14 (IC 50 : 1.4 nM)
Rohrer, L. et al. (1993) Proc. Natl. Acad. Sci. USA, 90: 4196-4200.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5
log [drug] (M)
▲ somatostatin-14
● [D-Trp 8 ]-
somatostatin
■ somatostatin-28
▼ BIM 23056
sst 4
cellul ar
Ref. 2095
Ref. 2103
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control somatostatin-14 (100 nM)
Reference somatostatin-14 (EC 50 : 0.21 nM)
Antagonist effect Stimulant somatostatin-14 (3 nM)
Reference unavailable
Engström, M. et al. (2005) J. Pharm. Exp. Ther., 312: 332-338.
[Solvent] must be kept 0.3%
sst 5 - agonist radioligand
Source
human recombinant (CHO cells)
Ligand
[ 125 I]Tyr 11 -somatostatin-14 (0.1 nM)
binding
Kd
0.2 nM
Ref. 0626
Non specific somatostatin-14 (1 µM)
Q 3 weeks
Reference somatostatin-14 (IC 50 : 0.76 nM)
Included in:
Organ safety profile
Yamada, Y. et al. (1993) Biochem. Biophys. Res. Commun., 195: 844-852.
specific binding (% of control)
100
50
0
log [drug] (M)
-13 - 12 -11 - 10 -9 -8 -7 -6
somatostatin-14
[D-Trp 8 ]-
somatostatin
somatostatin-28
BIM 23056
sst 5
cellul ar
Ref. 2087
Ref. 2088
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control somatostatin-14 (300 nM)
Reference somatostatin-14 (EC 50 : 6.1 nM)
Antagonist effect Stimulant somatostatin-14 (100 nM)
Reference unavailable
Carruthers, A.M. et al. (1999) Brit. J. Pharmacol., 126: 1221-1229.
[Solvent] must be kept 0.3%
For some binding assays two models are available using either agonist or antagonist as radioligand.
❚ For radioligand binding assays, how should I choose between the agonist and the antagonist models when both are
available?
G-protein-coupled receptors have both high-affinity and low-affinity states that are bound differently by agonists and antagonists. Whereas
the antagonists bind with an equal affinity to both affinity states, agonists bind poorly to the low affinity state of the receptor. Therefore,
it is advisable to use an antagonist radioligand to evaluate the binding of antagonists knowing that this may fail to reveal the binding
of agonists. On the other hand, an assay using an agonist radioligand is suitable to evaluate both agonists and antagonists.
The testing of a compound in both assays and the comparison of its competition curves against each radioligand may provide information
about its functional activity at the receptor.

75
❚ thyrotropin releasing hormone
TRH 1 - agonist radioligand
binding
Ref. 1616
Q 3 weeks
Included in:
Diversity profile
Organ safety profile
TRH 1
cellul ar
Ref. 1617
Ref. 2057
Q 3 weeks
Agonist effect
Antagonist effect
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]Me-TRH (2 nM)
3.9 nM
TRH (10 µM)
TRH (IC 50 : 39 nM)
Hinuma, S. et al. (1994) Biochem. Biophys. Acta., 1219: 251-259.
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control TRH (100 nM)
Reference TRH (EC 50 : 0.16 nM)
Antagonist effect Stimulant TRH (1 nM)
Reference unavailable
Yamada, M. et al. (1993) Biochem. Biophys. Res. Com., 195: 737-745.
specific binding (% of control)
Ca 2+ mobilization (% of control)
100
50
0
100
50
0
-11 -10 -9 -8 -7 -6 -5
-12 -11
log [drug] (M)
log [agonist] (M)
TRH
Me-TRH
-10 -9 -8 -7
[Solvent] must be kept ≤ 0.1%
TRH
Me-TRH
antagonist effect:
no graph available
Cerep
services
Receptors
[GPCRs]
Ion
channels
Transporters
❚ urotensin-ii
UT - agonist radioligand
binding
Ref. 1386
Q 3 weeks
Included in:
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 125 I]urotensin-II (0.1 nM)
0.29 nM
urotensin-II (3 µM)
urotensin-II (IC 50 : 0.98 nM)
Maguire, J.J. et al. (2000) Brit. J. Pharmacol. 131: 441-446.
-12 -11
-12 -11
specific binding (% of control)
-11 -10
100
-12 -11
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7
-10 -9 -8 -7
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
50
0
-11 -10
log [drug] (M)
-9 -8 -7 -6 -5 -4
-12 -11 -10 -9 -8 -7 -6
urotensin-II
Kinases
Epigenetic &
DNA-related
enzymes
Other
enzymes
UT
cellul ar
Ref. 1376
Ref. 1836
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control human urotensin-II (100 nM)
Reference human urotensin-II (EC 50 : 2 nM)
Antagonist effect Stimulant human urotensin-II (10 nM)
Reference unavailable
Herold, C.L. et al. (2003) Brit. J. Pharmacol., 139: 203-207.
Ca 2+ mobilization (% of control)
100
50
0
-12 -11
-10 -9 -8 -7
log [agonist] (M)
human urotensin-II
[Orn 8 ]-urotensin-II
rat urotensin-II
[Solvent] must be kept ≤ 0.1%
antagonist effect:
no graph available
Specialized
cellular
assays
Standard
profiles
❚ vasoactive intestinal peptide
PAC 1 (PACAP) - agonist radioligand
binding
Ref. 1518
Q 3 weeks
Included in:
High-throughput profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 125 I]PACAP 1-27 (0.015 nM)
0.092 nM
PACAP 1-27 (100 nM)
PACAP 1-38 (IC 50 : 0.13 nM)
Ohtaki, T. et al. (1998) J. Biol. Chem., 273: 15464-15473.
-12 -11
-12 -11
specific binding (% of control)
-11 -10
100
-12 -11
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7
-10 -9 -8 -7
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
50
0
-11 -10
log [drug] (M)
-9 -8 -7 -6 -5 -4
-12 -11 -10 -9 -8 -7 -6 -5
PACAP1-38
PACAP1-27
VIP
Testing
conditions
Ordering
information
Assay list
& index

76 in vitro pharmacology 2011 catalog
❚ vasoactive intestinal peptide
PAC 1 (PACAP)
cellul ar
Ref. 1843
Ref. 1844
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control PACAP 1-38 (1 nM)
Reference PACAP 1-38 (EC 50 : 0.022 nM)
Antagonist effect Stimulant PACAP 1-38 (0.1 nM)
Reference PACAP 6-38 (IC 50 : 57 nM)
Ohtaki, T. et al. (1998) J. Biol. Chem., 273: 15464-15473.
cAMP modulation (% of control)
100
100
50
50
0
0
-13 -12 -11 -10 -9 -8 -7 -6 -5 -10 -9 -8 -7 -6 -5
log [agonist] (M)
log [antagonist] (M)
PACAP 1-38
PACAP
PACAP 1-27
PACAP
VIP
[Solvent] must be kept ≤ 0.3%
6-38
6-27
VPAC 1 (VIP 1 ) - agonist radioligand
binding
Ref. 0157
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 125 I]VIP (0.04 nM)
0.05 nM
VIP (1 µM)
VIP (IC 50 : 0.11 nM)
Couvineau, A. et al. (1985) Biochem. J., 231: 139-143.
specific binding (% of control)
-12 -11
-11 -10
-12 -11
100
-12 -11
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7
-10 -9 -8 -7
50
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
0
-11 -10
-9 -8 -7 -6 -5 -4
-13 -12 -11 -10 -9 -8 -7 -6
log [drug] (M)
-12 -11 -10 -9 -8 -7 -6 -5 -4
-12 -11 -10 -9 -8 -7 -6 -5 -4
VIP
PACAP1-27
helodermin
VPAC 1 (VIP 1 )
cellul ar
Ref. 0486 Agonist effect
Ref. 0515 Antagonist effect
Q 3 weeks
Source
HT-29 cells (endogenous)
Measured product cAMP
Detection method HTRF
Agonist effect Control VIP (100 nM)
Reference VIP (EC 50 : 0.5 nM)
Antagonist effect Stimulant VIP (3 nM)
Reference VIP GRF 8-27 (IC 50 : 15 nM)
Summers, M.A. et al. (2003) J. Pharmacol. Exp. Ther., 306: 638-645.
cAMP modulation (% of control)
100
100
50
50
0
0
-12 -11 -10 -9 -8 -7 -6 -5 -10 -9 -8 -7 -6
log [agonist] (M)
log [antagonist] (M)
VIP
VIP GRF
PACAP 1-27
VIP6-28
PACAP 1-38
secretin
[Solvent] must be kept ≤ 0.3%
8-27
VPAC 2 (VIP 2 ) - agonist radioligand
Source
human recombinant (CHO cells)
Ligand
[ 125 I]VIP (0.05 nM)
Kd
0.56 nM
Non specific VIP (1 µM)
binding
Reference VIP (IC 50 : 0.34 nM)
Ref. 0487
Q 3 weeks
Gourlet, P. et al. (1997) Peptides, 18: 403-408.
specific binding (% of control)
-12 -11
-12 -11
-11 -10
-12 -11
100
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7
-10 -9 -8 -7
50 -10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
0
-11 -10
-9 -8 -7 -6 -5 -4
-13 -12 -11 -10 -9 -8 -7 -6
log [drug] (M)
-12 -11 -10 -9 -8 -7 -6 -5 -4
-11 -10 -9 -8 -7 -6 -5
VIP
PACAP1-27
helodermin
VPAC 2 (VIP 2 )
cellul ar
Ref. 0513 Agonist effect
Ref. 0516 Antagonist effect
Q 3 weeks
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control VIP (100 nM)
Reference VIP (EC 50 : 1 nM)
Antagonist effect Stimulant VIP (10 nM)
Reference VIP 6-28 (IC 50 : 3.3 µM)
Gourlet, P. et al. (1997) Peptides, 18: 403-408.
cAMP modulation (% of control)
100
50
0
-10 -9 -8 -7 -6 -8 -7 -6 -5
-12 -11 -4
log [agonist] (M)
VIP
helodermin
PACAP1-27
100
[Solvent] must be kept ≤ 0.3%
50
0
log [antagonist] (M)
VIP6-28
(Ac-His 1 ,D-Phe 2 ,-Lys 15 ,
Arg 16 ,Leu 27 )-VIP 1-7-GRF8-27
[Lys 1 ,Pro 2,5 ,Arg 3,4 ,-Tyr 6 ]-VIP
VPAC 2 (VIP 2 )
tissue
Ref. 0622
Q 4 weeks
Source
guinea-pig trachea
(precontracted with 3 µM histamine)
Agonist VIP (porcine) (pD 2 = 8.8)
Antagonist not available
Test concentrations 3 concentrations, n=2 (2 tissues) f
or both activities
[Solvent] must be kept ≤ 0.1%
Undem, B. J. et al. (1996) J. Pharmacol. Exp. Ther., 278: 964-970.
tension (% of control)
-12 -11
-12 -11
-11 -10
-12 -11
100
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7
-10 -9 -8 -7
50 -10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
0
-11 -10
-9 -8 -7 -6 -5 -4
-13 -12 -11 -10 -9 -8 -7 -6
log [agonist] (M)
-12 -11 -10 -9 -8 -7 -6 -5 -4
-11 -10 -9 -8 -7 -6

77
❚ vasopressin
Cerep
services
OT
cellul ar
Ref. 2196
Ref. 2197
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (ECV304 cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control oxytocin (10 µM)
Reference oxytocin (EC 50 : 27 nM)
Antagonist effect Stimulant oxytocin (100 nM)
Reference L 371,257 (IC 50 : 79 nM)
Tahara, A. et al. (2000) Brit. J. Pharmacol., 129: 131-139.
Ca 2+ mobilization (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5 -11 -10 -9 -8 -7 -6 -5 -4
log [agonist] (M)
log [antagonist] (M)
oxytocin
L 371,257
[Thr 4 ,Gly 7 ]-oxytocin
atosiban
AVP
SR 49059
dDAVP
[adamantaneacetyl 1 ,O-Et-D
-Tyr 2 ,-Val 4 ,aminobutyryl 6 ]-AVP
[Solvent] must be kept ≤ 0.1%
100
50
0
Receptors
[GPCRs]
Ion
channels
OT
tissue
Ref. 0331
Q 4 weeks
Source
rat uterus
Agonist oxytocin (pD 2 = 8.2)
Antagonist L-368,899
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Pettibone, D.J. et al. (1991) J. Pharmacol. Exp. Ther., 256: 304-308.
tension (% of max.)
-12 -11
-11 -10
100-12 -11
-12 -11
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7
-10 -9 -8 -7
50
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
0
-11 -10
-9 -8 -7 -6 -5 -4
-13 -12 -11 -10 -9 -8 -7 -6
-10 -9 -8 -7 -6
log [agonist] (M)
-12 -11 -10 -9 -8 -7 -6 -5 -4
Transporters
Kinases
V 1a - agonist radioligand
binding
Ref. 0159
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]AVP (0.3 nM)
0.5 nM
AVP (1 µM)
[d(CH 2 ) 5
1,Tyr(Me) 2 ]-AVP (IC 50 : 0.89 nM)
Tahara, A. et al. (1998) Brit. J. Pharmacol., 125: 1463-1470.
[custom offer] rat A7r5 cells model (Ref. 0158), please contact us at customresearch@cerep.com
Epigenetic &
DNA-related
enzymes
Other
enzymes
V 1a
cellul ar
Ref. 1033
Ref. 1034
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control AVP (1 µM)
Reference AVP (EC 50 : 0.7 nM)
Antagonist effect Stimulant AVP (10 nM)
Reference [d(CH 2 ) 5
1,Tyr(Me) 2 ]-AVP
(IC 50 : 30 nM)
Tahara, A. et al. (1998) Brit. J. Pharmacol., 125: 1463-1470.
[Solvent] must be kept 0.1%
Specialized
cellular
assays
Standard
profiles
V 1a
tissue
Ref. 0338
Q 4 weeks
Source
rat caudal artery (endothelium-denuded)
Agonist AVP (pD 2 = 9)
Antagonist [d(CH 2 ) 5
1,Tyr(Me) 2 ]-AVP (pA 2 = 10.2)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Clineschmidt, B.V. and Lis, E.V. (1986) Arch. Int. Pharmacodyn., 284: 72-84.
tension (% of max.)
100
50
[d(CH 2) 5
1,Tyr(Me) 2]
-AVP
none
0.3 nM
1 nM
0
3 nM
-10 -9 -8 -7 -6 -5
log [agonist] (M)
Testing
conditions
Ordering
information
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Assay developed in 2010 New assay conditions Human Q Standard turnaround time
Assay list
& index

78 in vitro pharmacology 2011 catalog
❚ vasopressin
V 1b - agonist radioligand
binding
Ref. 0588
Q 3 weeks
Included in:
Organ safety profile
V 2 - agonist radioligand
binding
Ref. 0497
Q 3 weeks
Included in:
Diversity profile
BioPrint ® profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]AVP (0.1 nM)
0.1 nM
AVP (0.1 µM)
AVP (IC 50 : 0.33 nM)
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5
log [drug] (M)
Tahara, A. et al. (1998) Brit. J. Pharmacol., 125: 1463-1470.
[custom offer] rat cDNA model (Ref. 0466), please contact us at customresearch@cerep.com
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]AVP (0.3 nM)
0.76 nM
AVP (1 µM)
AVP (IC 50 : 0.954 nM)
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
AVP
[d(CH 2
) 51
,Tyr(Me) 2
]
-AVP
oxytocin
SR 49059
AVP
[d(CH 2 ) 51 ,Tyr(Me) 2 ]
-AVP
SR 121463B
oxytocin
Tahara, A. et al. (1998) Brit. J. Pharmacol., 125: 1463-1470.
[custom offer] porcine LLC-PK1 cells model (Ref. 0160), please contact us at customresearch@cerep.com
V 2
cellul ar
Ref. 0237
Ref. 0569
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product cAMP
Detection method HTRF
Agonist effect Control AVP (1 nM)
Reference AVP (EC 50 : 0.013 nM)
Antagonist effect Stimulant AVP (0.03 nM)
Reference [adamantaneacetyl 1 ,O-Et-D-
Tyr 2 ,Val 4 ,aminobutyryl 6 ]-AVP
(IC 50 : 30 nM)
Cotte, N. et al. (1998) J. Biol. Chem., 273: 29462-29468.
cAMP modulation (% of control)
100
100
50
50
0
0
-13 -12 -11 -10 -9 -8 -7 -6 -10 -9 -8 -7 -6 -5
log [agonist] (M)
log [antagonist] (M)
AVP
[adamantaneacetyl 1 ,O-Et-D
Val 4 -dDAVP
-Tyr 2 ,-Val 4 ,aminobutyryl 6 ]-AVP
dDAVP
SR 121463B
oxytocin
[d(CH 2 ) 51 ,Tyr(Me) 2 ]-AVP
[Solvent] must be kept ≤ 0.3%
-11 -10
-9 -8 -7 -6 -5 -4
-12 -11
-10 -9 -8 -7
-11 -10 -9 -8 -7 -6 -5 -4
-13 -12 -11 -10 -9 -8 -7 -6
-12 -11
-10 -9 -8 -7
-12 -11
-10 -9 -8 -7 -6 -5
-12 -11 -10 -9 -8 -7 -6 -5 -4
-9 -8 -7 -6 -5
-10 -4
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Assay developed in 2010 New assay conditions Human Q Standard turnaround time

79
Cerep
services
receptors
Receptors
[Nuclear
receptors]
[Nuclear receptors]
Ion
channels
❚ Steroid nuclear receptors
AR - agonist radioligand
binding
Ref. 0933
Q 3 weeks
Included in:
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
ER (non-selective) - agonist radioligand
binding
Ref. 0152
Q 3 weeks
Included in:
Diversity profile
LNCaP cells (cytosol)
[ 3 H]methyltrienolone (1 nM)
0.8 nM
mibolerone (1 µM)
mibolerone (IC 50 : 2.6 nM)
Zava, D.T. et al. (1979) Endocrinology, 104: 1007-1012.
[Custom offer] rat prostate model (Ref. 0155), please contact us at customresearch@cerep.com
Source
Ligand
Kd
Non specific
Reference
MCF-7 cells (cytosol)
[ 3 H]estradiol (0.4 nM)
0.2 nM
17-β-estradiol (6 µM)
17-β-estradiol (IC 50 : 0.35 nM)
Kurata, Y. et al. (2005) J. Pharmacol. Exp. Ther., 313: 916-920.
specific binding (% of control)
100
50
0
-12 -11 -10 -7 -6 -4 -3
-9 -8 -5
log [drug] (M)
β
17-β-estradiol
mibolerone
testosterone
progesterone
Transporters
Kinases
Epigenetic &
DNA-related
enzymes
Other
enzymes
Specialized
cellular
assays
ERα - agonist fluoligand
binding
Ref. 0484
Q 3 weeks
Included in:
BioPrint ® profile
Organ safety profile
fluorimetry
Source
Ligand
Kd
Non specific
human recombinant (Sf9 cells)
fluormone TM ES2 (1 nM)
4 nM
17-β-estradiol (10 µM)
Reference 17-β-estradiol (IC 50 : 18 nM)
Parker, G.J. et al. (2000) J. Biomol. Screen., 5: 77-88.
specific binding (% of control)
100
50
0
-10 -9 -8 -7 -6 -5 -4 -3
-11 -10 -9 -8 -7 -6 -5 -4 -3
-12 -11 -10 -9 -8 -7 -6 -5 -4
-13 -12 -11 -10 -9 -8 -7 -6 -5
-9 -8 -7 -6
-10
-10 -7 -9 -8 -6 -5 -4
17-β-estradiol
DES
-12 -10 -9 -7 -6 -4 -3
-11 -8 -5
-9 -8 -6 -5
-10 -7
log -10[drug] -9 (M) -8 -12 -11 -7 -6 -5
-11 -10 -7 -6 -5 -4
-9 -8
Standard
profiles
Testing
conditions
ERb - agonist fluoligand
fluorimetry
Source
human recombinant (Hi5 cells)
Ligand
fluormone TM ES2 (1 nM)
Kd
4 nM
binding
Non specific 17-β-estradiol (10 µM)
Ref. 0485
Reference 17-β-estradiol (IC 50 : 13 nM)
Q 4 weeks
Parker, G.J. et al. (2000) J. Biomol. Screen., 5: 77-88.
specific binding (% of control)
100
50
17-β-estradiol
0
DES
-10 -9 -8 -7 -6 -5
log [drug] (M)
Ordering
information
Assay list
& index

80 in vitro pharmacology 2011 catalog
❚ steroid nuclear receptors
GR - agonist radioligand
binding
Ref. 0469
Q 3 weeks
Included in:
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
IM-9 cells (cytosol)
[ 3 H]dexamethasone (1.5 nM)
1.5 nM
triamcinolone (10 µM)
dexamethasone (IC 50 : 4.3 nM)
Clark, A.F. et al. (1996) Invest. Ophtalmol. Vis. Sci., 37: 805-813.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5
log [drug] (M)
dexamethasone
triamcinolone
progesterone
17-β-estradiol
PR - agonist radioligand
binding
Ref. 2341
Q 3 weeks
Included in:
Diversity profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
T47D cells (cytosol)
[ 3 H]progesterone (0.5 nM)
2 nM
promegestone (1 µM)
promegestone (IC 50 : 1.68 nM)
Sarup, J.C. et al. (1988) J. Biol. Chem., 263: 5624-5633
β
PR
Ref. 2855
Ref. 2860
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant
Measured product coactivator recruitment
Detection method AlphaScreen
Agonist effect Control progesterone (10 µM)
Reference progesterone (EC 50 : 14 nM)
Antagonist effect Stimulant progesterone (100 nM)
Reference mifepristone (IC 50 : 13 nM)
Onate, S.A. et al. (1998) J. Biol. Chem., 273: 12101-12108.
β
❚ Non-steroid nuclear receptors
CAR
Ref. 3141
Ref. 3145
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant
Measured product coactivator recruitment
Detection method AlphaScreen
Agonist effect Control CITCO (100 µM)
Reference CITCO (EC 50 : 605 nM)
Antagonist effect Stimulant CITCO (3 µM)
Reference PK11195 (IC 50 : 4900 nM)
Li, L., (2008) Mol. Pharmacol., 74: 443-453.
CAR - inverse agonist effect
Ref. 3354
Q 3 weeks
Source
human recombinant
Measured product coactivator recruitment
Detection method AlphaScreen
Control
Reference
PK11195 (100 µM)
PK11195 (EC 50 : 450 nM)
Li, L., (2008) Mol. Pharmacol., 74: 443-453.
selected cerep assays
❚ Functional nuclear receptor assays
In addition to our large selection of nuclear receptor binding assays, Cerep has developed functional assays for the determination of
agonist and antagonist effects of compounds. These assays are coactivator recruitment assays measuring biochemical interaction between
the receptor ligand binding domain and a specific coactivator. The recombinant protein for these assays are produced in-house using
adapted systems (E.coli or baculovirus). Each batch is quality controlled before use.

81
LXRb - agonist radioligand
binding
Ref. 2047
Q 3 weeks
Included in:
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (BL21/DE3 cells)
[ 3 H]hydroxycholesterol (25 nM)
55 nM
22(R)-hydroxycholesterol (30 µM)
22(R)-hydroxycholesterol (IC 50 : 2.2 µM)
Janowski, B.A. et al. (1999) Proc. Natl. Acad. Sci. USA, 96: 266-271.
non-steroid nuclear receptors ❚
specific binding (% of control)
100
50
0
-9 -8 -7 -6 -5 -4
log [drug] (M)
hydroxycholesterol
paxilline
LXRα-β agonist
Cerep
services
Receptors
[Nuclear
receptors]
PPARa - agonist radioligand
Source
human recombinant (E. coli)
binding
Ligand
[ 3 H]WY 14643 (200 nM)
Kd
4000 nM
Ref. 0640
Non specific GW 7647 (10 µM)
Q 3 weeks
Reference GW 7647 (IC 50 : 52 nM)
Included in:
Organ safety profile
Seethala, R. et al. (2006) Anal. Biochem., 363: 263-274.
Ion
channels
Transporters
PPARa
Ref. 2811
Ref. 2813
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant
Measured product coactivator recruitment
Detection method AlphaScreen
Agonist effect Control GW 7647 (1 µM)
Reference GW 7647 (EC 50 : 4 nM)
Antagonist effect Stimulant GW 7647 (100 nM)
Reference GW 9662 (IC 50 : 2.8 µM)
Duncan, J.G. et al. (2007) Circulation, 115: 909-917.
Kinases
Epigenetic &
DNA-related
enzymes
PPARg - agonist radioligand
binding
Ref. 0641
Q 3 weeks
Included in:
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (E. coli)
[ 3 H]rosiglitazone (5 nM)
5.7 nM
rosiglitazone (10 µM)
rosiglitazone (IC 50 : 11 nM)
Ferry, G. et al. (2001) Eur. J. Pharmacol., 417: 77-89.
specific binding (% of control)
100
50
rosiglitazone
ciglitazone
T0070907
15-Deoxy-∆- 12-14 -
0
Prostaglandine J2
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
Other
enzymes
Specialized
cellular
assays
PPARg
Ref. 2771
Ref. 2772
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant
Measured product coactivator recruitment
Detection method AlphaScreen
Agonist effect Control rosiglitazone (10 µM)
Reference rosiglitazone (EC 50 : 333 nM)
Antagonist effect Stimulant rosiglitazone (1 µM)
Reference GW 9662 (IC 50 : 63 nM)
Yang, W. et al. (2000) Mol. Cell. Biol., 20: 8008-8017.
Standard
profiles
Testing
conditions
PPARd
Ref. 3082
Ref. 3083
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant
Measured product coactivator recruitment
Detection method AlphaScreen
Agonist effect Control GW 0742 (100 nM)
Reference GW 0742 (EC 50 : 1.8 nM)
Antagonist effect Stimulant GW 0742 (10 nM)
Reference GSK 0660 (IC 50 : 61.3 µM)
Rieck, M. et al. (2008) Mol. Pharmacol., 74: 1269-1277.
Ordering
information
Assay list
& index

82 in vitro pharmacology 2011 catalog
❚ NON-steroid nuclear receptors
PXR - agonist radioligand
Source
human recombinant (insect cells)
Ligand
[ 3 H]SR 12813 (35 nM)
Kd
35 nM
Non specific SR 12813 (30 µM)
binding
Ref. 2538
Reference T0901317 (IC 50 : 80 nM)
Q 3 weeks
Zhu, Z. et al.(2004) J. Biomol. Screen., 9: 533-540.
RARa - agonist radioligand
Source
human recombinant (insect cells)
Ligand
[ 3 H]9-cis retinoid acid (1 nM)
Kd
1 nM
Non specific all-trans retinoid acid (1 µM)
binding
Ref. 2084
Reference all-trans retinoid acid (IC 50 : 6.5 nM)
Q 3 weeks
Boehm, F.M. et al. (1994) J. Med. Chem., 37: 408-414.
specific binding (% of control)
100
50
all-trans-retinoic
acid
TTNPB
LE 135
9-cis-retinoic
0
acid
-11 -10 -7 -6 -5 -4
-9 -8
log [drug] (M)
TR (TH) - agonist radioligand
binding
Ref. 0156
Q 3 weeks
Included in:
BioPrint ® profile
Source
Ligand
Kd
Non specific
Reference
rat liver
[ 125 I]T 3 (0.1 nM)
0.24 nM
T 3 (1 µM)
T 3 (IC 50 : 0.44 nM)
Inoue, A. et al. (1983) Anal. Biochem., 134: 176-183.
specific binding (% of control)
100-10 -9 -8 -7 -6 -5 -4 -3
-12 -11 -10 -9 -8 -7 -6 -5 -4
50
-10 -9 -8 -7 -6
0 -10 -9 -8 -7 -6 -5 -4
-12 -11 -10 -7
-9 -8
log [drug] (M)
-9 -8 -7 -12 -11 -10 -6 -5
T 3
VDR - agonist radioligand
Source
human recombinant (Sf9 cells)
Ligand
[ 3 H]1α,25-(OH) 2 D 3 (0.3 nM)
Kd
1.7 nM
Non specific 1α,25-(OH) 2 D 3 (100 nM)
binding
Ref. 0499
Reference 1α,25-(OH) 2 D 3 (IC 50 : 3.4 nM)
Q 4 weeks
Ross, T. K. et al. (1991) Proc. Natl. Acad. Sci. USA, 88: 6555-6559.
specific binding (% of control)
100
50
0
-10 -9 -8 -7 -6 -5
log [drug] (M)
1α,25-(OH)2D3
1α-(OH)D3
25-(OH)D3
❚ For radioligand binding assays, how should I choose between the agonist and the antagonist models when both are
available?
For some binding assays two models are available using either agonist or antagonist as radioligand.
G-protein-coupled receptors have both high-affinity and low-affinity states that are bound differently by agonists and antagonists. Whereas
the antagonists bind with an equal affinity to both affinity states, agonists bind poorly to the low affinity state of the receptor. Therefore,
it is advisable to use an antagonist radioligand to evaluate the binding of antagonists knowing that this may fail to reveal the binding
of agonists. On the other hand, an assay using an agonist radioligand is suitable to evaluate both agonists and antagonists.
The testing of a compound in both assays and the comparison of its competition curves against each radioligand may provide information
about its functional activity at the receptor.

83
Cerep
services
receptors
Receptors
[Other
receptors]
[Other receptors]
Ion
channels
❚ ATRIAL NATRIURETIC PEPTIDE
Transporters
ANP - agonist radioligand
Source
guinea-pig cerebellum
Ligand
[ 125 I]ANP (0.05 nM)
Kd
0.14 nM
Non specific ANP (0.1 µM)
binding
Reference ANP (IC 50 : 0.085 nM)
Ref. 0027
Q 6 weeks
Quirion, R. et al. (1986) Proc. Natl. Acad. Sci. USA, 83: 174-178.
specific binding (% of control)
100
50
0
-12 -11 -10 -9 -8 -7
log [drug] (M)
ANP
Kinases
Epigenetic &
DNA-related
enzymes
❚ Benzodiazepine
Other
enzymes
BZD (peripheral) - antagonist radioligand
Source
rat heart
Ligand
[ 3 H]PK 11195 (0.2 nM)
binding
Kd
1.8 nM
Non specific PK 11195 (10 µM)
Ref. 0029
Q 3 weeks
Reference PK 11195 (IC 50 : 0.98 nM)
Included in:
High-throughput profile
Le Fur, G. et al. (1983) Life Sci., 33: 449-457.
Specialized
cellular
assays
Standard
profiles
❚ Cytokines
Testing
conditions
TNF-a - agonist radioligand
binding
Ref. 0076
Q 3 weeks
Included in:
High-throughput profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
U-937 cells
[ 125 I]TNF-a (0.1 nM)
0.05 nM
TNF-a (10 nM)
TNF-a (IC 50 : 0.1 nM)
Brockhaus, M. et al. (1990) Proc. Natl. Acad. Sci. USA, 87: 3127-3131.
α
β
Ordering
information
Assay list
& index

84 in vitro pharmacology 2011 catalog
❚ cytokines
IL-1b - agonist radioligand
binding
Ref. 0073
[Custom offer]
Please contact us at:
customresearch@cerep.com
Source
Ligand
Kd
Non specific
Reference
Balb/c 3T3 cells
[ 125 I]IL-1β (0.1 nM)
0.49 nM
IL-1β (10 nM)
IL-1β (IC 50 : 0.06 nM)
Bird, T.A. et al. (1987) FEBS Lett., 225: 21-26.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7
log [drug] (M)
IL-1β
IL-1α
TNF-α
IL-2 - agonist radioligand
binding
Ref. 0353
[Custom offer]
Please contact us at:
customresearch@cerep.com
Source
Ligand
Kd
Non specific
Reference
CTLL-2 cells
[ 125 I]IL-2 (0.02 nM)
0.02 nM
IL-2 (50 nM)
IL-2 (IC 50 : 0.06 nM)
Robb, R.J. et al. (1984) J. Exp. Med., 160: 1126-1146.
specific binding (% of control)
100
50
0
-13 -12 -11 -10 -9 -8
log [drug] (M)
IL-2
IL-1β
IL-4
IL-6
IL-4 - agonist radioligand
binding
Ref. 0074
[Custom offer]
Please contact us at:
customresearch@cerep.com
Source
Ligand
Kd
Non specific
Reference
MLA 144 cells
[ 125 I]IL-4 (0.03 nM)
0.03 nM
IL-4 (100 nM)
IL-4 (IC 50 : 0.1 nM)
Galizzi, J.P. et al. (1990) J. Biol. Chem., 265: 439-444.
specific binding (% of control)
100
50
0
-12 -11 -10 -9 -8
log [drug] (M)
IL-4
IL-1α
IL-6 - agonist radioligand
binding
Ref. 0075
[Custom offer]
Please contact us at:
customresearch@cerep.com
Source
Ligand
Kd
Non specific
Reference
U-266 cells
[ 125 I]IL-6 (0.05 nM)
0.25 nM
IL-6 (20 nM)
IL-6 (IC 50 : 0.3 nM)
Taga, T. et al. (1987) J. Exp. Med., 166: 967-981.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7
log [drug] (M)
IL-6
IL-1α
IL-4
IL-2
❚ GABA
GABA (non-selective) - agonist radioligand
binding
Ref. 0057
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]GABA (10 nM)
15 nM
GABA (100 µM)
GABA (IC 50 : 25 nM)
Tsuji, A. et al. (1988) Antimicrob. Agents Chemother., 32: 190-194.
specific binding (% of control)
100
50
0
-10 -9 -8 -7 -6 -5 -4 -3
log [drug] (M)
GABA
muscimol
baclofen
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Assay developed in 2010 New assay conditions Human Q Standard turnaround time

85
gaba ❚
GABA A1 (a1, b2, g2) - agonist radioligand
binding
Ref. 3051
Q 3 weeks
Included in:
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd (nM)
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]muscimol (15 nM)
30 nM
muscimol (10 µM)
muscimol (IC 50 : 75 nM)
Wang, X.K. (2001) Acta. Pharmacol. Sin., 22: 521-523.
Cerep
services
Receptors
[Other
receptors]
GABA A (automated patch-clamp)
cellul ar
Ref. 3260
Ref. 3393
Ref. 3394
Q 2 weeks
Agonist effect
Antagonist effect
Potentiator effect
Source
GABA A (α1β2γ2) CHO-K1 cell line
Test concentration 0.1, 1, and 10 µM
Detection method automated whole-cell patch-clamp
Agonist effect Reference muscimol (EC 50 : 3.4 μM)
Antagonist effect Reference bicuculline (IC 50 : 460 nM)
Potentiator effect Reference diazepam (EC 50 : 19 nM)
Sieghart, W. (1995) Pharmacol. Rev. 47(2):181-234.
GABA A (automated patch-clamp, functional screening)
cellul ar
Ref. G193
Q 2 weeks
Source
GABA A (conventional patch-clamp)
cellul ar
Ref. 2859
Ref. 3395
Ref. 3396
Q 2 weeks
Agonist effect
Antagonist effect
Potentiator effect
GABA A (α1β2γ2) CHO-K1 cell line
Test concentration 0.1, 1, and 10 µM
Detection method automated whole-cell patch-clamp
Agonist effect Reference muscimol (EC 50 : 3.4 μM)
Modulation effect Reference diazepam (EC 50 : 19 nM)
bicuculline (IC 50 : 460 nM)
Sieghart, W. (1995) Pharmacol. Rev. 47(2):181-234.
❚ This assay screens agonists, antagonists, and potentiators
Source
GABA A (α1β2γ2) CHO-K1 cell line
Test concentration 1 µM
Detection method conventional whole-cell patch-clamp
Agonist effect Reference muscimol (EC 50 : 1.7 μM)
Antagonist effect Reference bicuculline (IC 50 : 700 nM)
Potentiator effect Reference diazepam (EC 50 : 29 nM)
Sieghart, W. (1995) Pharmacol. Rev. 47(2):181-234.
no graph available
Ion
channels
Transporters
Kinases
Epigenetic &
DNA-related
enzymes
Other
enzymes
Specialized
cellular
assays
GABA A
tissue
Source
guinea-pig ileum
Agonist 3-APSA (pD 2 = 4.7)
Antagonist bicuculline (pA 2 = 5.7)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
tension (% of max.)
100
50
0
bicuculline
none
3 µM
10 µM
30 µM
Standard
profiles
Ref. 0314
Q 4 weeks
[Solvent] must be kept ≤ 0.1%
Giotti, A. et al. (1983) Brit. J. Pharmacol., 78: 469-478.
-6 -5 -4 -3
log [agonist] (M)
Testing
conditions
BZD (central) - agonist radioligand
binding
Ref. 0028
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]flunitrazepam (0.4 nM)
2.1 nM
diazepam (3 µM)
diazepam (IC 50 : 8.6 nM)
Speth, R.C. et al. (1979) Life Sci., 24: 351-358.
Ordering
information
Assay list
& index

86 in vitro pharmacology 2011 catalog
❚ gaba
Cl – channel (GABA-gated) - antagonist radioligand
binding
Ref. 0170
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 35 S]TBPS (3 nM)
14.6 nM
picrotoxinin (20 µM)
picrotoxinin (IC 50 : 150 nM)
Lewin, A.H. et al. (1989) Mol. Pharmacol., 35: 189-194.
specific binding (% of control)
100
50
picrotoxinin
muscimol
0
GABA
-9 -8 -7 -6 -5 -4
log [drug] (M)
❚ See other GABA assays pp. 38, 97 and 104
❚ Glutamate
AMPA - agonist radioligand
binding
Ref. 0064
Q 3 weeks
Included in:
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]AMPA (8 nM)
82 nM
L-glutamate (1 mM)
L-glutamate (IC 50 : 535 nM)
Murphy, D.E. et al. (1987) Neurochem. Res., 12: 775-781.
specific binding (% of control)
100
50
0
-8 -7 -6 -5 -4
log [drug] (M)
L-glutamate
kainic acid
CGS 19755
kainate - agonist radioligand
binding
Ref. 0065
Q 3 weeks
Included in:
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]kainic acid (5 nM)
19 nM
L-glutamate (1 mM)
kainic acid (IC 50 : 40 nM)
Monaghan, D.T. and Cotman, C.W. (1982) Brain Res., 252: 91-100.
specific binding (% of control)
100
50
0
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
kainic acid
L-glutamate
CGS 19755
NMDA - antagonist radioligand
binding
Ref. 0066
Q 3 weeks
Included in:
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]CGP 39653 (5 nM)
23 nM
L-glutamate (100 µM)
CGS 19755 (IC 50 : 550 nM)
Sills, M.A. et al. (1991) Eur. J. Pharmacol., 192: 19-24.
specific binding (% of control)
100
50
CGS 19755
L-glutamate
0
kainic acid
-9 -8 -7 -6 -5 -4
log [drug] (M)
PCP - antagonist radioligand
binding
Ref. 0124
Q 3 weeks
Included in:
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]TCP (10 nM)
13 nM
MK 801 (10 µM)
MK 801 (IC 50 : 5.3 nM)
Vignon, J. et al. (1986) Brain Res., 378: 133-141.
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Assay developed in 2010 New assay conditions Human Q Standard turnaround time

87
glycine (strychnine-insensitive) - antagonist radioligand
binding
Ref. 0068
Q 3 weeks
Included in:
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]MDL 105,519 (0.5 nM)
5 nM
glycine (1 mM)
glycine (IC 50 : 160 nM)
Baron, B.M. et al. (1996) J. Pharmacol. Exp. Ther., 279: 62-68.
specific binding (% of control)
GLUTAMATE ❚
100
50
glycine
7-Cl-kinurenate
0
strychnine
-9 -8 -7 -6 -5 -4
log [drug] (M)
Cerep
services
Receptors
[Other
receptors]
❚ Glycine
Ion
channels
strychnine-sensitive - antagonist radioligand
Source
rat spinal cord
Ligand
[ 3 H]strychnine (2 nM)
Kd
20 nM
Non specific strychnine (100 µM)
binding
Reference strychnine (IC 50 : 6.6 nM)
Ref. 0067
Q 3 weeks
Marvizon, J.C. et al. (1986) Mol. Pharmacol., 30: 590-597.
specific binding (% of control)
100
50
0
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
strychnine
glycine
7-Cl-kinurenate
Transporters
Kinases
❚ Growth factors
Epigenetic &
DNA-related
enzymes
EGF - agonist radioligand
Source
A-431 cells
Ligand
[ 125 I]EGF (0.05 nM)
Kd
0.63 nM
Non specific EGF (0.1 µM)
binding
Reference EGF (IC 50 : 1 nM)
Ref. 0069
Q inquire
Higashiyama, S. et al. (1991) Science, 251: 936-939.
specific binding (% of control)
100
50
0
-13 -12 -11 -10 -9 -8
log [drug] (M)
EGF
PDGF BB
TGF-β1
Other
enzymes
Specialized
cellular
assays
PDGF - agonist radioligand
binding
Ref. 0070
Q 3 weeks
Included in:
High-throughput profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
Balb/c 3T3 cells
[ 125 I]PDGF BB (0.03 nM)
0.15 nM
PDGF BB (10 nM)
PDGF BB (IC 50 : 0.0422 nM)
Williams, L.T. et al. (1984) J. Biol. Chem., 259: 5287-5294.
specific binding (% of control)
100
50
0
-11 -10 -9 -8
log [drug] (M)
PDGF BB
EGF
Standard
profiles
Testing
conditions
TGF-b - agonist radioligand
binding
Ref. 0071
[Custom offer]
Please contact us at:
customresearch@cerep.com
Source
Ligand
Kd
Non specific
Reference
Balb/c 3T3 cells
[ 125 I]TGF-b1 (0.05 nM)
0.15 nM
TGF-b1 (10 nM)
TGF-b1 (IC 50 : 0.5 nM)
Massague, J. (1987) Methods Enzymol., 146: 174-195.
β
Ordering
information
Assay list
& index

88 in vitro pharmacology 2011 catalog
❚ growth factors
VEGF - agonist radioligand
binding
Ref. 0672
[Custom offer]
Please contact us at:
customresearch@cerep.com
Source
Ligand
Kd
Non specific
Reference
HUV-EC-C cells
[ 125 I]VEGF (0.015 nM)
0.03 nM
VEGF (3 nM)
VEGF (IC 50 : 0.016 nM)
Gitay-Goren, H. et al. (1996) J. Biol. Chem., 271: 5519-5523.
β
❚ Imidazoline
I 1 - agonist radioligand
binding
Ref. 0642
Q 3 weeks
Included in:
Diversity profile
BioPrint ® profile
Organ safety profile
Source
bovine adrenal medulla glands
Ligand [ 3 H]clonidine (15 nM) (+ 10 µM RX 821002)
Kd
16 nM
Non specific rilmenidine (10 µM)
Reference
rilmenidine (IC 50 : 230 nM)
Moldering, G.J. et al. (1993) Naun.-Sch. Arch. Pharm., 348: 70-76.
specific binding (% of control)
100
50
0
-10 -9 -8 -7 -6 -5
log [drug] (M)
rilmenidine
I 2 - antagonist radioligand
binding
Ref. 0081
Q 3 weeks
Included in:
Diversity profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]idazoxan (2 nM) (+ 1 µM yohimbine)
4 nM
cirazoline (10 µM)
idazoxan (IC 50 : 8.4 nM)
Brown, C.M. et al. (1990) Brit. J. Pharmacol., 99: 803-809.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
idaxoxan
guanabenz
clonidine
phentolamine
❚ Insulin
insulin - agonist radioligand
binding
Ref. 0084
[Custom offer]
Please contact us at:
customresearch@cerep.com
Source
Ligand
Kd
Non specific
Reference
rat liver
[ 125 I]insulin (0.03 nM)
8 nM
insulin (10 µM)
insulin (IC 50 : 17 nM)
Koch, R. and Weber, U. (1981) Hoppe-Seyler’s Z. Physiol. Chem., 362: 347-351.
specific binding (% of control)
100
50
0
-10 -9 -8 -7 -6
log [drug] (M)
insulin
glucagon

89
❚ Melatonin
MT 3 (ML 2 ) - agonist radioligand
binding
Ref. 0088
Q 3 weeks
Included in:
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
hamster brain
[ 125 I]2-iodomelatonin (0.1 nM)
4.8 nM
melatonin (30 µM)
melatonin (IC 50 : 96.5 nM)
Pichering, D.S. and Niles, L.P. (1990) Eur. J. Pharmacol., 175: 71-77.
❚ See other Melatonin assays, page 49
Cerep
services
Receptors
[Other
receptors]
Ion
channels
❚ Nicotinic
Transporters
N muscle-type - antagonist radioligand
binding
Ref. 0936
Q 3 weeks
Included in:
BioPrint ® profile
Source
Ligand
Kd
Non specific
Reference
TE671 cells (endogenous)
N neuronal (a4b2) - agonist radioligand
binding
Ref. 3029
Q 3 weeks
Included in:
Diversity profile
BioPrint ® profile
Organ safety profile
[ 125 I]α-bungarotoxin (0.5 nM)
9.5 nM
α-bungarotoxin (5 µM)
α-bungarotoxin (IC 50 : 14 nM)
specific binding (% of control)
100
50
0
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
α-bungarotoxin
tubocurarine
nicotine
atropine
Lukas, R.J. (1986) J. Neurochem., 46: 1936-1941.
[Custom offer] mouse BC3H1 cells model (Ref. 0111), please contact us at customresearch@cerep.com
Source
Ligand
Kd (nM)
Non specific
Reference
SH-SY5Y cells (endogenous)
[ 3 H]cytisine (0.6 nM)
0.3 nM
nicotine (10 µM)
nicotine bitartrate salt (IC 50 : 3 nM)
Gopalakrishnan et al.(1996) J. Pharmacol. Exp. Ther., 276: 289-297.
α
Kinases
Epigenetic &
DNA-related
enzymes
Other
enzymes
Specialized
cellular
assays
N neuronal (a4b2) - agonist radioligand
binding
Ref. 0110
[Custom offer]
Please contact us at:
customresearch@cerep.com
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]cytisine (1.5 nM)
1.8 nM
nicotine (10 µM)
nicotine (IC 50 : 8.7 nM)
Pabreza, L.A. et al. (1991) Mol. Pharmacol., 39: 9-12.
specific binding (% of control)
100
50
nicotine
carbachol
atropine
0
α-bungarotoxin
-10 -8 -7 -6 -5 -4 -9 -3
log [drug] (M)
Standard
profiles
Testing
conditions
N neuronal (a7) - antagonist radioligand
Source
SH-SY5Y cells (endogenous)
Ligand
[ 125 I]α-bungarotoxin
binding
Kd (nM) 0.34 nM
Ref. 3010
Non specific α-bungarotoxin (1 µM)
Q 3 weeks
Reference α-bungarotoxin (IC 50 : 2.1 nM)
Included in:
Organ safety profile
Sharples et al.(2000) J. Neurosci., 20: 2783-2791.
α
Ordering
information
Assay list
& index

90 in vitro pharmacology 2011 catalog
❚ nicotinic
N neuronal (a7) - antagonist radioligand
binding
Ref. 0567
[Custom offer]
Please contact us at:
customresearch@cerep.com
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 125 I]α-bungarotoxin (1 nM)
0.3 nM
α-bungarotoxin (1 µM)
α-bungarotoxin (IC 50 : 1.7 nM)
Sharples, C.G.V. et al. (2000) J. Neurosci., 20: 2783-2791.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4 -3
log [drug] (M)
α-bungarotoxin
epibatidine
tubocurarine
nicotine
❚ Purinergic
P2X - agonist radioligand
binding
Ref. 0127
Q 3 weeks
Included in:
High-throughput profile
Diversity profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat urinary bladder
[ 3 H]α,β-MeATP (3 nM)
2.6 nM
α,β-MeATP (10 µM)
α,β-MeATP (IC 50 : 3.5 nM)
Bo, X. and Burnstock, G. (1990) Brit. J. Pharmacol., 101: 291-296.
specific binding (% of control)
100
50
0
-10 -9 -8 -7 -6 -5 -4 -3
log [drug] (M)
α,β-MeATP
suramin
adenosine
P2X
tissue
Ref. 0332
Q 4 weeks
Source
rabbit ear artery (endothelium-denuded)
Agonist α,βMeATP (pD 2 = 6.9)
Antagonist suramin (pA 2 = 4.9)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
O’Connor, S.E. et al. (1990) Brit. J. Pharmacol., 101: 640-644.
tension (% of max.)
100
50
0
-9 -8 -7 -6 -5 -4
log [agonist] (M)
suramin
none
30 µM
100 µM
300 µM
❚ See other Purinergic assays, pp. 67 and 101
❚ Serotonin
5-HT 3 - antagonist radioligand
binding
Ref. 0411
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]BRL 43694 (0.5 nM)
1.15 nM
MDL 72222 (10 µM)
MDL 72222 (IC 50 : 10 nM)
Hope, A.G. et al. (1996) Brit. J. Pharmacol., 118: 1237-1245.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4 -3
log [drug] (M)
MDL 72222
serotonin
8-OH-DPAT
ketanserin
5-HT 3
tissue
Ref. 0335
Q 4 weeks
Source
guinea-pig colon
Agonist serotonin (pD 2 = 5.6)
Antagonist MDL 72222 (pA 2 = 5.7)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Butler, A. et al. (1990) Brit. J. Pharmacol., 101: 591-598.
tension (% of max.)
100
50
0
-8 -7 -6 -5 -4
log [agonist] (M)
MDL 72222
none
1 µM
3 µM
10 µM
❚ See other Serotonin assays pp. 68, 101 and 105

91
❚ Sigma
Cerep
services
sigma (non-selective) - agonist radioligand
binding
Ref. 0146
Q 3 weeks
Included in:
High-throughput profile
Diversity profile
BioPrint ® profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]DTG (8 nM)
29 nM
haloperidol (10 µM)
haloperidol (IC 50 : 48 nM)
Shirayama, Y. et al. (1993) Eur. J. Pharmacol., 237: 117-126.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
haloperidol
(+)3-PPP
(+)pentazocine
(+)SKF 10,047
Receptors
[Other
receptors]
Ion
channels
sigma (non-selective)
tissue
Ref. 0337
Q 4 weeks
Source
guinea-pig vas deferens (field-stimulated)
Agonist (+)SKF 10,047 (pD 2 = 4.7)
Antagonist rimcazole
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Vaupel, D.B. and Su, T.P. (1987) Eur. J. Pharmacol., 139: 125-128.
tension (% of max.)
100
50
0
-6 -5 -4
log [agonist] (M)
Transporters
Kinases
sigma 1 - agonist radioligand
Source
Jurkat cells (endogenous)
Ligand
[ 3 H](+)pentazocine (15 nM)
binding
Kd
37 nM
Ref. 0889
Non specific haloperidol (10 µM)
Q 3 weeks
Reference haloperidol (IC 50 : 11.4 nM)
Included in:
Organ safety profile
Ganapathy, M.E. et al. (1999) J. Pharmacol. Exp. Ther., 289: 251-260.
sigma 2 - agonist radioligand
-10 -9 -8 -7 -6 -5 -4 -3
100
-11 -10 -9 -8 -7 -6 -5 -4 -3
-12 -11 -10 -9 -8 -7 -6 -5 -4
50
-13 -12 -11 -10 -9 -8 -7 -6 -5
-9 -8 -7 -6
-10
haloperidol
(+)3-PPP
-10 -9 -8 -7 -6 -5 -4
0
(+)SKF 10,047
-3
-11 -12 - 10 -11 -9 -10-8 -9 -7-8 -7 -6 -6-5 -5 -4 -4
log [drug] (M)
-9 -8 -7 -12 -11 -10 -6 -5
-11 -10 -9 -8 -7 -6 -5 -4
[Custom offer] guinea-pig brain model (Ref. 0147), please contact us at customresearch@cerep.com
Source
rat cerebral cortex
Ligand
[ 3 H]DTG (5 nM) (+ 300 nM (+)pentazocine)
binding
Kd
32 nM
Ref. 0148
Non specific haloperidol (10 µM)
Q 3 weeks
Reference haloperidol (IC 50 : 120 nM)
Included in:
Organ safety profile
Bowen, W.D. et al. (1993) Mol. Neuropharmacol., 3: 117-126.
specific binding (% of control)
specific binding (% of control)
100
50
haloperidol
0
(+)3-PPP
(+)SKF 10,047
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
Epigenetic &
DNA-related
enzymes
Other
enzymes
Specialized
cellular
assays
Standard
profiles
Testing
conditions
Ordering
information
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Assay developed in 2010 New assay conditions Human Q Standard turnaround time
Assay list
& index

92 in vitro pharmacology 2011 catalog
❚ notes
❚ see also ADME-Tox & PK 2011 catalog
ADME-Tox & PK
2011 CATALOG
IN VITRO ADME
Solution properties
Drug absorption/drug transport
Drug metabolism
Drug-drug interactions
IN VITRO TOXICITY
Cardiac toxicity
Cytotoxicity
Genetic toxicity
IN VIVO PK/BIOANALYTICAL
In vivo PK
Bioanalytical
ASSAY SELECTION GUIDE
STANDARD PROFILES
APPLICATION NOTES

93
Cerep
services
[Voltage-gated channels]
ion channels
Receptors
Ion
channels
❚ Ca 2+ channels
Transporters
Ca 2+ - L (dihydropyridine site) - antagonist radioligand
binding
Ref. 0161
Q 3 weeks
Included in:
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]nitrendipine (0.2 nM)
0.4 nM
nifedipine (1 µM)
nitrendipine (IC 50 : 0.27 nM)
Gould, R.J. et al. (1982) Proc. Natl. Acad. Sci. USA, 79: 3656-3660.
specific binding (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
nitrendipine
nifedipine
D 600
diltiazem
Kinases
Epigenetic &
DNA-related
enzymes
Ca 2+ - L (diltiazem site) (benzothiazepines) - antagonist radioligand
binding
Ref. 0162
Q 3 weeks
Included in:
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]diltiazem (15 nM)
52 nM
diltiazem (10 µM)
diltiazem (IC 50 : 32 nM)
Shoemaker, H. and Langer, S.Z. (1985) Eur. J. Pharmacol., 111: 273-277.
Other
enzymes
Specialized
cellular
assays
Ca 2+ - L (verapamil site) (phenylalkylamine) - antagonist radioligand
binding
Ref. 0163
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H](-)D 888 (3 nM)
3 nM
D 600 (10 µM)
D 600 (IC 50 : 49 nM)
Reynolds, I.J. et al. (1986) J. Pharmacol. Exp. Ther., 237: 731-738.
Standard
profiles
Testing
conditions
Ca 2+ - L
tissue
Source
Agonist
Antagonist
rat aorta (endothelium-denuded)
KCl
nitrendipine
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
tension (% of control)
100
50
0
nitrendipine
Ordering
information
Ref. 0339
Q 4 weeks
[Solvent] must be kept ≤ 0.1%
Okamiya, Y. et al. (1991) Eur. J. Pharmacol., 205: 49-54.
-11 -10 -9 -8
log [agonist] (M)
Assay list
& index

94 in vitro pharmacology 2011 catalog
❚ voltage-gated channels [Ca 2+ channels]
Ca 2+ - N - antagonist radioligand
binding
Ref. 0164
Q 3 weeks
Included in:
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 125 I]ω-conotoxin GVIA (1 pM)
0.7 pM
ω-conotoxin GVIA (10 nM)
ω-conotoxin GVIA (IC 50 : 1.5 pM)
Wagner, J.A. et al. (1988) J. Neurosci., 8: 3354-3359.
specific binding (% of control)
100
50
ω-conotoxin
GVIA
0
neomycin
nitrendipine
-13 -12 -11 -10 -9 -8 -7 -6 -5
log [drug] (M)
❚ See other Ca 2+ channels assays, page 102
❚ K + channels
hERG (membrane preparation) - antagonist radioligand
Source
human recombinant (HEK-293 cells)
Ligand
[ 3 H]astemizole (2 nM)
binding
Kd
2 nM
Non specific astemizole (10 µM)
Ref. 1868
Q 3 weeks
Reference astemizole (IC 50 : 3 nM)
Included in:
Organ safety profile
Finlayson, K. et al. (2001) Eur. J. Pharmacol., 412: 203-212.
specific binding (% of control)
100
50
0
astemizole
dofetilide
amiodarone
cisapride
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
hERG (automated patch-clamp)
cellul ar
Ref. 2245
Q 2 weeks
Included in:
Organ safety profile
ADME-Tox Option II [Lead selection
/Prioritization]
electrophysiology
Source
hERG CHO-K1 cell line
Test concentration 0.1, 1, and 10 µM
Detection method automated whole-cell patch-clamp
Reference E-4031 (IC 50 : 25.6 nM)
❚ Recommended for screening of hERG liability
Mathes, C. (2006) Expert Opin. Ther. Targets, 10 (2): 230-241
hERG (conventional patch-clamp)
cellul ar
Ref. 2027
Q 2 weeks
electrophysiology
Source
hERG HEK-293 cell line
Test concentration 1 µM
Detection method conventional whole-cell patch-clamp
Reference E-4031 (IC 50 : 8.2 nM)
❚ Recommended for a rigorous characterization of hERG interaction
Zhou, Z. et al. (1998) Biophys. Journal, 74: 230-241.
current amplitude (% of control)
100
50
0
-10 -9 -8 -7 -6
log [drug] (M)
E-4031
terfenadine
astemizole
K ATP - antagonist radioligand
binding
Ref. 0165
Q 3 weeks
Included in:
Diversity profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]glibenclamide (0.1 nM)
0.05 nM
glibenclamide (1 µM)
glibenclamide (IC 50 : 0.16 nM)
Angel, I. and Bidet, S. (1991) Fundam. Clin. Pharmacol., 5: 107-115.

voltage-gated channels [K + channels] ❚
95
K ATP
tissue
Source
rat aorta (precontracted with 20 mM KCl)
Agonist cromakalim (pD 2 = 7.2)
Antagonist glibenclamide (pA 2 = 7.4)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
tension (% of control)
100
50
0
glibenclamide
none
0.1 µM
0.3 µM
1 µM
Cerep
services
Ref. 0340
Q 4 weeks
[Solvent] must be kept ≤ 0.1%
Newgreen, D.T. et al. (1990) Brit. J. Pharmacol., 100: 605-613.
-9 -8 -7 -6 -5
log [agonist] (M)
Receptors
K V - antagonist radioligand
binding
Ref. 0166
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 125 I]α-dendrotoxin (0.01 nM)
0.04 nM
α-dendrotoxin (50 nM)
α-dendrotoxin (IC 50 : 0.1 nM)
Sorensen, R.G. and Blaustein, M.P. (1989) Mol. Pharmacol., 36: 689-698.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6
log [drug] (M)
α-dendrotoxin
charybdotoxin
apamin
glibenclamide
Ion
channels
Transporters
SK Ca - antagonist radioligand
binding
Ref. 0167
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 125 I]apamin (7 pM)
7 pM
apamin (100 nM)
apamin (IC 50 : 0.0091 nM)
Hugues, M. et al. (1982) J. Biol. Chem., 257: 2762-2769.
specific binding (% of control)
100
50
0
-13 -12 -11 -10 -9 -8 -7 -6 -5
log [drug] (M)
apamin
charybdotoxin
glibenclamide
Kinases
Epigenetic &
DNA-related
enzymes
selected cerep assays
❚ ion channel patch-clamp assays
Electrophysiological assays are developed using both conventional (manual) and automated patch-clamp (Qpatch) to measure agonist,
antagonist and modulator effect of compounds.
The automated patch-clamp system is based on planar glass-coated silicon chips with micro-etched patch-clamp holes. It performs a true
giga-ohm seal patch-clamp, which is the principle used in conventional patch-clamp. Mammalian cell lines (HEK-293 or CHO-K1) stably
expressing various ion channel genes are used. The automated patch-clamp performs multiple independent patch-clamp experiments in
parallel in a disposable electrode array.
❚ binding assays
Binding assays are developed according to the competition assay principle. There are three assay formats used: filtration, scintillation
proximity assay (SPA) and centrifugation. All formats utilize a radiolabeled ligand and a source of receptor (membranes, soluble/purified).
Large batches of cells, from which prepared membranes are frozen and stored, are produced in-house. Membrane preparations are
quality controlled before use.
❚ tissue bioassays
Tissue bioassays are functional assays designed to evaluate the agonist and antagonist activities of compounds at various receptors and
ion channels in whole tissues. The tissues used are isolated from contractile cardiac and smooth muscles of the cardiovascular, respiratory,
gastrointestinal and urogenital tracts of rodents, rabbit or human. The selected tissues are assayed in organ bath systems to record the
contractile activity in conditions as selective as possible to avoid any potential interaction with other receptors known to be present in the
tissue used.
Other
enzymes
Specialized
cellular
assays
Standard
profiles
Testing
conditions
Ordering
information
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Assay developed in 2010 New assay conditions Human Q Standard turnaround time
Assay list
& index

96 in vitro pharmacology 2011 catalog
❚ Na + channels
Na + - site 2 - antagonist radioligand
binding
Ref. 0169
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]batrachotoxinin (10 nM)
91 nM
veratridine (300 µM)
veratridine (IC 50 : 4.5 µM)
Brown, G.B. (1986) J. Neurosci., 6: 2064-2070.
specific binding (% of control)
100
50
0
-10 -9 -8 -7 -6 -5 -4 -3
log [drug] (M)
veratridine
tetrodotoxin
lidocaine
Na +
cellul ar
Ref. 0219 Activator effect
Ref. 0220 Inhibitor effect
[Custom offer]
Please contact us at:
[CUSTOM OFFER]
Source
SK-N-SH cells
Measured product 22 Na uptake
Detection method scintillation counting
Activator effect Control veratridine (0.1 mM)
Reference veratridine (EC 50 : 7 µM)
Inhibitor effect Stimulant veratridine (100 µM)
Reference tetrodotoxin (IC 50 : 6 nM)
Jacques, Y. et al. (1978) J. Biol. Chem., 253: 7383-7392..
[Solvent] must be kept 0.1%
Na V 1.5 (automated patch-clamp)
cellul ar
Ref. 2393
Q 2 weeks
electrophysiology
Source
Na V 1.5 HEK-293 cell line
Test concentration 0.1, 1, and 10 µM
Detection method automated whole-cell patch-clamp
Reference
tetracaine (IC 50 : 2.5 µM)
Krafte, D. et al. (1995) J. Mol. Cell Cardiol. 27:823-830
Na V 1.5 (conventional patch-clamp)
cellul ar
Ref. 1938
Q 2 weeks
electrophysiology
Source
Na V 1.5 HEK-293 cell line
Test concentration 10 µM
Detection method conventional whole-cell patch-clamp
Reference
tetracaine (IC 50 : 4.0 µM)
Krafte, D. et al. (1995) J. Mol. Cell Cardiol. 27:823-830
❚
transient receptor potential channels
TRPM8
cellul ar
Ref. 3316
Ref. 3317
Q 3 weeks
Source
human recombinant
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control icilin (3 µM)
Reference icilin (EC 50 : 63 nM)
Antagonist effect Stimulant icilin (100 nM)
Reference BCTC (IC 50 : 1400 nM)
Behrendt, H.J., (2004) Br. J. Pharmacol., 141: 737-745.
[Solvent] must be kept 0.1%

transient receptor potential channels ❚
97
TRPV1 (VR1)
cellul ar
Ref. 1640
Ref. 1641
Q 3 weeks
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control capsaicin (1 µM)
Reference capsaicin (EC 50 : 12.5 nM)
Antagonist effect Stimulant capsaicin (30 nM)
Reference capsazepin (IC 50 : 296 nM)
Phelps, P.T. et al. (2005) Eur. J. Pharmacol., 513: 57-66.
Ca 2+ mobilization (% of control)
100
100
50
50
0
0
-10 -9 -8 -7 -6 -5 -8 -7 -6 -5
log [agonist] (M)
log [antagonist] (M)
capsaicin
capsazepin
resiniferatoxin
ruthenium red
olvanil
AMG 9810
AM 404
[Solvent] must be kept ≤ 0.3%
Cerep
services
Receptors
TRPV3
cellul ar
Ref. 2719
Ref. 2722
Q 3 weeks
Source
human recombinant (HEK-293 cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control 2-APB (200 µM)
Reference 2-APB (EC 50 : 13 µM)
Antagonist effect Stimulant 2-APB (50 µM)
Reference ruthenium red (IC 50 : 1.4 µM)
Chung, M.K. et al. (2004) J. Neurosci., 24: 5177-5182.
-12 -11 -10 -9 -8 -7
-11 -10
-12 -11 -10 -9 -8 -7
-12 -11
-11 -10 -9 -8 -7 -6 -5 -4
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
-9 -8 -7 -6 -5 -4
[Solvent] must be kept 0.3%
Ion
channels
Transporters
[membrane
ligand-gated channels]
Kinases
❚ GABA channels
Epigenetic &
DNA-related
enzymes
GABA A1 (a1, b2, g2) - agonist radioligand
binding
Ref. 3051
Q 3 weeks
Included in:
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd (nM)
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]muscimol (15 nM)
30 nM
muscimol (10 µM)
muscimol (IC 50 : 75 nM)
Wang, X.K. (2001) Acta. Pharmacol. Sin., 22: 521-523.
Other
enzymes
Specialized
cellular
assays
GABA A (automated patch-clamp)
cellul ar
Ref. 3260
Ref. 3393
Ref. 3394
Q 2 weeks
Agonist effect
Antagonist effect
Potentiator effect
Source
GABA A (α1β2γ2) CHO-K1 cell line
Test concentration 0.1, 1, and 10 µM
Detection method automated whole-cell patch-clamp
Agonist effect Reference muscimol (EC 50 : 3.4 μM)
Antagonist effect Reference bicuculline (IC 50 : 460 nM)
Potentiator effect Reference diazepam (EC 50 : 19 nM)
Sieghart, W. (1995) Pharmacol. Rev. 47(2):181-234.
GABA A (automated patch-clamp, functional screening)
cellul ar
Ref. G193
Q 2 weeks
Source
GABA A (α1β2γ2) CHO-K1 cell line
Test concentration 0.1, 1, and 10 µM
Detection method automated whole-cell patch-clamp
Agonist effect Reference muscimol (EC 50 : 3.4 μM)
Modulation effect Reference diazepam (EC 50 : 19 nM)
bicuculline (IC 50 : 460 nM)
Sieghart, W. (1995) Pharmacol. Rev. 47(2):181-234.
❚ This assay screens agonists, antagonists, and potentiators
no graph available
Standard
profiles
Testing
conditions
Ordering
information
Assay list
& index

98 in vitro pharmacology 2011 catalog
❚ membrane ligand-gated channels [gaba]
GABA A (conventional patch-clamp)
cellul ar
Ref. 2859
Ref. 3395
Ref. 3396
Q 2 weeks
Agonist effect
Antagonist effect
Potentiator effect
Source
GABA A (α1β2γ2) CHO-K1 cell line
Test concentration 1 µM
Detection method conventional whole-cell patch-clamp
Agonist effect Reference muscimol (EC 50 : 1.7 μM)
Antagonist effect Reference bicuculline (IC 50 : 700 nM)
Potentiator effect Reference diazepam (EC 50 : 29 nM)
Sieghart, W. (1995) Pharmacol. Rev. 47(2):181-234.
GABA A
tissue
Source
guinea-pig ileum
Agonist 3-APSA (pD 2 = 4.7)
Antagonist bicuculline (pA 2 = 5.7)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
tension (% of max.)
100
50
0
bicuculline
none
3 µM
10 µM
30 µM
Ref. 0314
Q 4 weeks
[Solvent] must be kept ≤ 0.1%
Giotti, A. et al. (1983) Brit. J. Pharmacol., 78: 469-478.
-6 -5 -4 -3
log [agonist] (M)
BZD (central) - agonist radioligand
binding
Ref. 0028
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]flunitrazepam (0.4 nM)
2.1 nM
diazepam (3 µM)
diazepam (IC 50 : 8.6 nM)
Speth, R.C. et al. (1979) Life Sci., 24: 351-358.
Cl – channel (GABA-gated) - antagonist radioligand
binding
Ref. 0170
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 35 S]TBPS (3 nM)
14.6 nM
picrotoxinin (20 µM)
picrotoxinin (IC 50 : 150 nM)
Lewin, A.H. et al. (1989) Mol. Pharmacol., 35: 189-194.
specific binding (% of control)
100
50
picrotoxinin
muscimol
0
GABA
-9 -8 -7 -6 -5 -4
log [drug] (M)
❚ See other GABA assays, pp. 38, 84 and 104
❚ glutamate channels
AMPA - agonist radioligand
binding
Ref. 0064
Q 3 weeks
Included in:
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]AMPA (8 nM)
82 nM
L-glutamate (1 mM)
L-glutamate (IC 50 : 535 nM)
Murphy, D.E. et al. (1987) Neurochem. Res., 12: 775-781.
specific binding (% of control)
100
50
0
-8 -7 -6 -5 -4
log [drug] (M)
L-glutamate
kainic acid
CGS 19755

99
kainate - agonist radioligand
binding
Ref. 0065
Q 3 weeks
Included in:
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]kainic acid (5 nM)
19 nM
L-glutamate (1 mM)
kainic acid (IC 50 : 40 nM)
Monaghan, D.T. and Cotman, C.W. (1982) Brain Res., 252: 91-100.
membrane ligand-gated channels [glutamate] ❚
specific binding (% of control)
100
50
0
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
kainic acid
L-glutamate
CGS 19755
Cerep
services
Receptors
NMDA - antagonist radioligand
binding
Ref. 0066
Q 3 weeks
Included in:
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]CGP 39653 (5 nM)
23 nM
L-glutamate (100 µM)
CGS 19755 (IC 50 : 550 nM)
Sills, M.A. et al. (1991) Eur. J. Pharmacol., 192: 19-24.
specific binding (% of control)
100
50
CGS 19755
L-glutamate
0
kainic acid
-9 -8 -7 -6 -5 -4
log [drug] (M)
Ion
channels
Transporters
PCP - antagonist radioligand
binding
Ref. 0124
Q 3 weeks
Included in:
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]TCP (10 nM)
13 nM
MK 801 (10 µM)
MK 801 (IC 50 : 5.3 nM)
Vignon, J. et al. (1986) Brain Res., 378: 133-141.
Kinases
Epigenetic &
DNA-related
enzymes
glycine (strychnine-insensitive) - antagonist radioligand
binding
Ref. 0068
Q 3 weeks
Included in:
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]MDL 105,519 (0.5 nM)
5 nM
glycine (1 mM)
glycine (IC 50 : 160 nM)
Baron, B.M. et al. (1996) J. Pharmacol. Exp. Ther., 279: 62-68.
specific binding (% of control)
100
50
0
-9 -8 -7 -6 -5 -4
log [drug] (M)
glycine
7-Cl-kinurenate
strychnine
Other
enzymes
Specialized
cellular
assays
❚ glycine channels
Standard
profiles
strychnine-sensitive - antagonist radioligand
Source
rat spinal cord
Ligand
[ 3 H]strychnine (2 nM)
Kd
20 nM
Non specific strychnine (100 µM)
binding
Ref. 0067
Reference strychnine (IC 50 : 6.6 nM)
Q 3 weeks
Marvizon, J.C. et al. (1986) Mol. Pharmacol., 30: 590-597
specific binding (% of control)
100
50
0
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
strychnine
glycine
7-Cl-kinurenate
Testing
conditions
Ordering
information
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Assay developed in 2010 New assay conditions Human Q Standard turnaround time
Assay list
& index

100 in vitro pharmacology 2011 catalog
❚ nicotinic channels
N muscle-type - antagonist radioligand
binding
Ref. 0936
Q 3 weeks
Included in:
BioPrint ® profile
Source
Ligand
Kd
Non specific
Reference
TE671 cells (endogenous)
N neuronal (a4b2) - agonist radioligand
binding
Ref. 3029
Q 3 weeks
Included in:
Diversity profile
BioPrint ® profile
Organ safety profile
[ 125 I]α-bungarotoxin (0.5 nM)
9.5 nM
α-bungarotoxin (5 µM)
α-bungarotoxin (IC 50 : 14 nM)
specific binding (% of control)
100
50
0
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
α-bungarotoxin
tubocurarine
nicotine
atropine
Lukas, R.J. (1986) J. Neurochem., 46: 1936-1941.
[Custom offer] mouse BC3H1 cells model (Ref. 0111), please contact us at customresearch@cerep.com
Source
Ligand
Kd (nM)
Non specific
Reference
SH-SY5Y cells (endogenous)
[ 3 H]cytisine (0.6 nM)
0.3 nM
nicotine (10 µM)
nicotine bitartrate salt (IC 50 : 3 nM)
Gopalakrishnan et al.(1996) J. Pharmacol. Exp. Ther., 276: 289-297.
α
N neuronal (a4b2) - agonist radioligand
binding
Ref. 0110
[Custom offer]
Please contact us at:
customresearch@cerep.com
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 3 H]cytisine (1.5 nM)
1.8 nM
nicotine (10 µM)
nicotine (IC 50 : 8.7 nM)
Pabreza, L.A. et al. (1991) Mol. Pharmacol., 39: 9-12.
specific binding (% of control)
100
50
nicotine
carbachol
atropine
0
α-bungarotoxin
-10 -8 -7 -6 -5 -4 -9 -3
log [drug] (M)
N neuronal (a7) - antagonist radioligand
binding
Ref. 0567
[Custom offer]
Please contact us at:
customresearch@cerep.com
Source
Ligand
Kd
Non specific
Reference
rat cerebral cortex
[ 125 I]α-bungarotoxin (1 nM)
0.3 nM
α-bungarotoxin (1 µM)
α-bungarotoxin (IC 50 : 1.7 nM)
Sharples, C.G.V. et al. (2000) J. Neurosci., 20: 2783-2791.
specific binding (% of control)
100
50
0
-10 -9 -7 -6 -5 -4 -3
-11 -8
log [drug] (M)
α-bungarotoxin
epibatidine
tubocurarine
nicotine
N neuronal (a7) - antagonist radioligand
Source
SH-SY5Y cells (endogenous)
Ligand
[ 125 I]α-bungarotoxin
binding
Kd (nM) 0.34 nM
Ref. 3010
Non specific α-bungarotoxin (1 µM)
Q 3 weeks
Reference α-bungarotoxin (IC 50 : 2.1 nM)
Included in:
Organ safety profile
Sharples et al.(2000) J. Neurosci., 20: 2783-2791.
α
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Assay developed in 2010 New assay conditions Human Q Standard turnaround time

101
❚ purinergic channels
Cerep
services
P2X - agonist radioligand
binding
Ref. 0127
Q 3 weeks
Included in:
High-throughput profile
Diversity profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
rat urinary bladder
[ 3 H]α,β-MeATP (3 nM)
2.6 nM
α,β-MeATP (10 µM)
α,β-MeATP (IC 50 : 3.5 nM)
Bo, X. and Burnstock, G. (1990) Brit. J. Pharmacol., 101: 291-296.
specific binding (% of control)
100
50
0
-10 -9 -8 -7 -6 -5 -4 -3
log [drug] (M)
α,β-MeATP
suramin
adenosine
Receptors
Ion
channels
P2X
tissue
Ref. 0332
Q 4 weeks
Source
rabbit ear artery (endothelium-denuded)
Agonist α,βMeATP (pD 2 = 6.9)
Antagonist suramin (pA 2 = 4.9)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
O’Connor, S.E. et al. (1990) Brit. J. Pharmacol., 101: 640-644.
❚ serotonin channels
5-HT 3 - antagonist radioligand
binding
Ref. 0411
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
BioPrint ® profile
Organ safety profile
5-HT 3
tissue
Ref. 0335
Q 4 weeks
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]BRL 43694 (0.5 nM)
1.15 nM
MDL 72222 (10 µM)
MDL 72222 (IC 50 : 10 nM)
Hope, A.G. et al. (1996) Brit. J. Pharmacol., 118: 1237-1245.
Source
selected cerep assays
guinea-pig colon
Agonist serotonin (pD 2 = 5.6)
Antagonist MDL 72222 (pA 2 = 5.7)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Butler, A. et al. (1990) Brit. J. Pharmacol., 101: 591-598.
tension (% of max.)
100
50
0
-9 -8 -7 -6 -5 -4
log [agonist] (M)
suramin
none
30 µM
100 µM
300 µM
❚ See other Purinergic assays, pp.67 and 90
specific binding (% of control)
tension (% of max.)
100
50
0
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4 -3
log [drug] (M)
-8 -7 -6 -5 -4
log [agonist] (M)
MDL 72222
serotonin
8-OH-DPAT
ketanserin
MDL 72222
none
1 µM
3 µM
10 µM
❚ See other Serotonin assays, pp. 69, 90 and 105
❚ binding assays
Binding assays are developed according to the competition assay principle. There are three assay formats used: filtration, scintillation proximity
assay (SPA) and centrifugation. All formats utilize a radiolabeled ligand and a source of receptor (membranes, soluble/purified). Large batches of
cells, from which prepared membranes are frozen and stored, are produced in-house. Membrane preparations are quality controlled before use.
❚ tissue bioassays
Tissue bioassays are functional assays designed to evaluate the agonist and antagonist activities of compounds at various receptors and
ion channels in whole tissues. The tissues used are isolated from contractile cardiac and smooth muscles of the cardiovascular, respiratory,
gastrointestinal and urogenital tracts of rodents, rabbit or human. The selected tissues are assayed in organ bath systems to record the contractile
activity in conditions as selective as possible to avoid any potential interaction with other receptors known to be present in the tissue used.
Transporters
Kinases
Epigenetic &
DNA-related
enzymes
Other
enzymes
Specialized
cellular
assays
Standard
profiles
Testing
conditions
Ordering
information
Assay list
& index

102 in vitro pharmacology 2011 catalog
[Intracellular ligand-gated channels]
❚ Ca 2+ channels
IP 3 - agonist radioligand
Source
rat cerebellum
Ligand
[ 3 H]D-(1,4,5)IP 3 (0.5 nM)
Kd
11 nM
Non specific D-(1,4,5)IP 3 (1 µM)
binding
Ref. 0083
Reference D-(1,4,5)IP 3 (IC 50 : 23 nM)
Q 3 weeks
Worley, P.F. et al. (1987) J. Biol. Chem., 262: 12132-12136.
RY3 (ryanodine) - agonist radioligand
Source
rat cerebral cortex
Ligand
[ 3 H]ryanodine (3 nM)
Kd
6 nM
Non specific ryanodine (10 µM)
binding
Ref. 0627
Reference ryanodine (IC 50 : 7.7 nM)
Q 3 weeks
Padua, R. A. et al. (1992) Brain Res., 542: 135-140.
specific binding (% of control)
100
50
0
ryanodine
ruthenium red
heparin
-11 -10 -9 -8 -7 -6 -5 -4 -3
log [drug] (M)
❚ For radioligand binding assays, how should I choose between the agonist and the antagonist models when both are
available?
For some binding assays two models are available using either agonist or antagonist as radioligand.
G-protein-coupled receptors have both high-affinity and low-affinity states that are bound differently by agonists and antagonists. Whereas
the antagonists bind with an equal affinity to both affinity states, agonists bind poorly to the low affinity state of the receptor. Therefore,
it is advisable to use an antagonist radioligand to evaluate the binding of antagonists knowing that this may fail to reveal the binding
of agonists. On the other hand, an assay using an agonist radioligand is suitable to evaluate both agonists and antagonists.
The testing of a compound in both assays and the comparison of its competition curves against each radioligand may provide information
about its functional activity at the receptor.

103
Cerep
services
transporters
Receptors
❚ adenosine
adenosine transporter - antagonist radioligand
Source
guinea-pig cerebral cortex
binding
Ligand
[ 3 H]NBTI (0.15 nM)
Kd
0.08 nM
Ref. 0007
Non specific NBTI (5 µM)
Q 3 weeks
Reference NBTI (IC 50 : 0.2 nM)
Included in:
Organ safety profile
Verma, A. and Marangos, P.J. (1985) Life Sci., 36: 286-290.
specific binding (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
NBTI
dipyridamole
CPA
Ion
channels
Transporters
adenosine uptake
cellul ar
Ref. 3374
Q 3 weeks
Source
Hela cells
Tracer
[ 3 H]2-8 adenosine (0.1 µM)
Measured product [ 3 H]2-8 adenosine incorporation into Hela
cells
Detection method scintillation counting
Reference
❚ cannabinoid
anandamide uptake
cellul ar
Ref. 0647
Q 4 weeks
❚ choline
NBTI (IC 50 : 1.1 nM)
Harley, E.R. et al.(1982) Cancer Res., 42: 1289-1295.
Source
U-937 cells
Tracer
[ 3 H]AEA (2 nM) + AEA (98 nM)
Measured product [ 3 H]AEA incorporation into U-937 cells
Detection method scintillation counting
Reference
AM 404 (IC 50 : 1 µM)
Maccarrone, M. et al. (1998) J. Biol. Chem., 273: 32332-32339.
choline transporter (CHT1) - antagonist radioligand
binding
Ref. 1552
Q 3 weeks
Included in:
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]hemicholinium-3 (3 nM)
3.9 nM
hemicholinium-3 (10 µM)
hemicholinium-3 (IC 50 : 14 nM)
Apparsundaram, S. et al. (2000) Bioch. Biophys. Res. Com., 276: 862-867.
❚ See other Adenosine assays, page 13
AEA uptake (% of control)
100
50
0
-9 -8 -7 -6 -5 -4
log [drug] (M)
AM 404
AEA
❚ See other Cannabinoid assays, page 27
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4 -3 -2 -1
log [drug] (M)
hemicholinium-3
choline
carbachol
Kinases
Epigenetic &
DNA-related
enzymes
Other
enzymes
Specialized
cellular
assays
Standard
profiles
Testing
conditions
Ordering
information
Assay list
& index

104 in vitro pharmacology 2011 catalog
❚ dopamine
dopamine transporter - antagonist radioligand
binding
Ref. 0052
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
dopamine uptake
cellul ar
Ref. 0394
Q 3 weeks
❚ gaba
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]BTCP (4 nM)
4.5 nM
BTCP (10 µM)
BTCP (IC 50 : 7.1 nM)
specific binding (% of control)
100
50
0
-11 - 10 -9 -8 -7 -6 -5 -4 -3
log [drug] (M)
Pristupa, Z.B. et al. (1994) Mol. Pharmacol., 45: 125-135.
[Custom offer] rat striatum model (Ref. 0051), please contact us at customresearch@cerep.com
Source
rat striatum synaptosomes
Tracer
[ 3 H]DA (0.2 µCi/ml)
Measured product [ 3 H]DA incorporation into synaptosomes
Detection method scintillation counting
Reference GBR 12909 (IC 50 : 3 nM)
Janowsky, A. et al. (1986) J. Neurochem., 46: 1272-1276.
GABA transporter - antagonist radioligand
binding
Ref. 0060
Q 3 weeks
Included in:
Diversity profile
BioPrint ® profile
Organ safety profile
Source
❚ norepinephrine
rat cerebral cortex
Ligand
[ 3 H]GABA (10 nM) (+ 10 µM isoguvacine)
(+ 10 µM baclofen)
Kd 4.6 µM
Non specific GABA (1 mM)
Reference nipecotic acid (IC 50 : 4.9 µM)
Shank, R.P. et al. (1990) J. Neurochem., 54: 2007-2015.
DA uptake (% of control)
100
50
0
-11 -10 -9 -8 -7 -6
log [drug] (M)
BTCP
GBR 12909
nomifensine
dopamine
GBR 12909
❚ See other dopamine assays, page 32
specific binding (% of control)
100
50
0
-9 -8 -7 -6 -5 -4
log [drug] (M)
nipecotic acid
GABA
muscimol
baclofen
❚ See other gaba assays, pp. 38, 84, and 97
norepinephrine transporter - antagonist radioligand
binding
Ref. 0355
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]nisoxetine (1 nM)
2.9 nM
desipramine (1 µM)
protriptyline (IC 50 : 5.4 nM)
Pacholczyk, T. et al. (1991) Nature, 350: 350-354.
specific binding (% of control)
100
50
0
-11 - 10 -9 -8 -7 -6 -5
log [drug] (M)
protriptyline
desipramine
imipramine
GBR 12909
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Assay developed in 2010 New assay conditions Human Q Standard turnaround time

105
norepinephrine ❚
norepinephrine uptake
Source
rat hypothalamus synaptosomes
Tracer
[ 3 H]NE (0.2 µCi/ml)
Measured product [ 3 H]NE incorporation into synaptosomes
Detection method scintillation counting
NE uptake (% of control)
100
50
Cerep
services
cellul ar
Ref. 0393
Q 3 weeks
Reference protriptyline (IC 50 : 1.5 nM)
Perovic, S. and Muller, W.E.G. (1995) Arzneim-Forsch. Drug Res., 45: 1145-1148.
0
-11 -10 -9 -8 -7 -6
log [drug] (M)
protryptiline
Receptors
❚ serotonin
Ion
channels
5-HT transporter - antagonist radioligand
binding
Ref. 0439
Q 3 weeks
Included in:
ExpresS Profile
High-throughput profile
Diversity profile
BioPrint ® profile
Organ safety profile
5-HT uptake
cellul ar
Ref. 0392
Q 3 weeks
Source
Ligand
Kd
Non specific
Reference
human recombinant (CHO cells)
[ 3 H]imipramine (2 nM)
1.7 nM
imipramine (10 µM)
imipramine (IC 50 : 2.1 nM)
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
Tatsumi, M. et al. (1999) Eur. J. Pharmacol., 368: 277-283.
[Custom offer] rat brain model (Ref. 0145), please contact us at [CUSTOM OFFER]
Source
rat brain synaptosomes
Tracer
[ 3 H]5-HT (0.2 µCi/ml)
Measured product [ 3 H]5-HT incorporation into synaptosomes
Detection method scintillation counting
imipramine
serotonin
zimelidine
citalopram
Reference imipramine (IC 50 : 30 nM)
Perovic, S. and Muller, W.E.G. (1995) Arzneim-Forsch. Drug Res., 45: 1145-1148.
❚ See other serotonin assays, pp. 68, 90, and 101
Transporters
Kinases
Epigenetic &
DNA-related
enzymes
Other
enzymes
Specialized
cellular
assays
Standard
profiles
Testing
conditions
Ordering
information
Assay list
& index

106 in vitro pharmacology 2011 catalog
❚ notes
❚ see also ADME-Tox & PK 2011 catalog
ADME-Tox & PK
2011 CATALOG
IN VITRO ADME
Solution properties
Drug absorption/drug transport
Drug metabolism
Drug-drug interactions
IN VITRO TOXICITY
Cardiac toxicity
Cytotoxicity
Genetic toxicity
IN VIVO PK/BIOANALYTICAL
In vivo PK
Bioanalytical
ASSAY SELECTION GUIDE
STANDARD PROFILES
APPLICATION NOTES

107
Cerep
services
Kinases
Receptors
Cerep’s panel of kinases has increased from 205 biochemical assays as of January,1, 2009 to 271 (including 16 cellular kinase assays)
as of January 1, 2011 allowing to provide a wider coverage of all major families in the human kinome (Manning G. et al. (2002)
Science, 298: 1912-1934).
Kinases sub-families 1 P.
Protein-tyrosine kinases 108
RTK Receptor Tyrosine Kinases 108
CTK Cytoplasmic Tyrosine Kinases 118
Protein-serine/threonine kinases 124
CMGC Cyclin-dependent-(CDK), Mitogen-activated-(MAPK), Glycogen-synthase-(GSK) and CDK-like kinases 124
CaMK Ca 2+ /calmodulin-dependent protein kinases 130
AGC protein kinases A, G and C cyclic nucleotide regulated and phospholipid-regulated kinases and ribosomal S6 kinases 137
CK1 Casein Kinases 1 144
STE homologs of yeast sterile kinases 144
TKL Tyrosine Kinase-Like 149
other kinases 151
atypical kinases 156
1 Cohen P. (2002), Nature Reviews/Drug Discovery, 1: 309-315
Cerep kinase assays
Ion
channels
Transporters
Kinases
Epigenetic &
DNA-related
enzymes
❚ Biochemical kinase assays
Majority of our biochemical kinase assays use activated kinases. They are usually full length kinase or cytoplasmic domain of RTK. Assays
are designed to be as close as possible to ATP and substrate Km.
The technology used to measure substrate phosphorylation is TR-FRET (HTRF ® or LANCE ® ). A few assays are cascade of activation.
NOTE: A majority of our kinase assays have been converted from HTRF ® to LANCEUltra ® technology. Both technologies are TR-FRET
with the difference in europium labelling: europium cryptate for HTRF ® and europium chelate for LANCEUltra ® .
Assays are converted following a standard procedure consisting of Time course experiment, Km determination and pharmacology
characterization of the enzyme by inhibiting its activity with known inhibitors. IC 50 values obtained for known inhibitors are compared
to literature and to those obtained using HTRF ® technology. If all values are in agreement with the previous ones, LANCE ® technology
is validated for the kinase of interest. This conversion allows us to standardize and automate our kinase assays providing shorter
turnaround times for both profiling and screening experiments.
❚ cellular Kinase assays
In order to complement our existing biochemical assay platform, we have implemented cellular kinase assays. These assays allow to
confirm inhibitors activity in a relevant cellular background and profile their selectivity against multiple signaling pathways.
- Cellular kinase phosphorylation assays
Cellular kinase phosphorylation assays are developed using AlphaScreen ® Surefire ® assay kits. The assays are optimized for directly
measuring kinase activation following treatment of cells with activators of signaling pathways.
- Cellular tyrosine kinase receptor activity assays
We have demonstrated that the impedance-based technology can be used to monitor the activity of the main tyrosine kinase receptor
families. These label-free assays allow the identification of inhibitors targeting either the ligand binding domain or the kinase domain.
These assays can be developed in virtually any cancer cell lines or primary cells. As an example, we have developed and validated
the EGFR cellular assay in the following cancer cell lines: A431, HELA and MDA-MB-231.
❚ binding Kinase assays
To expand our existing kinase services, we offer binding kinase assays to identify type II inhibitors on unphosphorylated kinases, to
compare compounds activity on unphosphorylated and phophorylated kinases and to discriminate between ATP and non-ATP competitive
inhibitors. In addition, we are now using ADP readout to develop kinase assays on intractable substrates (for which no antibody exist)
which allows us to profile kinase activity on different natural substrates in order to identify substrate selective inhibitors. These assays are
displayed as part of our custom research.
For further information, please contact us at customresearch@cerep.com.
Other
enzymes
Specialized
cellular
assays
Standard
profiles
Testing
conditions
Ordering
information
Assay list
& index

108 in vitro pharmacology 2011 catalog
❚ Protein-tyrosine kinases [RTK]
ALK
Ref. 2678
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-CKKSRGDYMTMQIG
(150 nM)
Measured product phospho-Ulight-CKKSRGDYMTMQIG
Detection method LANCE
Reference
staurosporine (IC 50 : 6.3 nM)
Motegi, A. et al. (2004) J. Cell. Sci., 117: 3319-3329.
Axl kinase
Ref. 3062
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-TK peptide
(100 nM)
Measured product phospho-Ulight-TK peptide
Detection method LANCE
Reference
staurosporine (IC 50 : 2.9 nM)
O'Bryan, J.P. et al. (1991) Mol. Cell. Biol., 11: 5016-5031.
c-kit kinase
Ref. 3070
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-TK peptide
(100 nM)
Measured product phospho-Ulight-TK peptide
Detection method LANCE
Reference
staurosporine (IC 50 : 1.2 nM)
Blume-Jensen, P. et al. (1995) J. Biol. Chem., 270: 14192-14200.
c-Met kinase
Ref. 2867
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate
ATP + Ulight-CAGAGAIETDKEYYTVKD
(25 nM)
Measured product phospho-Ulight-CAGAGAIETDKEYYTVKD
Detection method LANCE
Reference
staurosporine (IC 50 : 180 nM)
Bardelli, A. et al. (1998) Proc. Natl. Acad. Sci. U S A., 95: 14379-14383.
c-Met kinase (HGFR)
cellul ar
Ref. 3179
Ref. 3180
Q 3 weeks
Activator effect
Inhibitor effect
Source
MDA-MB-231 cells
Measured product impedance
Detection method cellular dielectric spectroscopy
Activator effect Control HGF (3 nM)
Reference HGF (EC 50 : 0.39 nM)
Inhibitor effect Stimulant HGF (1 nM)
Reference PHA665752 (IC 50 : 75 nM)
Puri, N. et al. (2007) Cancer Res., 67: 3529-3534
[Solvent] must be kept 0.1%
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Assay developed in 2010 New assay conditions and/or assay converted from HTRF ® to LANCEUltra ®
Human Q Standard turnaround time

109
DDR2 kinase
Ref. 2783
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-Poly GAT[EAY(1:1:1)]n
(50 nM)
Measured product phospho-Ulight-Poly GAT[EAY(1:1:1)]n
Detection method LANCE
Reference
staurosporine (IC 50 : 3.1 nM)
Vogel, W. (1999) FASEB J., 13: S77-82.
protein-tyrosine kinases [Rtk] ❚
Cerep
services
Receptors
EGFR kinase
Ref. 2865
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate
ATP + Ulight-CAGAGAIETDKEYYTVKD
(100 nM)
Measured product phospho-Ulight-CAGAGAIETDKEYYTVKD
Detection method LANCE
Reference
PD153035 (IC 50 : 0.21 nM)
Weber, W. et al. (1984) J. Biol. Chem., 259: 14631-14636.
Ion
channels
Transporters
EGFR kinase (A431 cells) - AlphaScreen
cellul ar
Ref. 3100
Ref. 3105
Q 3 weeks
Activator effect
Inhibitor effect
Source
A431 cells
Measured product phosphorylation
Detection method AlphaScreen
Activator effect Control EGF (1 µM)
Reference EGF (EC 50 : 17.2 nM)
Inhibitor effect Stimulant EGF (300 nM)
Reference AG1478 (IC 50 : 3.1 nM)
Zhang, Y.G. et al.(2008) Int. J. Oncol., 33: 595-602.
EGFR kinase (A431 cells) - impedance
cellul ar
Ref. 3210
Ref. 3215
Q 3 weeks
Activator effect
Inhibitor effect
EGFR kinase (Hela cells)
cellul ar
Ref. 3209
Ref. 3212
Q 3 weeks
Activator effect
Inhibitor effect
Source
A431 cells
Measured product impedance
Detection method cellular dielectric spectroscopy
Activator effect Control EGF (100 nM)
Reference EGF (EC 50 : 0.3 nM)
Inhibitor effect Stimulant EGF (3 nM)
Reference AG1478 (IC 50 : 124 nM)
Kondratov, K.A. et al.(2009) Cell. Biol. Int., 34: 81-87.
Source
EGFR kinase (MDA-MB-231 cells)
cellul ar
Ref. 3211
Ref. 3214
Q 3 weeks
Activator effect
Inhibitor effect
Hela cells
Measured product impedance
Detection method cellular dielectric spectroscopy
Activator effect Control EGF (1 nM)
Reference EGF (EC 50 : 0.033 nM)
Inhibitor effect Stimulant EGF (0.1 nM)
Reference AG1478 (IC 50 : 21 nM)
Abulrob, A. et al. (2010) J. Biol. Chem., 285: 3145-3156.
Source
MDA-MB-231 cells
Measured product impedance
Detection method cellular dielectric spectroscopy
Activator effect Control EGF (10 nM)
Reference EGF (EC 50 : 0.16 nM)
Inhibitor effect Stimulant EGF (1 nM)
Reference AG1478 (IC 50 : 47 nM)
Amorino, G.P., et al. (2002) Mol. Biol. Cell., 13: 2233-2344
[Solvent] must be kept 0.3%
[Solvent] must be kept 0.3%
[Solvent] must be kept 0.1%
[Solvent] must be kept 0.1%
Kinases
Epigenetic &
DNA-related
enzymes
Other
enzymes
Specialized
cellular
assays
Standard
profiles
Testing
conditions
Ordering
information
Assay list
& index

110 in vitro pharmacology 2011 catalog
❚ protein-tyrosine kinases [Rtk]
EphA1 kinase
Source
human recombinant (insect cells)
Substrate
ATP + biotinyl-bAbAbAAEEEIYEEIEAKKK
(100 nM)
Ref. 1873
Measured product phospho-biotinyl-bAbAbAAEEEIYEEIEAKKK
Detection method HTRF
Q 3 weeks
Included in:
Reference
staurosporine (IC 50 : 140 nM)
Comprehensive kinase profile Coulthard, M.G. et al. (2001) Growth Factors, 18: 303-317.
enzyme activity (% of control)
100
50
0
-9 -8 -7 -6 -5 -4
log [drug] (M)
staurosporine
PP1
PP2
PD153035
EphA2 kinase
Ref. 3055
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Comprehensive kinase profile
Source
human recombinant
Substrate
Measured product
Detection method
Reference
-11
-10 -9 -8 -7 -6 -5 -4 -3
-9 -8 -7 -6 -5 -4
-10
ATP + Ulight-TK peptide
(50 nM)
phospho-Ulight-TK peptide
LANCE
staurosporine (IC 50 : 150 nM)
Kinch, M.S. et al. (2003) Clin. Cancer Res., 9: 613-618.
-10 -9 -8 -7 -6 -5 -4 -3
-8 -7 -6 -5 -4
-10 -9 -8 -7 -6 -5
-10 -9 -8 -7 -6 -5 -4
EphA3 kinase
Ref. 3066
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-TK peptide
(50 nM)
Measured product phospho-Ulight-TK peptide
Detection method LANCE
Reference
staurosporine (IC 50 : 57.5 nM)
Sharfe, N. et al. (2003) J. Immunol., 170: 6024-6032.
EphA4 kinase
Ref. 1702
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate
ATP + biotinyl-βAβAβAAEEEIYEEIEAKKK
(400 nM)
Measured product phospho-biotinyl-βAβAβAAEEEIYEEIEAKKK
Detection method HTRF
Reference
staurosporine (IC 50 : 150 nM)
Binns, K.L. et al. (2000) Mol. Cell. Biol., 20: 4791-4805.
EphA5 kinase
Ref. 2640
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-Poly GAT[EAY(1:1:1)]n
(5 nM)
Measured product phospho-Ulight-Poly GAT[EAY(1:1:1)]n
Detection method LANCE
Reference
staurosporine (IC 50 : 60 nM)
Binns, K.L. et al. (2000) Mol. Cell. Biol., 20: 4791-4805.
EphA6 kinase
Ref. 3071
Q 3 weeks
Source
human recombinant
Substrate
ATP + Ulight-TK peptide
(100 nM)
Measured product phospho-Ulight-TK peptide
Detection method LANCE
Reference
staurosporine (IC 50 : 28.3 nM)
Hafner, C. et al. (2004) Clin. Cell., 50: 490-499.

111
protein-tyrosine kinases [Rtk] ❚
EphA7 kinase
Ref. 3058
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-TK peptide
(100 nM)
Measured product phospho-Ulight-TK peptide
Detection method LANCE
Reference
staurosporine (IC 50 : 130 nM)
Hafner, C. et al. (2004) Clin. Chem., 50: 490-499.
Cerep
services
Receptors
EphA8 kinase
Ref. 3072
Q 3 weeks
Source
human recombinant
Substrate
ATP + Ulight-TK peptide
(100 nM)
Measured product phospho-Ulight-TK peptide
Detection method LANCE
Reference
staurosporine (IC 50 : 140 nM)
Park, S. (2003) J. Biochem. Mol. Biol., 36: 288-293.
Ion
channels
Transporters
EphB1 kinase
Ref. 3053
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-TK peptide
(50 nM)
Measured product phospho-Ulight-TK peptide
Detection method LANCE
Reference
staurosporine (IC 50 : 81.3 nM)
Vindis, C. et al. (2003) J. Cell. Biol., 162: 661-671.
Kinases
Epigenetic &
DNA-related
enzymes
EphB2 kinase
Ref. 3054
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-TK peptide
(50 nM)
Measured product phospho-Ulight-TK peptide
Detection method LANCE
Reference
PP2 (IC 50 : 95.7 nM)
Binns, K.L. et al. (2000) Mol. Cell. Biol., 20: 4791-4805.
Other
enzymes
Specialized
cellular
assays
EphB3 kinase
Ref. 2731
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-Poly GAT[EAY(1:1:1)]n
(5 nM)
Measured product phospho-Ulight-Poly GAT[EAY(1:1:1)]n
Detection method LANCE
Reference
PP2 (IC 50 : 400 nM)
Bembenek, M.E. et al. (2003) Assay Drug Dev. Technol., 1: 555-563.
Standard
profiles
Testing
conditions
EphB4 kinase
Ref. 3059
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate
ATP + Ulight-TK peptide
(100 nM)
Measured product phospho-Ulight-TK peptide
Detection method LANCE
Reference
staurosporine (IC 50 : 300 nM)
Sturz, A. et al. (2004) Biochem. Biophys. Res. Commun., 313: 80-88.
Ordering
information
Assay list
& index

112 in vitro pharmacology 2011 catalog
❚ protein-tyrosine kinases [Rtk]
FGFR kinase
cellul ar
Ref. 3173
Ref. 3174
Q 3 weeks
Activator effect
Inhibitor effect
Source
Measured product
Detection method
Balb/c 3T3 cells
impedance
cellular dielectric spectroscopy
Activator effect Control FGFb (5 nM)
Reference FGFb (EC 50 : 0.43 nM)
Inhibitor effect Stimulant FGFb (1 nM)
Reference PD173074 (IC 50 : 78 nM)
Mohammadi, M. et al. (1998) Embo. J., 17: 5896-5904
[Solvent] must be kept 0.1%
FGFR1 kinase
Ref. 2868
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate
ATP + Ulight-CAGAGAIETDKEYYTVKD
(100 nM)
Measured product phospho-Ulight-CAGAGAIETDKEYYTVKD
Detection method LANCE
Reference
staurosporine (IC 50 : 12 nM)
Mohammadi, M. et al. (1997) Science, 276: 955-960.
FGFR2 kinase
Ref. 2893
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-CAGAGAIETDKEYYTVKD
(25 nM)
Measured product phospho-Ulight-CAGAGAIETDKEYYTVKD
Detection method LANCE
Reference
staurosporine (IC 50 : 4.9 nM)
Robertson, S.C. et al. (1998) Proc. Natl. Acad. Sci. U S A., 95: 4567-4572.
FGFR3 kinase
Ref. 2894
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Organ safety profile
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-CAGAGAIETDKEYYTVKD
(100 nM)
Measured product phospho-Ulight-CAGAGAIETDKEYYTVKD
Detection method LANCE
Reference
staurosporine (IC 50 : 11 nM)
Hart, K.C. et al. (2000) Oncogene, 19: 3309-3320.
FGFR4 kinase
Ref. 2895
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate
ATP + Ulight-CAGAGAIETDKEYYTVKD
(100 nM)
Measured product phospho-Ulight-CAGAGAIETDKEYYTVKD
Detection method LANCE
Reference
staurosporine (IC 50 : 180 nM)
Hart, K.C. et al. (2000) Oncogene, 19: 3309-3320.
FLT-1 kinase (VEGFR1)
Ref. 3068
Q 3 weeks
Included in:
BioPrint ® profile
Comprehensive kinase profile
Source
Substrate
Measured product
Detection method
Reference
human recombinant (Sf9 cells)
ATP + Ulight-TK peptide
(100 nM)
phospho-Ulight-TK peptide
LANCE
staurosporine (IC 50 : 10 nM)
Itokawa, T. et al. (2002) Mol. Cancer. Ther., 1: 295-302.

113
FLT-3 kinase
Ref. 2866
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate
ATP + Ulight-CAGAGAIETDKEYYTVKD
(100 nM)
Measured product phospho-Ulight-CAGAGAIETDKEYYTVKD
Detection method LANCE
Reference
staurosporine (IC 50 : 0.67 nM)
Dosil, M. et al. (1993) Mol. Cell. Biol., 13: 6572-6585.
protein-tyrosine kinases [Rtk] ❚
Cerep
services
Receptors
FLT-3 D835Y kinase
Source
human recombinant (insect cells)
Substrate
ATP + Ulight-TK peptide (50 nM)
Measured product phospho-Ulight-TK-peptide
Detection method LANCE
Ref. 3208
Reference
staurosporine (IC 50 : 0.7 nM)
Q 3 weeks
Zhang, W. et al.(2008) J. Natl. Cancer Inst., 100: 184-198.
FLT-4 kinase (VEGFR3)
Source
human recombinant
Substrate
ATP + Ulight-CAGAGAIETDKEYYTVKD
(100 nM)
Measured product phospho-Ulight-CAGAGAIETDKEYYTVKD
Ref. 2896
Detection method LANCE
Q 3 weeks
Included in:
Reference
staurosporine (IC 50 : 2.3 nM)
Comprehensive kinase profile Kirkin, V. et al. (2001) Eur. J. Biochem., 268: 5530-5540.
Ion
channels
Transporters
Kinases
Epigenetic &
DNA-related
enzymes
Fms/CSFR kinase
Ref. 3069
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-TK peptide
(100 nM)
Measured product phospho-Ulight-TK peptide
Detection method LANCE
Reference
staurosporine (IC 50 : 0.95 nM)
Carlberg, K. and Rohrschneider, L. (1994) Mol. Cell. Biol., 5: 81-95.
Other
enzymes
Specialized
cellular
assays
HER2/ErbB2 kinase
Ref. 1598
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate
ATP + biotinyl-bAbAbAAEEEEYFELVAKKK
(600 nM)
Measured product phospho-biotinyl-bAbAbAAEEEEYFELVAKKK
Detection method HTRF
Reference
PD153035 (IC 50 : 1.8 µM)
Qian, X. et al. (1992) Proc. Natl. Acad. Sci. USA, 89: 1330-1334.
Standard
profiles
Testing
conditions
HER4/ErbB4 kinase
Ref. 1875
Q 3 weeks
Source
human recombinant (insect cells)
Substrate
ATP + biotinyl-bAbAbAAEEEEYFELVAKKK
(25 nM)
Measured product phospho-biotinyl-bAbAbAAEEEEYFELVAKKK
Detection method HTRF
Reference
PD153035 (IC 50 : 300 nM)
Plowman, G.D. et al. (1993) Proc. Natl. Acad. Sci. USA, 90: 1746-1750.
enzyme activity (% of control)
100
50
0
-9 -8 -7 -6 -5 -4
log [drug] (M)
PD153035
staurosporine
Ordering
information
Assay list
& index
-11
-10 -9 -8 -7 -6 -5 -4
-3
-10
-9 -8 -7 -6 -5 -4
-3
-9 -8 -7 -6 -5 -4 -8 -7 -6 -5 -4

114 in vitro pharmacology 2011 catalog
❚ protein-tyrosine kinases [Rtk]
IGF1R kinase
Ref. 3061
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
Substrate
Measured product
Detection method
Reference
human recombinant
ATP + Ulight-TK peptide
(50 nM)
phospho-Ulight-TK peptide
LANCE
staurosporine (IC 50 : 85.8 nM)
Wang, Y. et al. (2004) J. Exp. Ther. Oncol., 4: 111-119.
IGF1Rb kinase
cellul ar
Ref. 3109 Activator effect
Ref. 3111 Inhibitor effect
Q 3 weeks
Source
Measured product
Detection method
A431 cells
phosphorylation
AlphaScreen
Activator effect Control IGF1 (30 nM)
Reference IGF1 (EC 50 : 1.6 nM)
Inhibitor effect Stimulant IGF1 (5 nM)
Reference unavailable
Pappano, W.N. et al.(2009) BMC Cancer., 9: 314.
[Solvent] must be kept 0.1%
IRK (InsR)
Ref. 2898
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
BioPrint ® profile
Organ safety profile
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-Poly GAT[EAY(1:1:1)]n
(50 nM)
Measured product phospho-Ulight-Poly GAT[EAY(1:1:1)]n
Detection method LANCE
Reference
staurosporine (IC 50 : 38.5 nM)
Al-Hasani, H. et al. (1994) FEBS Lett., 349: 17-22.
IRK (InsRb)
cellul ar
Ref. 3110 Activator effect
Ref. 3112 Inhibitor effect
Q 3 weeks
Source
Measured product
Detection method
HepG2 cells (endogenous)
phosphorylation
AlphaScreen
Activator effect Control insulin (100 nM)
Reference insulin (EC 50 : 0.33 nM)
Inhibitor effect Stimulant insulin (3 nM)
Reference AG538 (IC 50 : 2.4 µM)
Duronio, V. (1990) Biochem. J., 270: 27-32
[Solvent] must be kept 0.1%
IRR kinase
Ref. 3073
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-TK peptide
(100 nM)
Measured product phospho-Ulight-TK peptide
Detection method LANCE
Reference
staurosporine (IC 50 : 25 nM)
Zhang, B. and Roth, R.A. (1992) J. Biol. Chem., 267: 18320-18328.
❚ Assays converted from HTRF ® to LANCEUltra ® technology
A majority of our kinase assays have been converted from HTRF ® to LANCEUltra ® technology. Both technologies
are
TR-FRET
with the
difference in europium labelling: europium cryptate for HTRF ® and europium chelate for LANCEUltra ® .
Assays are converted following a standard procedure consisting of time course experiment, Km determination and pharmacology
characterization of the enzyme by inhibiting its activity with known inhibitors. IC 50 values obtained for known inhibitors are compared
to literature and to those obtained using HTRF ® technology. If all values are in agreement with the previous ones, LANCE ® technology is
validated for the kinase of interest.
This conversion allows us to standardize and automate our kinase assays providing shorter turnaround times
for
both
profiling
and
screening
experiments.

115
KDR kinase (VEGFR2)
Ref. 2864
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Comprehensive kinase profile
Source
human recombinant (Sf9 cells)
Substrate
ATP + Ulight-CAGAGAIETDKEYYTVKD
(100 nM)
Measured product phospho-Ulight-CAGAGAIETDKEYYTVKD
Detection method LANCE
Reference
staurosporine (IC 50 : 3 nM)
Itokawa, T. et al. (2002) Mol. Cancer Ther., 1: 295-302.
protein-tyrosine kinases [Rtk] ❚
Cerep
services
Receptors
LTK
Ref. 2642
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
Substrate
Measured product
Detection method
Reference
human recombinant
ATP + Ulight-Poly GAT[EAY(1:1:1)]n
(5 nM)
phospho-Ulight-Poly GAT[EAY(1:1:1)]n
LANCE
staurosporine (IC 50 : 5.3 nM)
Ueno, H. et al. (1996) J. Biol. Chem., 271: 27707-27714.
Ion
channels
Transporters
Mer kinase
Ref. 3075
Q 3 weeks
Source
Substrate
Measured product
Detection method
Reference
human recombinant
ATP + Ulight-TK peptide
(50 nM)
phospho-Ulight-TK peptide
LANCE
staurosporine (IC 50 : 2.4 nM)
Camenisch, T.D. et al. (1999) J. Immunol., 162: 3498-3503.
Kinases
Epigenetic &
DNA-related
enzymes
MusK
Ref. 2899
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
Substrate
Measured product
Detection method
Reference
human recombinant (Sf9 cells)
ATP + Ulight-CAGAGAIETDKEYYTVKD
(100 nM)
phospho-Ulight-CAGAGAIETDKEYYTVKD
LANCE
staurosporine (IC 50 : 2.4 nM)
Watty, A. and Burden, S.J. (2002) J. Biol. Chem., 277: 50457-50462.
Other
enzymes
Specialized
cellular
assays
PDGFR
cellul ar
Ref. 3156 Activator effect
Ref. 3160 Inhibitor effect
Q 3 weeks
Source
Measured product
Detection method
Balb/c 3T3 cells
impedance
cellular dielectric spectroscopy
Activator effect Control PDGF-BB (3 nM)
Reference PDGF-BB (EC 50 : 0.044 nM)
Inhibitor effect Stimulant PDGF-BB (0.1 nM)
Reference PDGF inhib. IV (IC 50 : 282 nM)
Maldonado, P.E. et al. (1988) J. Membr. Biol., 106: 203-210
[Solvent] must be kept 0.1%
Standard
profiles
Testing
conditions
PDGFRa kinase
Ref. 3064
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
Substrate
Measured product
Detection method
Reference
human recombinant
ATP + Ulight-TK peptide
(100 nM)
phospho-Ulight-TK peptide
LANCE
staurosporine (IC 50 : 0.38 nM)
Songyang, Z. et al. (1995) Nature, 373: 536-539.
Ordering
information
Assay list
& index

116 in vitro pharmacology 2011 catalog
❚ protein-tyrosine kinases [Rtk]
PDGFRb kinase
Ref. 2900
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate
ATP + Ulight-Poly GAT[EAY(1:1:1)]n
(25 nM)
Measured product phospho-Ulight-Poly GAT[EAY(1:1:1)]n
Detection method LANCE
Reference
staurosporine (IC 50 : 1 nM)
Baxter, R.M. et al. (1998) J. Biol. Chem., 273: 17050-17055.
Ret kinase
Ref. 1593
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate
ATP + biotinyl-bAbAbAAEEEEYFELVAKKK
(100 nM)
Measured product phospho-biotinyl-bAbAbAAEEEEYFELVAKKK
Detection method HTRF
Reference
staurosporine (IC 50 : 8 nM)
Borrello, M.G. et al. (1996) Mol. Cell. Biol., 16: 2151-2163.
-9 -8 -7 -6 -5 -4
enzyme activity (% of control)
100
50
staurosporine
SU4312
SU4984
0
PD153035
-10 -9 -8 -7 -6 -5 -4
-11
log [drug] (M)
Ron kinase
Ref. 3067
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-TK peptide
(20 nM)
Measured product phospho-Ulight-TK peptide
Detection method LANCE
Reference
staurosporine (IC 50 : 470 nM)
Santoro, M.M. et al. (1998) Oncogene, 17: 741-749.
-10 -9 -8 -7 -6 -5 -4
-8 -7 -6 -5 -9 -4
-9 -8 -7 -6 -5 -4
-8 -7 -6 -5 -4
-11 -10 -9 -8 -7 -6 -5 -4
PD153035
staurosporine
AG1478
AG825
Ros kinase
Ref. 1594
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (Sf21 cells)
Substrate
ATP + biotinyl-bAbAbAAAEEEYMMMFAKKK
(75 nM)
Measured product phospho-biotinyl-bAbAbAAAEEEYMMFAKKK
Detection method HTRF
Reference
staurosporine (IC 50 : 7.6 nM)
Birchmeier C. et al. (1990) Proc. Natl. Acad. Sci. USA, 87: 4799-4803.
-9 -8 -7 -6 -5 -4
enzyme activity (% of control)
100
50
staurosporine
PD153035
0
K252a
-9 -8 -7 -6 -5 -4
-10
log [drug] (M)
-11 -10 -9 -8 -7 -6 -5 -4
TIE2 kinase
Ref. 2736
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-Poly GT [EY(4:1)]n
(50 nM)
Measured product phospho-Ulight-Poly GT [EY(4:1)]n
Detection method LANCE
Reference
staurosporine (IC 50 : 260 nM)
Deng, S-J. et al. (2001) Comb. Chem. High Throughput Screen., 4: 525-533.
-10 -9 -8 -7 -6 -5 -4
-9 -8 -7 -6 -5 -4
-4
-9 -8 -7 -6 -5
-8 -7 -6 -5 -4
-11 -10 -9 -8 -7 -6 -5 -4
PD153035
staurosporine
AG1478
AG825
TRKA
Ref. 2901
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate
ATP + Ulight-Poly GAT[EAY(1:1:1)]n
(5 nM)
Measured product phospho-Ulight-Poly GAT[EAY(1:1:1)]n
Detection method LANCE
Reference
staurosporine (IC 50 : 5.5 nM)
Angeles, T.S. et al. (1998) Arch. Biochem. Biophys., 349: 267-274.

117
TRKB
Ref. 2902
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-Poly GAT[EAY(1:1:1)]n
(5 nM)
Measured product phospho-Ulight-Poly GAT[EAY(1:1:1)]n
Detection method LANCE
Reference
staurosporine (IC 50 : 3.3 nM)
Middlemas, D.S. et al. (1994) J. Biol. Chem., 269: 5458-5466.
protein-tyrosine kinases [Rtk] ❚
Cerep
services
Receptors
TRKC
Ref. 3080
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-TK peptide
(50 nM)
Measured product phospho-Ulight-TK peptide
Detection method LANCE
Reference
staurosporine (IC 50 : 1.7 nM)
Robinson, L.L. et al. (2003) J. Clin. Endocrinol. Metab., 88: 3943-3951.
Ion
channels
Transporters
Tyro3/Sky kinase
Ref. 3081
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-TK peptide
(50 nM)
Measured product phospho-Ulight-TK peptide
Detection method LANCE
Reference
staurosporine (IC 50 : 6.1 nM)
Lan, Z. et al. (2000) Blood, 95: 633-638.
Kinases
Epigenetic &
DNA-related
enzymes
VEGFR kinase
cellul ar
Ref. 2696 Activator effect
Ref. 2697 Inhibitor effect
Q 3 weeks
Source
HUV-EC-C cells
Measured product impedance
Detection method cellular dielectric spectroscopy
Activator effect Control VEGF (1 nM)
Reference VEGF (EC 50 : 0.029 nM)
Inhibitor effect Stimulant VEGF (0.1 nM)
Reference VEGF receptor tyrosine kinase
inhibitor II (IC 50 : 168 nM)
Furet, P. et al. (2003) Bioorg. Med. Chem. Lett., 13: 2967-2971.
[Solvent] must be kept 0.1%
Other
enzymes
Specialized
cellular
assays
selected cerep assays
❚ Biochemical kinase assays
Kinase assays are enzymatic assays mostly using activated kinases. Those are usually full length kinase or cytoplasmic domain of RTK.
Assays are designed to be as close as possible to ATP and substrate Km.
The technology used to measure substrate phosphorylation is TR-FRET (HTRF ® or LANCE ® ). A few assays are cascade of activation.
❚ Cellular kinase assays
In order to complement our existing biochemical assay platform, we have implemented cellular kinase assays. These assays allow to
confirm inhibitors activity in a relevant cellular background and profile their selectivity against multiple signaling pathways.
- Cellular kinase phosphorylation assays
Cellular kinase phosphorylation assays are developed using AlphaScreen ® Surefire ® assay kits. The assays are optimized for directly
measuring kinase activation following treatment of cells with activators of signaling pathways.
- Cellular tyrosine kinase receptor activity assays
We have demonstrated that the impedance-based technology can be used to monitor the activity of the main tyrosine kinase receptor
families. These label-free assays allow the identification of inhibitors targeting either the ligand binding domain or the kinase domain.
These assays can be developed in virtually any cancer cell lines or primary cells. As an example, we have developed and validated
the EGFR cellular assay in the following cancer cell lines: A431, HELA and MDA-MB-231.
❚ Binding kinase assays
See page 107.
Standard
profiles
Testing
conditions
Ordering
information
Assay list
& index

118 in vitro pharmacology 2011 catalog
❚ Protein-tyrosine kinases [CTK]
Abl kinase
Ref. 3056
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
BioPrint ® profile
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate
ATP + Ulight-TK peptide
(100 nM)
Measured product phospho-Ulight-TK peptide
Detection method LANCE
Reference
staurosporine (IC 50 : 101 nM)
Park, Y.M. et al. (1999) Anal. Biochem., 269: 94-104.
Ack
Ref. 3052
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-TK peptide
(100 nM)
Measured product phospho-Ulight-TK peptide
Detection method LANCE
Reference
staurosporine (IC 50 : 2.6 nM)
Mahajan, N.P. et al. (2005) Cancer. Res., 65: 10514-10523.
Arg kinase
Ref. 3057
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-TK peptide
(100 nM)
Measured product phospho-Ulight-TK peptide
Detection method LANCE
Reference
staurosporine (IC 50 : 60.8 nM)
De Keersmaecker, K. and Cools, J. (2006) Leukemia, 20: 200-205.
BLK
Ref. 1697
Q 3 weeks
Source
human recombinant (insect cells)
Substrate
ATP + biotinyl-bAbAbAAEEEIYEEIEAKKK
(300 nM)
Measured product phospho-biotinyl-bAbAbAAEEEIYEEIEAKKK
Detection method HTRF
Reference
staurosporine (IC 50 : 5.4 nM)
Saouaf, S.J. et al. (1995) J. Biol. Chem., 270: 27072-27078.
BMX (Etk) kinase
Ref. 1587
Q 3 weeks
Source
human recombinant (insect cells)
Substrate
ATP + biotinyl-bAbAbAEEEPQYEEIPIYLELLP
(400 nM)
Measured product phospho-biotinyl-bAbAbAEEEPQYEEIPIYLELLP
Detection method HTRF
Reference
staurosporine (IC 50 : 93 nM)
Jiang, T. et al. (2004) J. Biol.Chem., 279: 50181-50189.
enzyme activity (% of control)
100
50
0
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
staurosporine
PP1
AG538
AG1112
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Assay developed in 2010 New assay conditions and/or assay converted from HTRF ® to LANCEUltra ®
Human Q Standard turnaround time

119
protein-tyrosine kinases [Ctk] ❚
Brk
Ref. 3063
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate
ATP + Ulight-TK peptide
(100 nM)
Measured product phospho-Ulight-TK peptide
Detection method LANCE
Reference
PP1 (IC 50 : 35 nM)
Qiu, H. and Miller, W.T. (2002) J. Biol. Chem., 277: 34634-34641.
Cerep
services
Receptors
BTK
Ref. 1589
Q 3 weeks
CSK
Ref. 1524
Q 3 weeks
Included in:
Organ safety profile
Source
human recombinant (insect cells)
Substrate
ATP + biotinyl-bAbAbAEEEPQYEEIPIYLELLP
(1.8 µM)
Measured product phospho-biotinyl-bAbAbAEEEPQYEEIPIYLELLP
Detection method HTRF
Reference
staurosporine (IC 50 : 50 nM)
Mahajan, S. et al. (2001) J. Biol. Chem., 276: 31216-31228.
-9 -8 -7 -6 -5 -4
Source
human recombinant (E. coli)
Substrate
ATP + biotinyl-bAbAbAEEEPQYEEIPIYLELLP
(40 nM)
Measured product phospho-biotinyl-bAbAbAEEEPQYEEIPIYLELLP
Detection method HTRF
Reference
staurosporine (IC 50 : 96 nM)
Ruzzene, M. et al. (1997) Eur. J. Biochem., 246: 433-439.
enzyme activity (% of control)
enzyme activity (% of control)
100
50
staurosporine
PP1
AG538
0
AG1112
-8 -7 -5 -10 -9 -6 -4
log [drug] (M)
-8 -7 -6 -5 -4
-9
100
-9 -8 -7 -6 -5 -4
-8 -7 -6 -5 -4
50
-10 -9 -8 -7 -6 -5 -4
staurosporine
PP1
PP2
0
AG1112
-9 -8 -7 -6 -5 -4
log [drug] (M)
Ion
channels
Transporters
Kinases
Epigenetic &
DNA-related
enzymes
CTK
Ref. 2638
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-Poly GAT[EAY(1:1:1)]n
(5 nM)
Measured product phospho-Ulight-Poly GAT[EAY(1:1:1)]n
Detection method LANCE
Reference
staurosporine (IC 50 : 593 nM)
Wood, A. et al. (2007) Mol. Cell. Biol., 27: 709-720.
Other
enzymes
Specialized
cellular
assays
FAK
Ref. 3065
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (Sf9 cells)
Substrate
ATP + Ulight-TK peptide
(100 nM)
Measured product phospho-Ulight-TK peptide
Detection method LANCE
Reference
staurosporine (IC 50 : 27 nM)
McLean, G.W. et al. (2000) J. Biol. Chem., 275: 23333-23339.
Standard
profiles
Testing
conditions
Fer kinase
Ref. 2641
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-Poly GAT[EAY(1:1:1)]n
(5 nM)
Measured product phospho-Ulight-Poly GAT[EAY(1:1:1)]n
Detection method LANCE
Reference
staurosporine (IC 50 : 4.1 nM)
Kim, L. and Wong T.W. (1998) J. Biol. Chem., 273: 23542-23548.
Ordering
information
Assay list
& index

120 in vitro pharmacology 2011 catalog
❚ protein-tyrosine kinases [Ctk]
Fes kinase
Ref. 1519
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate
ATP + biotinyl-βAβAβAAEEEIYEEIEAKKK
(100 nM)
Measured product phospho-biotinylβAβAβAAEEEIYEEIEAKKK
Detection method HTRF
Reference
staurosporine (IC 50 : 20 nM)
Songyang, Z. et al. (1995) Nature, 373: 536-539.
enzyme activity (% of control)
100
50
0
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
staurosporine
PP1
AG538
AG1112
Fgr kinase
Ref. 3060
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-TK peptide
(50 nM)
Measured product phospho-Ulight-TK peptide
Detection method LANCE
Reference
staurosporine (IC 50 : 2.8 nM)
Melander, F. et al. (2003) Biochem. J., 370: 687-694.
FRK
Ref. 2784
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-Poly GAT[EAY(1:1:1)]n
(50 nM)
Measured product phospho-Ulight-Poly GAT[EAY(1:1:1)]n
Detection method LANCE
Reference
staurosporine (IC 50 : 22 nM)
Welsh, M. et al. (2004) Biochem. J., 382: 261-268.
Fyn kinase
Ref. 0212
Q 3 weeks
Included in:
BioPrint ® profile
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate
ATP + biotinyl-βAβAβAYQAEENTYDEYEN
(2 µM)
Measured product phospho-biotinyl-βAβAβAYQAEENTYDEYEN
Detection method HTRF
Reference
PP1 (IC 50 : 166 nM)
Dente, L. et al. (1997) J. Mol. Biol., 269: 694-703.
enzyme activity (% of control)
100
50
PP1
staurosporine
piceatannol
0
PP2
-9 -8 -7 -6 -5 -4
-10
log [drug] (M)
HCK
Ref. 1590
Q 3 weeks
Source
human recombinant (insect cells)
Substrate
ATP + biotinyl-βAβAβAAEEEIYEEIEAKKK
(15 nM)
Measured product phospho-biotinyl-βAβAβAAEEEIYEEIEAKKK
Detection method HTRF
Reference
staurosporine (IC 50 : 7.4 nM)
Ziegler, S.F. et al. (1987) Mol. Cell. Biol., 7: 2276-2285.
enzyme activity (% of control)
100
50
0
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
staurosporine
PP1
PP2
piceatannol
ITK
Ref. 3074
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-TK peptide
(100 nM)
Measured product phospho-Ulight-TK peptide
Detection method LANCE
Reference
staurosporine (IC 50 : 17.7 nM)
Readinger, J.A. et al. (2008) Proc. Natl. Acad. Sci. U S A., 105: 6684-6689.

121
JAK1
Ref. 2619
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-CAGAGAIETDKEYYTVKD
(100 nM)
Measured product phospho-Ulight-CAGAGAIETDKEYYTVKD
Detection method LANCE
Reference
staurosporine (IC 50 : 1.6 nM)
Yamaoka, K. et al. (2004) Gen. Biol., 5: 253.
protein-tyrosine kinases [Ctk] ❚
Cerep
services
Receptors
JAK2
Ref. 2869
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (Sf21 cells)
Substrate
ATP + Ulight-CAGAGAIETDKEYYTVKD
(100 nM)
Measured product phospho-Ulight-CAGAGAIETDKEYYTVKD
Detection method LANCE
Reference
staurosporine (IC 50 : 1.5 nM)
Brizzi, M.F. et al. (1996) J. Biol. Chem., 271: 3562-3567.
Ion
channels
Transporters
JAK3
Ref. 2905
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-CAGAGAIETDKEYYTVKD
(100 nM)
Measured product phospho-Ulight-CAGAGAIETDKEYYTVKD
Detection method LANCE
Reference
staurosporine (IC 50 : 0.77 nM)
Zhou, Y.-J. et al. (1997) Proc. Natl. Acad. Sci. U.S.A., 94: 13850-13855.
Kinases
Epigenetic &
DNA-related
enzymes
Lck kinase
Ref. 2906
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate
ATP + Ulight-Poly GAT[EAY(1:1:1)]n
(25 nM)
Measured product phospho-Ulight-Poly GAT[EAY(1:1:1)]n
Detection method LANCE
Reference
staurosporine (IC 50 : 31 nM)
Park, Y.M. et al. (1999) Anal. Biochem., 269: 94-104.
Other
enzymes
Specialized
cellular
assays
Lyn A kinase
Ref. 0669
Q 3 weeks
Included in:
BioPrint ® profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate
ATP +biotinyl-βAβAβAKVEKIGEGTYGVVYK
(400 nM)
Measured product phospho-biotinyl-AβAβAKVEKIGEGTYGVVYK
Detection method HTRF
Reference
staurosporine (IC 50 : 18 nM)
Cheng, H.C. et al. (1992) J. Biol. Chem., 267: 9248-9256.
Standard
profiles
Testing
conditions
Lyn B kinase
Ref. 2201
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate
ATP + His-tagged Rb truncated protein
(70 nM)
Measured product phospho-His-tagged Rb truncated protein
Detection method HTRF
Reference
staurosporine (IC 50 : 11.6 nM)
Yi, T.L. et al. (1991) Mol. Cell. Biol., 11: 2391-2398.
Ordering
information
Assay list
& index

122 in vitro pharmacology 2011 catalog
❚ protein-tyrosine kinases [Ctk]
PYK2
Ref. 3077
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
Substrate
Measured product
Detection method
Reference
human recombinant
ATP + Ulight-TK peptide
(100 nM)
phospho-Ulight-TK peptide
LANCE
staurosporine (IC 50 : 5.1 nM)
Benbernou, N. et al. (2000) J. Biol. Chem., 275: 7060-7065.
Src kinase
Ref. 2907
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate
ATP + Ulight-Poly GAT[EAY(1:1:1)]n
(5 nM)
Measured product phospho-Ulight-Poly GAT[EAY(1:1:1)]n
Detection method LANCE
Reference
staurosporine (IC 50 : 9 nM)
Cheng, H.C. et al. (1992) J. Biol. Chem., 267: 9248-9256.
Srm kinase
Ref. 2646
Q 3 weeks
Source
human recombinant
Substrate
ATP + Ulight-Poly GAT[EAY(1:1:1)]n
(5 nM)
Measured product phospho-Ulight-Poly GAT[EAY(1:1:1)]n
Detection method LANCE
Reference
staurosporine (IC 50 : 625 nM)
Kohmura, N. et al. (1994) Mol. Cell. Biol., 14: 6915-6925.
Syk
Ref. 2780
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-CAGAGAIETDKEYYTVKD
(150 nM)
Measured product phospho-Ulight-CAGAGAIETDKEYYTVKD
Detection method LANCE
Reference
staurosporine (IC 50 : 2.1 nM)
Yamamoto, N. et al. (2003) Anal. Biochem., 315: 256-261.
TEC kinase
Ref. 3076
Q 3 weeks
Source
human recombinant
Substrate
ATP + Ulight-TK peptide
(100 nM)
Measured product phospho-Ulight-TK peptide
Detection method LANCE
Reference
staurosporine (IC 50 : 64 nM)
Lachance, G. et al. (2002) J. Biol. Chem., 277: 21537-21541.
Tnk1
Ref. 2785
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-Poly GAT[EAY(1:1:1)]n
(5 nM)
Measured product phospho-Ulight-Poly GAT[EAY(1:1:1)]n
Detection method LANCE
Reference
staurosporine (IC 50 : 2.1 nM)
Hoehn, G.T. et al. (1996) Oncogene, 12: 903-913.

123
TXK
Ref. 2786
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-Poly GAT[EAY(1:1:1)]n
(50 nM)
Measured product phospho-Ulight-Poly GAT[EAY(1:1:1)]n
Detection method LANCE
Reference
staurosporine (IC 50 : 57 nM)
Kashiwakura, J. et al. (2002) Biol. Pharm. Bull., 25: 718-721.
protein-tyrosine kinases [Ctk] ❚
Cerep
services
Receptors
Tyk2 (JTK1)
Ref. 2621
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-CAGAGAIETDKEYYTVKD
(100 nM)
Measured product phospho-Ulight-CAGAGAIETDKEYYTVKD
Detection method LANCE
Reference
staurosporine (IC 50 : 2.9 nM)
Ide, H. et al. (2008) Biochem. Biophys. Res. Commun., 369: 292-296.
Ion
channels
Transporters
Yes kinase
Ref. 1595
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate
ATP + biotinyl-βAβAβAYQAEENTYDEYEN
(200 nM)
Measured product phosphobiotinyl-βAβAβAYQAEENTYDEYEN
Detection method HTRF
Reference
staurosporine (IC 50 : 13 nM)
Sukegawa J. et al. (1987) Mol. Cell. Biol., 7: 41-47.
enzyme activity (% of control)
100
50
staurosporine
0
piceatannol
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
Kinases
Epigenetic &
DNA-related
enzymes
ZAP70 kinase
Ref. 0705
Q 3 weeks
Included in:
BioPrint ® profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate
ATP + biotinyl-βAβAβADEEEYFIPP
(2 µM)
Measured product phospho-biotinyl-βAβAβADEEEYFIPP
Detection method HTRF
Reference
staurosporine (IC 50 : 48 nM)
Park, Y.M. et al. (1999) Anal. Biochem., 269: 94-104.
Other
enzymes
Specialized
cellular
assays
selected cerep assays
❚ Biochemical kinase assays
Kinase assays are enzymatic assays mostly using activated kinases. Those are usually full length kinase or cytoplasmic domain of RTK.
Assays are designed to be as close as possible to ATP and substrate Km.
The technology used to measure substrate phosphorylation is TR-FRET (HTRF ® or LANCE ® ). A few assays are cascade of activation.
❚ Cellular kinase assays
In order to complement our existing biochemical assay platform, we have implemented cellular kinase assays. These assays allow to
confirm inhibitors activity in a relevant cellular background and profile their selectivity against multiple signaling pathways.
- Cellular kinase phosphorylation assays
Cellular kinase phosphorylation assays are developed using AlphaScreen ® Surefire ® assay kits. The assays are optimized for directly
measuring kinase activation following treatment of cells with activators of signaling pathways.
- Cellular tyrosine kinase receptor activity assays
We have demonstrated that the impedance-based technology can be used to monitor the activity of the main tyrosine kinase receptor
families. These label-free assays allow the identification of inhibitors targeting either the ligand binding domain or the kinase domain.
These assays can be developed in virtually any cancer cell lines or primary cells. As an example, we have developed and validated
the EGFR cellular assay in the following cancer cell lines: A431, HELA and MDA-MB-231.
❚ Binding kinase assays
See page 107.
Standard
profiles
Testing
conditions
Ordering
information
Assay list
& index

124 in vitro pharmacology 2011 catalog
❚ Protein-SERINE/THREONINE kinases [CMGC]
CDC2/CDK1 (cycB)
Ref. 2875
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate
ATP + Ulight-CFFKNIVTPRTPPPSQGK-amide
(100 nM)
Measured product phospho-Ulight-CFFKNIVTPRTPPPSQGKamide
Detection method LANCE
Reference
staurosporine (IC 50 : 8 nM)
Meijer, L. et al. (1997) Eur. J. Biochem., 243: 527-536.
CDK2 (cycA)
Ref. 2908
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
BioPrint ® profile
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-CFFKNIVTPRTPPPSQGK-amide
(50 nM)
Measured product phospho-Ulight-CFFKNIVTPRTPPPSQGKamide
Detection method LANCE
Reference
staurosporine (IC 50 : 7.1 nM)
Meijer, L. et al. (1997) Eur. J. Biochem., 243: 527-536.
CDK3 (cycE1)
Ref. 2679
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-CFFKNIVTPRTPPPSQGK-amide
(100 nM)
Measured product phospho-Ulight-CFFKNIVTPRTPPPSQGKamide
Detection method LANCE
Reference
Ro-318220 (IC 50 : 10.8 nM)
Braun, K. et al. (1998) Oncogene, 17: 2259-2269.
CDK4 (cycD1)
Ref. 2876
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (Sf9 cells)
Substrate
ATP + Ulight-CFFKNIVTPRTPPPSQGK-amide
(100 nM)
Measured product phospho-Ulight-CFFKNIVTPRTPPPSQGKamide
Detection method LANCE
Reference
staurosporine (IC 50 : 181 nM)
Kim, D.M. et al. (2003) Exp. Mol. Med., 35: 421-430.
CDK5/p35
Ref. 2877
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate
ATP + Ulight-CFFKNIVTPRTPPPSQGK-amide
(100 nM)
Measured product phospho-Ulight-CFFKNIVTPRTPPPSQGKamide
Detection method LANCE
Reference
staurosporine (IC 50 : 13.5 nM)
Meijer, L. et al. (1997) Eur. J. Biochem., 243: 527-536.
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Assay developed in 2010 New assay conditions and/or assay converted from HTRF ® to LANCEUltra ®
Human Q Standard turnaround time

125
CDK6 (cycD3)
Ref. 2909
Q 3 weeks
Included in:
Comprehensive kinase profile
CDK7/MAT1 (cycH)
Ref. 2910
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-CFFKNIVTPRTPPPSQGK-amide
(50 nM)
Measured product phospho-Ulight-CFFKNIVTPRTPPPSQGKamide
Detection method LANCE
Reference
staurosporine (IC 50 : 200 nM)
Sridhar, J. et al. (2006) AAPS Journal, 8: E204-E221.
Source
human recombinant
Substrate
ATP + Ulight-CFFKNIVTPRTPPPSQGK-amide
(50 nM)
Measured product phospho-Ulight-CFFKNIVTPRTPPPSQGKamide
Detection method LANCE
Reference
staurosporine (IC 50 : 20 nM)
Tamrakar, S. et al. (2005) J. Virology, 79: 15477-15493.
protein-SERINE/THREONINE kinases [CMGC] ❚
Cerep
services
Receptors
Ion
channels
Transporters
CDK8 (cycC)
Ref. 2911
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-RRRSLLE
(50 nM)
Measured product phospho-Ulight-RRRSLLE
Detection method LANCE
Reference
staurosporine (IC 50 : 80.5 nM)
Elmlund, H. et al. (2006) Proc. Natl. Acad. Sci. U S A., 103: 15788-15793.
Kinases
Epigenetic &
DNA-related
enzymes
CDK9 (cycT1)
Ref. 2912
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (Sf9 cells)
Substrate
ATP + Ulight-CFFKNIVTPRTPPPSQGK-amide
(100 nM)
Measured product phospho-Ulight-CFFKNIVTPRTPPPSQGKamide
Detection method LANCE
Reference
staurosporine (IC 50 : 8.5 nM)
De Falco, G. and Giordano, A. (1998) J. Cell. Physiol., 177: 501-506.
Other
enzymes
Specialized
cellular
assays
CK2 (casein kinase 2)
Ref. 2913
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
Substrate
Measured product
Detection method
Reference
human recombinant (E. coli)
ATP + Ulight-IkappaB-alpha
(100 nM)
phospho-Ulight-IkappaB-alpha
LANCE
heparin (IC 50 : 1.47 nM)
Pinna, L.A. (1990) Bioch. Biophys. Acta., 1054: 267-284.
Standard
profiles
Testing
conditions
CLK1
Ref. 2787
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-CFFKNIVTPRTPPPSQGK-amide
(100 nM)
Measured product phospho-Ulight-CFFKNIVTPRTPPPSQGKamide
Detection method LANCE
Reference
staurosporine (IC 50 : 9.6 nM)
Muraki, M. et al. (2004) J. Biol. Chem., 279: 24246-24254.
Ordering
information
Assay list
& index

126 in vitro pharmacology 2011 catalog
❚ protein-SERINE/THREONINE kinases [CMGC]
CLK2
Source
human recombinant (insect cells)
Substrate
ATP + biotinyl-βAβAβAAGAGKRREILSRRPS
YRK (10 nM)
Measured product phospho-biotinyl-βAβAβAAGAGKRREILSRR
Ref. 2019
PSYRK
Detection method HTRF
Q 3 weeks
Reference
Ro-318220 (IC
Included in:
50 : 75 nM)
Comprehensive kinase profile Nayler, O. et al. (1998) J. Biol. Chem., 273: 34341-34348.
enzyme activity (% of control)
100
50
0
Ro-318220
staurosporine
K252a
H-89
-10 -9 -8 -7 -6 -5 -4 -3
log [drug] (M)
DYRK1a
Ref. 2781
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-CFFKNIVTPRTPPPSQGK-amide
(100 nM)
Measured product phospho-Ulight-CFFKNIVTPRTPPPSQGKamide
Detection method LANCE
Reference
staurosporine (IC 50 : 16 nM)
Himpel, S. et al. (2000) J. Biol. Chem., 275: 2431-2438.
-12 -11 -10 -9 -8 -7 -6 -5 -4
-10 -9 -8 -7 -6
-10 -7 -9 -8 -6 -5 -4
-11 -10 -6 -5
-12 -9 -8 -7
DYRK2
Ref. 2788
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-CFFKNIVTPRTPPPSQGK-amide
(100 nM)
Measured product phospho-Ulight-CFFKNIVTPRTPPPSQGKamide
Detection method LANCE
Reference
staurosporine (IC 50 : 1100 nM)
Taira, N. et al. (2007) Mol. Cell., 25: 725-738.
DYRK3
Ref. 1963
Q 3 weeks
Source
human recombinant (insect cells)
Substrate
ATP + biotinyl-MBP
(40 nM)
Measured product phospho-biotinyl-MBP
Detection method HTRF
Reference
staurosporine (IC 50 : 37 nM)
Li, K. et al. (2002) J. Biol. Chem., 277: 47052-47060.
enzyme activity (% of control)
100
50
staurosporine
Ro-318220
K252a
0
H-89
-8 -7 -6 -4
-9 -5
log [drug] (M)
DYRK4
Ref. 1962
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate
ATP + biotinyl-MBP
(80 nM)
Measured product phospho-biotinyl-MBP
Detection method HTRF
Reference
hymenialdisine (IC 50 : 149 nM)
Li, K. et al. (2002) J. Biol. Chem., 277: 47052-47060.
enzyme activity (% of control)
-10 -9 -8 -7 -6 -5 -4
100
-9 -8 -7 -6 -5 -4
50
0
-10 -9 -5 -8 -7 -6 -4
log [drug] (M)
hymenialdisine
staurosporine
Bis 10
EGCG
❚ Assays converted from HTRF ® to LANCEUltra ® technology
A majority of our kinase assays have been converted from HTRF ® to LANCEUltra ® technology. Both technologies are TR-FRET with the
difference in europium labelling: europium cryptate for HTRF ® and europium chelate for LANCEUltra ® .
Assays are converted following a standard procedure consisting of time course experiment, Km determination and pharmacology
characterization of the enzyme by inhibiting its activity with known inhibitors. IC 50 values obtained for known inhibitors are compared
to literature and to those obtained using HTRF ® technology. If all values are in agreement with the previous ones, LANCE ® technology is
validated for the kinase of interest.
This conversion allows us to standardize and automate our kinase assays providing shorter turnaround times for both profiling and screening
experiments.

protein-SERINE/THREONINE kinases [CMGC] ❚
127
ERK 1
Ref. 2914
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (E.coli)
Substrate
ATP + Ulight-CFFKNIVTPRTPPPSQGK-amide
(50 nM)
Measured product phospho-Ulight-CFFKNIVTPRTPPPSQGKamide
Detection method LANCE
Reference
staurosporine (IC 50 : 1.3 µM)
Yung, Y. et al. (2001) J. Biol. Chem., 276: 35280-35289.
Cerep
services
Receptors
ERK 2 (P42 mapk )
Ref. 2878
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
BioPrint ® profile
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (E.coli)
Substrate
ATP + Ulight-CFFKNIVTPRTPPPSQGK-amide
(100 nM)
Measured product phospho-Ulight-CFFKNIVTPRTPPPSQGKamide
Detection method LANCE
Reference
staurosporine (IC 50 : 539 nM)
Bardwell, A.J. et al. (2003) Biochem. J., 370: 1077-1085.
Ion
channels
Transporters
ERK 1/2
cellul ar
Ref. 3101
Ref. 3106
Q 3 weeks
Activator effect
Inhibitor effect
Source
Measured product
Detection method
A431 cells
phosphorylation
AlphaScreen
Activator effect Control EGF (10 nM)
Reference EGF (EC 50 : 0.098 nM)
Inhibitor effect Stimulant EGF (0.1 nM)
Reference AG1478 (IC 50 : 39 nM)
Zhang, Y.G. et al.(2008) Int. J. Oncol., 33: 595-602.
[Solvent] must be kept 0.1%
Kinases
Epigenetic &
DNA-related
enzymes
ERK 5 (MAPK7)
Ref. 2680
Q 3 weeks
Included in:
Comprehensive kinase profile
GSK3a
Ref. 2842
Q 3 weeks
Included in:
Comprehensive kinase profile
GSK3b
Ref. 2879
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Organ safety profile
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-CFFKNIVTPRTPPPSQGK-amide
(100 nM)
Measured product phospho-Ulight-CFFKNIVTPRTPPPSQGKamide
Detection method LANCE
Reference
Ro-318220 (IC 50 : 40 nM)
Mody, N. et al. (2003) Biochem. J., 372: 567-575.
Source
human recombinant
Substrate
ATP + Ulight-CFFKNIVTPRTPPPSQGK-amide
(100 nM)
Measured product phospho-Ulight-CFFKNIVTPRTPPPSQGKamide
Detection method LANCE
Reference
staurosporine (IC 50 : 28 nM)
Meijer, L. et al. (2003) Chem. Biol., 10: 1255-1266.
Source
human recombinant
Substrate
ATP + Ulight-CFFKNIVTPRTPPPSQGK-amide
(100 nM)
Measured product phospho-Ulight-CFFKNIVTPRTPPPSQGKamide
Detection method LANCE
Reference
staurosporine (IC 50 : 50 nM)
Meijer, L. et al. (2003) Chem. Biol., 10: 1255-1266.
Other
enzymes
Specialized
cellular
assays
Standard
profiles
Testing
conditions
Ordering
information
Assay list
& index

128 in vitro pharmacology 2011 catalog
❚ protein-SERINE/THREONINE kinases [CMGC]
GSK3b
cellul ar
Ref. 3102
Ref. 3107
Q 3 weeks
Activator effect
Inhibitor effect
Source
A431 cells
Measured product phosphorylation
Detection method AlphaScreen
Activator effect Control EGF (100 nM)
Reference EGF (EC 50 : 0.083 nM)
Inhibitor effect Stimulant EGF (0.1 nM)
Reference AG1478 (IC 50 : 75 nM)
[Solvent] must be kept 0.1%
HIPK2
Ref. 2915
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-CFFKNIVTPRTPPPSQGK-amide
(50 nM)
Measured product phospho-Ulight-CFFKNIVTPRTPPPSQGKamide
Detection method LANCE
Reference
staurosporine (IC 50 : 500 nM)
Di Stefano, V. et al. (2004) Exp. Cell. Res., 293: 311-320.
HIPK3
Ref. 1980
Q 3 weeks
Source
human recombinant (insect cells)
Substrate
ATP + biotinyl-MBP
(400 nM)
Measured product phospho-biotinyl-MBP
Detection method HTRF
Reference
staurosporine (IC 50 : 250 nM)
Rochat-Steiner, V. et al. (2000) J. Exp. Med., 192: 1165-1174.
enzyme activity (% of control)
100
50
staurosporine
Ro-318220
0
K252a
-8 -7 -6 -9 -5
log [drug] (M)
HIPK4
Ref. 1981
Q 3 weeks
Source
Substrate
Measured product
Detection method
Reference
-11 -10 -9 -8 -7 -6 -5 -4 -3
human recombinant (insect cells)
ATP + biotinyl-MBP
(200 nM)
phospho-biotinyl-MBP
HTRF
-10
staurosporine (IC 50 : 250 nM)
Di Stefano, V. et al. (2004) Exp. Cell. Res., 293: 311-320.
-9 -8 -7 -6 -5 -4
enzyme activity (% of control)
100-10
-9 -8 -7 -6 -5 -4 -3
-8 -7 -6 -5 -4
-10 -9 -8 -7 -6 -5
50
-10 -9 -8 -7 -6 -5
staurosporine
H-89
Ro-318220
0
K252a
-9 -8 -7 -6 -5 -4 -3
log [drug] (M)
JNK1
Ref. 2880
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Comprehensive kinase profile
Source
Substrate
Measured product
Detection method
Reference
human recombinant (E.coli)
-11 -10 -9 -8 -7 -6 -5 -4 -3
-10
-9 -8 -7 -6 -5 -4
ATP + Ulight-CFFKNIVTPRTPPPSQGK-amide
(100 nM)
phospho-Ulight-CFFKNIVTPRTPPPSQGKamide
LANCE
staurosporine (IC 50 : 1550 nM)
Bennett, B.L. et al. (2001) Proc. Natl. Acad. Sci. USA., 98: 13681-13686.
-10 -9 -8 -7 -6 -5 -4 -3
-8 -7 -6 -5 -4
-10 -9 -8 -7 -6 -5
-10 -9 -8 -7 -6 -5
JNK2
Ref. 3368
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (E. Coli)
Substrate
ATP + ATF-2
(75 nM)
Measured product phospho-ATF-2
Detection method LANCE
Reference
SP600125 (IC 50 : 69.9 nM)
Bennett, B.L. et al. (2001) Proc. Natl. Acad. Sci. USA, 98: 13681-13686.

129
JNK3
Ref. 2916
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (E.coli)
Substrate
ATP + Ulight-CFFKNIVTPRTPPPSQGK-amide
(100 nM)
Measured product phospho-Ulight-CFFKNIVTPRTPPPSQGKamide
Detection method LANCE
Reference
staurosporine (IC 50 : 550 nM)
Lisnock, J.M. et al. (2000) Biochemistry, 39: 3141-3148.
protein-SERINE/THREONINE kinases [CMGC] ❚
Cerep
services
Receptors
JNK1/3
cellul ar
Ref. 3138 Activator effect
Ref. 3142 Inhibitor effect
Q 3 weeks
Source
Measured product
Detection method
HEK-293 cells
phosphorylation
AlphaScreen
Activator effect Control anisomycin (10 µM)
Reference anisomycin (EC 50 : 140 nM)
Inhibitor effect Stimulant anisomycin (300 nM)
Reference unavailable
Liu, B.H. et al.(2006) Toxicol. Sci., 89: 423-430.
[Solvent] must be kept 0.1%
Ion
channels
Transporters
p38 MAPK
cellul ar
Ref. 3313 Activator effect
Ref. 3314 Inhibitor effect
Q 3 weeks
Source
Measured product
Detection method
A431 cells
coactivator recruitment
AlphaScreen
Activator effect Control TNF-a (10 nM)
Reference TNF-a (EC 50 : 0.1 nM)
Inhibitor effect Stimulant TNF-a (300 nM)
Reference SB202190 (IC 50 : 26 nM)
Li, B.H. et al.(2001) J. Invest. Dermatol., 117: 1601-1611.
α
[Solvent] must be kept 0.1%
Kinases
Epigenetic &
DNA-related
enzymes
p38a kinase
Ref. 2881
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
BioPrint ® profile
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (E.coli)
Substrate
ATP + Ulight-CFFKNIVTPRTPPPSQGK-amide
(100 nM)
Measured product phospho-Ulight-CFFKNIVTPRTPPPSQGKamide
Detection method LANCE
Reference
SB202190 (IC 50 : 45.5 nM)
Frantz, B. et al. (1998) Biochemistry, 37: 13846-13853.
Other
enzymes
Specialized
cellular
assays
p38b2 kinase (SAPK2b2)
Source
human recombinant (E. coli)
Substrate
ATP + ATF-2
(500 nM)
Measured product phospho-ATF-2
Detection method HTRF
Ref. 1960
Reference
SB202190 (IC 50 : 160 nM)
Q 3 weeks
Jiang, Y. et al. (1996) J. Biol. Chem., 271: 17920-17926.
enzyme activity (% of control)
100
50
SB202190
SB203580
staurosporine
0
SP600125
-9 -8 -7 -6 -5 -4
-10
log [drug] (M)
Standard
profiles
Testing
conditions
p38g kinase
Ref. 1580
Q 3 weeks
Source
human recombinant (insect cells)
Substrate
ATP + ATF-2
(250 nM)
Measured product phospho-ATF-2
Detection method HTRF
Reference
staurosporine (IC 50 : 180 nM)
Enslen, H. et al. (1998) J. Biol. Chem., 273: 1741-1748.
-9 -8 -7 -6 -5 -4
enzyme activity (% of control)
-9 -8 -7 -6 -5 -4
100
-8 -7 -6 -5 -4
50 -10 -9 -8 -7 -6 -5 -4
staurosporine
SB202190
SB203580
0
SP600125
-9 -8 -7 -6 -5 -4
log [drug] (M)
-11 -10 -9 -8 -7 -6 -5 -4
Ordering
information
Assay list
& index
-10 -9 -8 -7 -6 -5 -4
-9 -8 -7 -6 -5 -4

130 in vitro pharmacology 2011 catalog
❚ protein-SERINE/THREONINE kinases [CMGC]
p38d kinase
Ref. 3116
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
Substrate
Measured product
Detection method
Reference
human recombinant (E. coli)
ATP + Ulight-CFFKNIVTPRTPPPSQGK-amide
(25 nM)
phospho-Ulight-CFFKNIVTPRTPPPSQGKamide
LANCE
staurosporine (IC 50 : 331 nM)
Kuma, Y. et al. (2005) J. Biol. Chem., 280: 19472-19479.
enzyme activity (% of control)
100
50
0
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
staurosporine
BIRB796
K252a
PCTAIRE1 kinase
Ref. 2025
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (Sf9 cells)
Substrate
ATP + His-tagged Rb truncated protein
(30 nM)
Measured product phospho-His-tagged Rb truncated protein
Detection method HTRF
Reference
staurosporine (IC 50 : 33.7 nM)
Charrasse, S. et al. (1999) Cell Growth Differ., 10: 611-620.
❚ Protein-SERINE/THREONINE kinases [CaMK]
AMPKa
Ref. 1572
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
rat liver
Substrate
ATP + biotinyl-βAβAβAAAEEEYFFLFAKKK
(60 nM)
Measured product phospho-biotinyl-βAβAβAAAEEEYFFLFAKKK
Detection method HTRF
Reference
staurosporine (IC 50 : 0.9 nM)
Li, Y. et al. (2003) Anal. Biochem., 321: 151-156.
enzyme activity (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5
log [drug] (M)
staurosporine
H-89
Ro-318220
BRSK1
Ref. 2738
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 1.23 nM)
Bright, N.J. et al. (2008) J. Biol. Chem., 283: 14946-14954.
CaMK1a
Ref. 2739
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 6.7 nM)
Corcoran, E.E. et al. (2003) J. Biol. Chem., 12: 10516-10522.
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Assay developed in 2010 New assay conditions and/or assay converted from HTRF ® to LANCEUltra ®
Human Q Standard turnaround time

131
CaMK1d
Ref. 2922
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 3.3 nM)
Corcoran, E.E. et al. (2003) J. Biol. Chem., 12: 10516-10522.
protein-SERINE/THREONINE kinases [CaMK] ❚
Cerep
services
Receptors
CaMK2a
Ref. 3024
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
BioPrint ® profile
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-CGSGSGRPRTSSFAEG
(50 nM)
Measured product phospho-Ulight-CGSGSGRPRTSSFAEG
Detection method LANCE
Reference
AIP (IC 50 : 88 nM)
Ichida, A. and Fujisawa, H. (1995) J. Biol. Chem., 270: 2163-2170.
enzyme activity (% of control)
100
50
AIP
staurosporine
K252a
0
Ro-318220
-9 -8 -7 -6 -10 -5
log [drug] (M)
Ion
channels
Transporters
CaMK2g
Ref. 2740
Q 3 weeks
Source
human recombinant
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 0.84 nM)
Ishida, A. and Fujisawa, H. (1995) J. Biol. Chem., 270: 2163-2170.
-10 -9 -8 -7 -6 -5 -4 -3
-11 -10 -9 -8 -7 -6 -5 -4 -3
-11 -10 -9 -8 -7 -6 -5 -4
-12
-10 -9 -8 -7 -6
-10 -9 -8 -7 -6 -5 -4
-12 -11 -10 -8 -7 -6 -9 -5 -4 -3
-10 -9 -8 -7 -6 -12 -11 -5
-11 -10 -9 -8 -7 -6 -5 -4
Kinases
Epigenetic &
DNA-related
enzymes
CaMK4
Ref. 1582
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (E. coli)
Substrate ATP + biotinyl-long CREB derived peptide
(100 nM)
Measured product phospho-biotinyl-long CREB derived peptide
Detection method HTRF
Reference
staurosporine (IC 50 : 50 nM)
Enslen, H. et al. (1994) J. Biol. Chem., 269: 15520-15527.
enzyme activity (% of control)
100
50
staurosporine
K252a
0
AIP
-8 -7 -6 -5 -9 -4
log [drug] (M)
Other
enzymes
Specialized
cellular
assays
CHK1
Ref. 2917
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 5.6 nM)
Zhao, B. et. al. (2002) J. Biol. Chem., 277: 46609-46615.
Standard
profiles
Testing
conditions
CHK2
Ref. 2882
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 27 nM)
Ng, C.-P. et. al. (2004) J. Biol. Chem., 279: 8808-8819.
Ordering
information
Assay list
& index

132 in vitro pharmacology 2011 catalog
❚ protein-SERINE/THREONINE kinases [CaMK]
DAPK1
Ref. 1717
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + biotinyl-βAβAβAKKLNRTLSFAEP
(800 nM)
Measured product phospho-biotinyl-βAβAβAKKLNRTLSFAEP
Detection method HTRF
Reference
staurosporine (IC 50 : 80 nM)
Valentza, A.V. et al. (2001) J. Biol. Chem., 276: 38956-38965.
enzyme activity (% of control)
100
50
0
-9 -8 -7 -6 -5 -4
log [drug] (M)
staurosporine
H-89
Ro-318220
K252a
DAPK2
Ref. 1930
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + biotinyl-βAβAβAKKLNRTLSFAEP
(200 nM)
Measured product phospho-biotinyl-βAβAβAKKLNRTLSFAEP
Detection method HTRF
Reference
staurosporine (IC 50 : 8.3 nM)
Kavai, T. et al. (1999) Oncogene, 18: 3471-3480.
enzyme activity (% of control)
-10 -9 -8 -7 -6 -5 -4
100
-8 -7 -6 -5 -4
50
-10 -9 -8 -7 -6 -5 -4
staurosporine
Ro-318220
H-89
0
K252a
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
DCAMKL1
Ref. 2613
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 80 nM)
Lin, P.T. et al. (2000) J. Neurosc., 20: 9152-9161.
-9 -8 -7 -6 -5 -4
-8 -7 -6 -5 -4
-10 -9 -8 -7 -6 -5 -4
DCAMKL2
Ref. 2741
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 14.5 nM)
Ohmae, S. et. al. (2006) J. Biol. Chem., 281: 20427-20439.
DRAK1
Ref. 2930
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-ARTKQTARKSTGGKAPRKQLA
GCG (50 nM)
Measured product phospho-Ulight-ARTKQTARKSTGGKAPRKQ
LAGCG
Detection method LANCE
Reference staurosporine (IC 50 : 48 nM)
Sanjo, H. et al. (1998) J. Biol. Chem, 273: 29066-29071.
❚ Assays converted from HTRF ® to LANCEUltra ® technology
A majority of our kinase assays have been converted from HTRF ® to LANCEUltra ® technology. Both technologies are TR-FRET with the
difference in europium labelling: europium cryptate for HTRF ® and europium chelate for LANCEUltra ® .
Assays are converted following a standard procedure consisting of time course experiment, Km determination and pharmacology
characterization of the enzyme by inhibiting its activity with known inhibitors. IC 50 values obtained for known inhibitors are compared
to literature and to those obtained using HTRF ® technology. If all values are in agreement with the previous ones, LANCE ® technology is
validated for the kinase of interest.
This conversion allows us to standardize and automate our kinase assays providing shorter turnaround times for both profiling and screening
experiments.

133
MAPKAPK2
Ref. 3367
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (E. coli)
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 453 nM)
Tan, Y. et al. (1996) Embo. J., 15: 4629-4642.
protein-SERINE/THREONINE kinases [CaMK] ❚
Cerep
services
Receptors
MAPKAPK5 (PRAK)
Ref. 2684
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 2047 nM)
Ross, H. et. al. (2002) Biochem. J., 366: 977-981.
Ion
channels
Transporters
MARK1
Ref. 3362
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-RRRSLLE
(50 nM)
Measured product phospho-Ulight-RRRSLLE
Detection method LANCE
Reference staurosporine (IC 50 :14.4 nM)
Timm, T. et al. (2008) BMC Neurosc., 9: S9.
Kinases
Epigenetic &
DNA-related
enzymes
MARK2
Ref. 1966
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + biotinyl-bAbAbAKKKVSRSGLYRSPMP
ENLNRPR (80 nM)
Measured product phospho-biotinyl-bAbAbAKKKVSRSGLYRSP
MPENLNRPR
Detection method HTRF
Reference
H-89 (IC 50 : 3.067 µM)
Biernat, J. et al. (2002) Mol. Biol. Cell., 13: 4013-4028.
enzyme activity (% of control)
100
50
H-89
Ro-318220
0
K252a
-9 -8 -7 -6 -5 -4
log [drug] (M)
Other
enzymes
Specialized
cellular
assays
MARK3
Ref. 2789
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-RRRSLLE
(50 nM)
Measured product phospho-Ulight-RRRSLLE
Detection method LANCE
Reference
staurosporine (IC 50 : 7.46 nM)
Goransson, O. et al. (2006) J. Cell Sci., 119: 4059-4070.
-10 -9 -8 -7 -6 -5 -4
-10 -9 -8 -7 -6 -5 -4
-8 -7 -6 -5 -4
Standard
profiles
Testing
conditions
MARK4
Ref. 1967
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + biotinyl-bAbAbAKKKVSRSGLYRSPMP
ENLNRPR (80 nM)
Measured product phospho-biotinyl-bAbAbAKKKVSRSGLYRSP
MMPENLNRPR
Detection method HTRF
Reference
hymenialdisine (IC 50 : 80 nM)
Schneider, A. et al. (2004) J. Neurochem., 88: 1114-1126.
enzyme activity (% of control)
100
50
hymenialdisine
staurosporine
H-89
0
K252a
-9 -8 -7 -6 -5 -4
-10
log [drug] (M)
Ordering
information
Assay list
& index
-10 -9 -8 -7 -6 -5 -4
-10 -9 -8 -7 -6 -5 -4
-8 -7 -6 -5 -4

134 in vitro pharmacology 2011 catalog
❚ protein-SERINE/THREONINE kinases [CaMK]
MELK
Ref. 2742
Q 3 weeks
Source
human recombinant
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 3.6 nM)
Beullens, M. et al. (2006) J. Biol. Chem., 280: 40003-40011.
MNK1
Ref. 2614
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 43 nM)
Chrestensen, C.A. et al. (2007) J. Biol. Chem., 282: 4243-4252.
MNK2
Ref. 2918
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (Sf21 cells)
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 25 nM)
Waskiewicz, A.J. et. al. (1997) Embo. J., 16: 1909-1920.
NIM1 kinase (MGC42105)
Ref. 2792
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-RRRSLLE
(50 nM)
Measured product phospho-Ulight-RRRSLLE
Detection method LANCE
Reference staurosporine (IC 50 : 270 nM)
Tang, Z. et al. (1993) Embo. J., 12: 3427-3436.
NuaK1 (ARK5)
Ref. 2743
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 17 nM)
Suzuki, A. et al. (2004) Mol. Cell. Biol., 24: 3526-3535.
PASK
Ref. 2744
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 34.7 nM)
Rutter, J. et al. (2001) Proc. Natl. Acad. Sci. USA., 98: 8991-8996.

135
PhKg1
Ref. 2745
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 0.78 nM)
Burwinkel, B. et al. (2003) Eur. J. Hum. Genet., 11: 516-526.
protein-SERINE/THREONINE kinases [CaMK] ❚
Cerep
services
Receptors
PhKg2
Ref. 2622
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 4.6 nM)
Burwinkel, B. et al. (1998) Hum. Mol. Gen., 7: 149-154.
Ion
channels
Transporters
Pim1 kinase
Ref. 2919
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 35 nM)
Hoover, D. et. al. (1991) J. Biol. Chem., 266: 14018-14023.
Kinases
Epigenetic &
DNA-related
enzymes
Pim2 kinase
Ref. 2920
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 17 nM)
Van der Lugt, N.M. et. al. (1995) Embo. J., 14: 2536-2544.
Other
enzymes
Specialized
cellular
assays
PKD1 (PKCµ)
Ref. 2204
Q 3 weeks
Source
human recombinant (Sf21 cells)
Substrate ATP + biotinyl-bAbAbAKEAKEKRQEQIAKRR
RLSSLRASTSKSGGSQK (20 nM)
Measured product phospho-biotinyl-bAbAbAKEAKEKRQEQIAK
RRRLSSLRASTSKSGGSQK
Detection method HTRF
Reference
Ro-318220 (IC 50 : 8 nM)
Hausser, A. et al. (1999) J. Biol. Chem., 274: 9258-9264.
Standard
profiles
Testing
conditions
PKD2
Ref. 1729
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + biotinyl-bAbAbAKKKVSRSGLYRSPSM
PENLNRPR (25 nM)
Measured product phospho-biotinyl-bAbAbAKKKVSRSGLYRSP
SMPENLNRPR
Detection method HTRF
Reference
staurosporine (IC 50 : 8.7 nM)
Sturany, S. et al. (2001) J. Biol. Chem., 276: 3310-3318.
enzyme activity (% of control)
100
50
staurosporine
H-89
Ro-318220
0
K252a
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
-10 -9 -8 -7 -6 -5 -4
Ordering
information
Assay list
& index
-10 -9 -8 -7 -6 -5 -4
-8 -7 -6 -5 -4

136 in vitro pharmacology 2011 catalog
❚ protein-SERINE/THREONINE kinases [CaMK]
PKD3
Ref. 1982
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + biotinyl-bAbAbAKKKVSRSGLYRSPMP
ENLNRPR (30 nM)
Measured product phospho-biotinyl-bAbAbAKKKVSRSGLYRSP
MPENLNRPR
Detection method HTRF
Reference
staurosporine (IC 50 : 12.4 nM)
Sturany, S. et al. (2001) J. Biol. Chem., 276: 3310-3318.
SIK
Ref. 2921
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Comprehensive kinase profile
Source
human recombinant (Sf21 cells)
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
Ro-318220 (IC 50 : 7.2 nM)
Junko, D. et. al. (2002) J. Biol. Chem., 277: 15629-15637.
smMLCK (MYLK)
Ref. 2026
Q 3 weeks
Source
human recombinant (insect cells)
Substrate ATP + biotinyl-βAβAβAAGAGKRREILSRRPSYRK
(20 nM)
Measured product phospho-biotinyl-βAβAβAAGAGKRREILSRRP
SYRK
Detection method HTRF
Reference
staurosporine (IC 50 : 1.3 nM)
Ikebe, M. and Hartshorne, D.J. (1985) J. Biol. Chem., 260: 10027-10031.
STK33
Ref. 3039
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 9 nM)
Mujica, A.O. et al. (2005) FEBS. J., 272: 4884-4898.
TSSK1
Ref. 2791
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-RRRSLLE
(50 nM)
Measured product phospho-Ulight-RRRSLLE
Detection method LANCE
Reference
staurosporine (IC 50 : 0.58 nM)
Hao, Z. et al. (2004) Mol. Hum. Reprod., 10: 433-444.
TSSK2 (STK22B)
Ref. 2015
Q 3 weeks
Source
human recombinant (insect cells)
Substrate ATP + Ulight-RRRSLLE
(50 nM)
Measured product phospho-Ulight-RRRSLLE
Detection method LANCE
Reference
staurosporine (IC 50 : 6.3 nM)
Hao, Z. et al. (2004) Mol. Hum. Reprod., 10: 433-444.

137
❚ protein-SERINE/THREONINE kinases [AGC]
Cerep
services
Akt1/PKBa
Ref. 2923
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 37 nM)
Barnett, S.F. et al. (2005) Biochem. J., 385: 399-408.
Receptors
Ion
channels
Akt2/PKBb
Ref. 2924
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-RRRSLLE
(50 nM)
Measured product phospho-Ulight-RRRSLLE
Detection method LANCE
Reference
staurosporine (IC 50 : 11.5 nM)
Barnett, S.F. et al. (2005) Biochem. J., 385: 399-408.
Transporters
Kinases
Akt3/PKBg
Ref. 2925
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-RRRSLLE
(50 nM)
Measured product phospho-Ulight-RRRSLLE
Detection method LANCE
Reference
staurosporine (IC 50 : 13 nM)
Barnett, S.F. et al. (2005) Biochem. J., 385: 399-408.
Epigenetic &
DNA-related
enzymes
Other
enzymes
Akt1/2
cellul ar
Ref. 3099 Activator effect
Ref. 3104 Inhibitor effect
Q 3 weeks
Source
A431 cells
Measured product phosphorylation
Detection method AlphaScreen
Activator effect Control EGF (1 µM)
Reference EGF (EC 50 : 1 nM)
Inhibitor effect Stimulant EGF (10 nM)
Reference wortmannin (IC 50 : 23 nM)
Kim, S.H. et al.(2009) Ann. N. Y. Acad. Sci., 1171: 642-648.
[Solvent] must be kept 0.1%
Specialized
cellular
assays
Standard
profiles
CRIK
Ref. 2628
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-ARTKQTARKSTGGKAPRKQLAGCG
(75 nM)
Measured product phospho-Ulight-ARTKQTARKSTGKAPRKQL
AGCG
Detection method LANCE
Reference staurosporine (IC 50 : 40 nM)
Zhao, Z.S. and Manser, E. (2005) Biochem. J., 386: 201-214.
Testing
conditions
Ordering
information
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Assay developed in 2010 New assay conditions and/or assay converted from HTRF ® to LANCEUltra ®
Human Q Standard turnaround time
Assay list
& index

138 in vitro pharmacology 2011 catalog
❚ protein-SERINE/THREONINE kinases [AGC]
GRK2 (ADRBK1)
Ref. 2200
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + His-tagged Rb truncated protein
(140 nM)
Measured product phospho-His-tagged Rb truncated protein
Detection method HTRF
Reference
staurosporine (IC 50 : 50 nM)
Laccarino, G. et al. (2005) Eur. Heart. J., 26: 1752-1758.
GRK3/BARK2 (ADRBK2)
Ref. 2627
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-ARTKQTARKSTGGKAPRKQLAGCG
(25 nM)
Measured product phospho-Ulight-ARTKQTARKSTGGKAPRKQL
AGCG
Detection method LANCE
Reference
staurosporine (IC 50 : 295 nM)
Luo, J. and Benovic, J.L. (2003) J. Biol. Chem., 278: 50908-50914.
GRK5
Ref. 2020
Q 3 weeks
Source
human recombinant (insect cells)
Substrate ATP + biotinyl-KKKKERLLDDRHDSGLDSMKDEE
(600 nM)
Measured product phospho-biotinyl-KKKKERLLDDRHDSGLDSKDEE
Detection method HTRF
Reference
staurosporine (IC 50 : 27 nM)
Kunapuli, P. et al. (1994) J. Biol. Chem., 269: 1099-1106.
MRCKa
Ref. 2629
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-ARTKQTARKSTGGKAPRKQLAGCG
(75 nM)
Measured product phospho-Ulight-ARTKQTARKSTGGKAPRKQL
AGCG
Detection method LANCE
Reference staurosporine (IC 50 : 18 nM)
Tan, I. et al. (2001) Mol. Cell. Biol., 21: 2767-2778.
selected cerep assays
❚ Biochemical kinase assays
Kinase assays are enzymatic assays mostly using activated kinases. Those are usually full length kinase or cytoplasmic domain of RTK.
Assays are designed to be as close as possible to ATP and substrate Km.
The technology used to measure substrate phosphorylation is TR-FRET (HTRF ® or LANCE ® ). A few assays are cascade of activation.
❚ Cellular kinase assays
In order to complement our existing biochemical assay platform, we have implemented cellular kinase assays. These assays allow to
confirm inhibitors activity in a relevant cellular background and profile their selectivity against multiple signaling pathways.
- Cellular kinase phosphorylation assays
Cellular kinase phosphorylation assays are developed using AlphaScreen ® Surefire ® assay kits. The assays are optimized for directly
measuring kinase activation following treatment of cells with activators of signaling pathways.
- Cellular tyrosine kinase receptor activity assays
We have demonstrated that the impedance-based technology can be used to monitor the activity of the main tyrosine kinase receptor
families. These label-free assays allow the identification of inhibitors targeting either the ligand binding domain or the kinase domain.
These assays can be developed in virtually any cancer cell lines or primary cells. As an example, we have developed and validated
the EGFR cellular assay in the following cancer cell lines: A431, HELA and MDA-MB-231.
❚ Binding kinase assays
See page 107.

139
MSK1
Ref. 1724
Q 3 weeks
Source
human recombinant (insect cells)
Substrate ATP + biotinyl-βAβAβAAGAGKRREILSRRPSYRK
(10 nM)
Measured product phospho-biotinyl-βAβAβAAGAGKRREILSRRP
SYRK
Detection method HTRF
Reference
staurosporine (IC 50 : 15 nM)
Ross, H. et aL. (2002) Biochem. J., 366: 977-981.
protein-SERINE/THREONINE kinases [AGC] ❚
enzyme activity (% of control)
100
50
0
-10 -9 -8 -7 -6 -5
log [drug] (M)
staurosporine
H-89
Bis 10
K252a
Cerep
services
Receptors
MSK2
Ref. 1983
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + biotinyl-βAβAβARARTSSFAEPG
(150 nM)
Measured product phospho-biotinyl-βAβAβARARTSSFAEPG
Detection method HTRF
Reference
staurosporine (IC 50 : 3.91 nM)
Wiggin, G.R. et al. (2000) Mol. Cell. Biol., 22: 2871-2881.
enzyme activity (% of control)
100
-10 -9 -8 -7 -6 -5 -4
-8 -7 -6 -5 -4
-8 -7 -6 -9 -5 -4
50
staurosporine
Ro-318220
SB203580
0
K252a
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
Ion
channels
Transporters
NDR1 kinase
Ref. 2758
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + ARTKQTARKSTGGKAPRKQLAGCG
(75 nM)
Measured product phospho-ARTKQTARKSTGGKAPRKQLAGCG
Detection method LANCE
Reference
staurosporine (IC 50 : 18.5 nM)
Devroe, E. et al. (2004) J. Biol. Chem., 279: 24444-24451.
-10 -9 -8 -7 -6 -5 -4 -3
-12 -11 -10 -9 -8 -7 -6 -5 -4
-10 -9 -8 -7 -6
-10 -7 -9 -8 -6 -5 -4
-12 -11 -10 -6 -5
-9 -8 -7
Kinases
Epigenetic &
DNA-related
enzymes
p70S6K
Ref. 2883
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 9 nM)
Sutherland, C. and Cohen, P. (1994) FEBS Lett., 338: 37-42.
Other
enzymes
Specialized
cellular
assays
p70S6Kb
Ref. 2747
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 3.6 nM)
Gäbele, E. et al. (2005) J. Biol. Chem., 280: 13374-13382.
Standard
profiles
Testing
conditions
PDK1
Ref. 2926
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + Ulight-FLGFTYVAP
(400 nM)
Measured product phospho-Ulight-FLGFTYVAP
Detection method LANCE
Reference
staurosporine (IC 50 : 40 nM)
Hill, M.M. et al. (2001) J. Biol. Chem., 276: 25643-25646.
Ordering
information
Assay list
& index

140 in vitro pharmacology 2011 catalog
❚ protein-SERINE/THREONINE kinases [AGC]
PKA
Ref. 2927
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (E. coli)
Substrate ATP + Ulight-RRRSLLE
(50 nM)
Measured product phospho-Ulight-RRRSLLE
Detection method LANCE
Reference
staurosporine (IC 50 : 5.5 nM)
Hagiwara, M. et al. (1993) Mol. Cell. Biol., 13: 4852-4859.
PKCa
Ref. 0348
Q 3 weeks
Included in:
Diversity profile
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + biotinyl-βAβAβAKIQASFRGHMARKK
(60 nM)
Measured product phospho-biotinyl-βAβAβAKIQASFRGHMARKK
Detection method HTRF
Reference
Bis 10 (IC 50 : 3.2 nM)
Chen, S.J. et al. (1993) Biochemistry, 32: 1032-1039.
enzyme activity (% of control)
100
50
0
Bis 10
staurosporine
Ro-318220
H-89
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
PKCb1
Ref. 2888
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
Bis 10 (IC 50 : 0.22 nM)
Chen, S.J. et al. (1993) Biochemistry, 32: 1032-1039.
PKCb2
Ref. 2750
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Organ safety profile
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 5 nM)
Chen, S.J. et al. (1993) Biochemistry, 32: 1032-1039.
PKCg
Ref. 0350
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + biotinyl-βAβAβAKIQASFRGHMARKK
(500 nM)
Measured product phospho-biotinyl-βAβAβAKIQASFRGHMARKK
Detection method HTRF
Reference
Bis 10 (IC 50 : 24 nM)
Chen, S.J. et al. (1993) Biochemistry, 32: 1032-1039.
enzyme activity (% of control)
100
50
0
Bis 10
staurosporine
Ro-318220
H-89
-9 -8 -7 -6 -5 -10 -4
log [drug] (M)
PKCd
Ref. 0614
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + biotinyl-βAβAβAKIQASFRGHMARKK
(400 nM)
Measured product phospho-biotinyl-βAβAβAKIQASFRGHMARKK
Detection method HTRF
Reference
Bis 10 (IC 50 : 55 nM)
Chen, S.J. et al. (1993) Biochemistry, 32: 1032-1039.
enzyme activity (% of control)
100
50
0
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
Bis 10
staurosporine
Ro-318220
H-89

141
PKCe
Ref. 2044
Q 3 weeks
PKCz
Ref. 2045
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + biotinyl-bAbAbAKIQASFRGHMARKK
(400 nM)
Measured product phospho-biotinyl-bAbAbAKIQASFRGHMA
RKK
Detection method HTRF
Reference
Bis 10 (IC 50 : 8 nM)
Chen, S.J. et al. (1993) Biochemistry, 32: 1032-1039.
Source
human recombinant (insect cells)
Substrate ATP + biotinyl-βAβAβAKIQASFRGHMARKK
(600 nM)
Measured product phospho-biotinyl-βAβAβAKIQASFRGHMARKK
Detection method HTRF
Reference
Bis 10 (IC 50 : 61.3 nM)
Chen, S.J. et al. (1993) Biochemistry, 32: 1032-1039.
protein-SERINE/THREONINE kinases [AGC] ❚
enzyme activity (% of control)
100
50
0
-11 -10 -9 -8 -7 -6
log [drug] (M)
-10 -9 -8 -7 -6 -5 -4 -3
-12 -11 -10 -9 -8 -7 -6 -5 -4
-10 -9 -8 -7 -6
-10 -9 -8 -7 -6 -5 -4
-12 -11 -10 -9 -8 -7 -6 -5
Bis 10
staurosporine
Ro-318220
Cerep
services
Receptors
Ion
channels
Transporters
PKCh
Ref. 2046
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + biotinyl-βAβAβAKIQASFRGHMARKK
(200 nM)
Measured product phospho-biotinyl-βAβAβAKIQASFRGHMARKK
Detection method HTRF
Reference
Bis 10 (IC 50 : 53.6 nM)
Chen, S.J. et al. (1993) Biochemistry, 32: 1032-1039.
Kinases
Epigenetic &
DNA-related
enzymes
PKCq
Ref. 2120
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + biotinyl-βAβAβAKIQASFRGHMARKK
(200 nM)
Measured product phospho-biotinyl-βAβAβAKIQASFRGHMARKK
Detection method HTRF
Reference
Bis 10 (IC 50 : 1.55 nM)
Manicassamy, S. et al. (2006) Cell. Mol. Immun., 3: 263-270.
Other
enzymes
Specialized
cellular
assays
PKCi
Ref. 2121
Q 3 weeks
Source
human recombinant (insect cells)
Substrate ATP + biotinyl-βAβAβAKIQASFRGHMARKK
(200 nM)
Measured product phospho-biotinyl-βAβAβAKIQASFRGHMARKK
Detection method HTRF
Reference
Bis 10 (IC 50 : 100 nM)
Stallings-Mann, M. et al. (2006) Cancer Res., 66: 1767-1774.
Standard
profiles
Testing
conditions
PKG1a
Ref. 2469
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (Sf21 cells)
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 11.2 nM)
Hou, Y. et al. (2003) J. Biol. Chem., 278: 16706-16712.
Ordering
information
Assay list
& index

142 in vitro pharmacology 2011 catalog
❚ protein-SERINE/THREONINE kinases [AGC]
PKG1b
Ref. 1730
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (Sf21 cells)
Substrate ATP + biotinyl-KEAKEKRQEQIAKRRRLSSLRA
STSKSGGSQK (20 nM)
Measured product phospho-biotinyl-KEAKEKRQEQIAKRRRLSSL
RASTSKSGGSQK
Detection method HTRF
Reference
staurosporine (IC 50 : 26.8 nM)
Orstavik, S. et al. (1997), Genomics, 42: 311-318.
enzyme activity (% of control)
100
50
0
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
staurosporine
H-89
Ro-318220
K252a
PKG2
Ref. 1928
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + biotinyl-KEAKEKRQEQIAKRRRLSSLRA
STSKSGGSQK (50 nM)
Measured product phospho-biotinyl-KEAKEKRQEQIAKRRRLSSL
RASTSKSGGSQK
Detection method HTRF
Reference
staurosporine (IC 50 : 1.1 nM)
Ross, H. et aL. (2002) Biochem. J., 366: 977-981.
enzyme activity (% of control)
-11 -10 -9 -8 -7 -6 -5 -4
100
-10 -9 -8 -7 -6 -5 -4
-8 -7 -6 -5 -4
-8 -7 -6 -9 -5 -4
50
staurosporine
H-89
Ro-318220
0
K252a
-11 -10 -9 -8 -7 -6 -5
log [drug] (M)
PKN1
Ref. 2615
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 2 nM)
Lartey, J. et al. (2007) Biol. Reprod., 76: 971-982.
-11 -10 -9 -8 -7 -6 -5 -4
-10 -9 -8 -7 -6 -5 -4
-8 -7 -6 -5 -4
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5 -4
PKN2
Ref. 2746
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 1.23 nM)
Schmidt, A. et al. (2007) Embo. J., 26: 1624-1636.
PRKX
Ref. 2681
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-RRRSLLE
(50 nM)
Measured product phospho-Ulight-RRRSLLE
Detection method LANCE
Reference
staurosporine (IC 50 : 6.8 nM)
Chiorini, J.A. et al. (1998) Mol. Cell. Biol., 18: 5921-5929.
ROCK1
Ref. 3364
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Organ safety profile
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-RRRSLLE
(50 nM)
Measured product phospho-Ulight-RRRSLLE
Detection method LANCE
Reference
staurosporine (IC 50 : 20.2 nM)
Doe, C. et al.(2007) J. Pharmacol. Exp. Ther., 320: 89-98.

143
ROCK2
Ref. 2884
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-RRRSLLE
(100 nM)
Measured product phospho-Ulight-RRRSLLE
Detection method LANCE
Reference
staurosporine (IC 50 : 13 nM)
Turner, M.S. et al. (2002) Arch. Biochem. Biophys., 405: 13-20.
protein-SERINE/THREONINE kinases [AGC] ❚
Cerep
services
Receptors
RSK1
Ref. 2616
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 1.9 nM)
Roberts, N.A. et al. (2005) Brit. J. Pharmacol., 145: 477-489.
Ion
channels
Transporters
RSK2
Ref. 2928
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 2.63 nM)
Cho, Y.Y. et al. (2007) Cancer Res., 67: 8104-8112.
enzyme activity (% of control)
100
50
staurosporine
Gö 6850
kaempferol
0
SL0101
-12 -11 -10 -9 -8 -7 -6 -5 -4 -3
log [drug] (M)
Kinases
Epigenetic &
DNA-related
enzymes
RSK3
Ref. 2682
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-RRRSLLE
(50 nM)
Measured product phospho-Ulight-RRRSLLE
Detection method LANCE
Reference
staurosporine (IC 50 : 5 nM)
Chen, R.H. et al. (1992) Mol. Cell. Biol., 12: 915-927.
-10 -9 -8 -7 -6 -5 -4 -3
-11 -10 -9 -8 -7 -6 -5 -4 -3
-12 -11 -10 -9 -8 -7 -6 -5 -4
-10 -9 -8 -7 -6
-10 -7 -4
-9 -8 -6 -5
-12 -11 -10 -9 -8 -7 -6 -5 -4 -3
-10 -9 -8 -7 -6 -5
-12 -11
Other
enzymes
Specialized
cellular
assays
SGK1
Ref. 2929
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Organ safety profile
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-RRRSLLE
(50 nM)
Measured product phospho-Ulight-RRRSLLE
Detection method LANCE
Reference
staurosporine (IC 50 : 12 nM)
Ross, H. et al. (2002) Biochem. J., 366: 977-981.
-11 -10 -9 -8 -7 -6 -5 -4
Standard
profiles
Testing
conditions
❚ Assays converted from HTRF ® to LANCEUltra ® technology
A majority of our kinase assays have been converted from HTRF ® to LANCEUltra ® technology. Both technologies are TR-FRET with the
difference in europium labelling: europium cryptate for HTRF ® and europium chelate for LANCEUltra ® .
Assays are converted following a standard procedure consisting of time course experiment, Km determination and pharmacology
characterization of the enzyme by inhibiting its activity with known inhibitors. IC 50 values obtained for known inhibitors are compared
to literature and to those obtained using HTRF ® technology. If all values are in agreement with the previous ones, LANCE ® technology is
validated for the kinase of interest.
This conversion allows us to standardize and automate our kinase assays providing shorter turnaround times for both profiling and screening
experiments.
Ordering
information
Assay list
& index

144 in vitro pharmacology 2011 catalog
❚ protein-SERINE/THREONINE kinases [AGC]
SGK2
Ref. 1969
Q 3 weeks
Source
human recombinant (insect cells)
Substrate ATP + biotinyl-bAbAbAKGSGSGRPRTSSFAEF
(20 nM)
Measured product phospho-biotinyl-bAbAbAKGSGSGRPRTSSFAEF
Detection method HTRF
Reference
staurosporine (IC 50 : 270 nM)
Kobayashi, T. et al. (1999) Biochem. J., 344: 189-197.
enzyme activity (% of control)
100
50
0
-9 -8 -7 -6 -5 -4
log [drug] (M)
staurosporine
SP600125
H-89
Ro-318220
SGK3
Ref. 2790
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-RRRSLLE
(50 nM)
Measured product phospho-Ulight-RRRSLLE
Detection method LANCE
Reference
staurosporine (IC 50 : 123.5 nM)
Kobayashi, T. et al. (1999) Biochem. J., 344: 189-197.
-10 -9 -8 -7 -6 -5 -4
-11 -10 -9 -8 -7 -6 -5 -4
-8 -7 -6 -5 -4
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7 -6 -5
❚ protein-SERINE/THREONINE kinases [CK1]
CK1a
Ref. 1716
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Organ safety profile
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-ARTKQTARKSTGGKAPRKQLAG
CG (25 nM)
Measured product phospho-Ulight-ARTKQTARKSTGGKAPRKQL
AGCG
Detection method LANCE
Reference
hymenialdisin (IC 50 : 5.25 µM)
Pulgar, V. et al. (1996) Biochem. J., 242: 519-528.
CK1e
Ref. 2630
Q 3 weeks
Included in:
Organ safety profile
Source
human recombinant
Substrate ATP + Ulight-ARTKQTARKSTGGKAPRKQLAG
CG (25 nM)
Measured product phospho-Ulight-ARTKQTARKSTGGKAPRKQL
AGCG
Detection method LANCE
Reference
hymenialdisin (IC 50 : 3 µM)
Brockschmidt, C. et al. (2008) Gut., 57: 799-806.
❚ protein-SERINE/THREONINE kinases [STE]
ASK1
Ref. 2124
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + biotinyl-bAbAbAGISALQDGLKRREILSR
PPSYRKLL (1.4 µM)
Measured product phospho-biotinyl-bAbAbAGISALQDGLKRREI
LSRPPSYRKLL
Detection method HTRF
Reference staurosporine (IC 50 : 8 nM)
Sayama, K. et al. (2001) J. Biol. Chem., 276: 999-1004.
enzyme activity (% of control)
100
50
0
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
staurosporine
Ro-318220
H-89
K252a
-10 -9 -8 -7 -6 -5 -4 -3

145
COT kinase (MAP3K8)
Ref. 2003
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-FLGFTYVAP
(150 nM)
Measured product phospho-Ulight-FLGFTYVAP
Detection method LANCE
Reference
Raf-1 inhibitor (IC 50 : 12.5 µM)
Jia, Y. et al. (2006) Anal. Biochem., 350: 268-276.
protein-SERINE/THREONINE kinases [STE] ❚
Cerep
services
Receptors
GCK (MAP4K2)
Ref. 2590
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-FLGFTYVAP
(200 nM)
Measured product phospho-Ulight-FLGFTYVAP
Detection method LANCE
Reference
staurosporine (IC 50 : 4.27 nM)
Katz, P. et al. (1994) J. Biol. Chem., 269: 16802-16809.
Ion
channels
Transporters
HGK (MAP4K4)
Ref. 3365
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Organ safety profile
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-FLGFTYVAP
(50 nM)
Measured product phospho-Ulight-FLGFTYVAP
Detection method LANCE
Reference
staurosporine (IC 50 : 14.9 nM)
Yao, Z. et al. (1999) J. Biol. Chem., 274: 2118-2125.
Kinases
Epigenetic &
DNA-related
enzymes
MEK1 (MAP2K1)
Ref. 3293
Q 3 weeks
Source
human recombinant (insect cells)
Substrate ATP + inactivated ERK 2
(50 nM)
Measured product phospho-ERK 2
Detection method LANCE
Reference
staurosporine (IC 50 : 16 nM)
Kupcho, K.R. et al.(2008) Curr. Chem. Genomics., 1: 43-53.
Other
enzymes
Specialized
cellular
assays
MEK1
cellul ar
Ref. 3103 Activator effect
Ref. 3108 Inhibitor effect
Q 3 weeks
Source
A431 cells
Measured product phosphorylation
Detection method AlphaScreen
Activator effect Control EGF (10 nM)
Reference EGF (EC 50 : 0.033 nM)
Inhibitor effect Stimulant EGF (0.3 nM)
Reference MEK1/2 inhib. (IC 50 : 116.7 nM)
Janmaat, M.L. et al.(2003) Clin. Cancer. Res., 9: 2316-2326.
[Solvent] must be kept 0.1%
Standard
profiles
Testing
conditions
MEK5 (MAP2K5)
Ref. 2631
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-ARTKQTARKSTGGKAPRKQLAGCG
(25 nM)
Measured product phospho-Ulight-ARTKQTARKSTGGKAPRKQL
AGCG
Detection method LANCE
Reference staurosporine (IC 50 : 300 nM)
Sato, Y. et al. (2005) Am. J. Pathol., 166: 49-60.
Ordering
information
Assay list
& index

146 in vitro pharmacology 2011 catalog
❚ protein-SERINE/THREONINE kinases [STE]
MEKK3 (MAP3K3)
Ref. 2760
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-ARTKQTARKSTGGKAPRKQLAGCG
(25 nM)
Measured product phospho-Ulight-ARTKQTARKSTGGKAPRKQL
AGCG
Detection method LANCE
Reference staurosporine (IC 50 : 6.2 nM)
Samanta, A.K. et al. (2004) J. Biol. Chem., 279: 7576-7583.
MEKK4 (MAP3K4)
Ref. 2759
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-ARTKQTARKSTGGKAPRKQLAGCG
(25 nM)
Measured product phospho-Ulight-ARTKQTARKSTGGKAPRKQL
AGCG
Detection method LANCE
Reference staurosporine (IC 50 : 110 nM)
Chi, H. et al. (2005) Proc. Natl. Acad. Sci. USA, 102: 3846-3851.
MINK
Ref. 2113
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + biotinyl-bAbAbAAAARARTSSFAEPG
(200 nM)
Measured product phospho-biotinyl-bAbAbAAAARARTSSFAEPG
Detection method HTRF
Reference
Bis 10 (IC 50 : 27 nM)
Nicke, B. et al. (2005) Mol. Cell., 20: 673-685.
enzyme activity (% of control)
100
50
0
Bis 10
staurosporine
H-89
SB202190
-8 -7 -5 -4
-10 -9 -6
log [drug] (M)
MKK4/JNK1
Ref. 1927
Q 3 weeks
Included in:
Organ safety profile
Source
mouse recombinant (E. coli)
Substrate ATP + inactive JNK1
(0.19 µg/ml)
Measured product phospho-ATF-2
Detection method HTRF
Reference
staurosporine (IC 50 : 36 nM)
Han, J. et al. (1996) J. Biol. Chem., 271: 2886-2891.
-10 -9 -8 -7 -6 -5 -4 -3
-12 -11 -10 -9 -8 -7 -6 -5 -4
-10 -9 -8 -7 -6
-10 -7 -9 -8 -6 -5 -4
-12 -11 -10 -7 -6 -5
-9 -8
MKK4/JNK2
Ref. 1953
Q 3 weeks
Source
mouse recombinant
Substrate ATP + inactive JNK2 (MAPK9)
(0.05 µg/mL)
Measured product phospho-ATF-2
Detection method HTRF
Reference
staurosporine (IC 50 : 41 nM)
Han, J. et al. (1996) J. Biol. Chem., 271: 2886-2891.
enzyme activity (% of control)
100
50
staurosporine
SP600125
0
SB202190
-9 -8 -7 -6 -5 -4
log [drug] (M)
MKK6
Ref. 2931
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + inactive p38a
(50 nM)
Measured product phospho-p38a
Detection method LANCE
Reference
-11
-10 -9 -8 -7 -6 -5 -4
-10
staurosporine (IC 50 : 11 nM)
Han, J. et al. (1996) J. Biol. Chem., 271: 2886-2891.
-9 -8 -7 -6 -5 -4
-3
-10
-9 -8 -7 -6 -5 -4
-8 -7 -6 -5 -4
-10 -9 -8 -7 -6 -5
-10 -9 -8 -7 -6 -5 -4
-3

147
MKK6/p38a (mutant active)
Ref. 1679
Q 3 weeks
Source
human recombinant
Substrate ATP + inactive p38a
(0.75 nM)
Measured product phospho-ATF-2
Detection method HTRF
Reference
staurosporine (IC 50 : 29 nM)
Han, J. et al. (1996) J. Biol. Chem., 271: 2886-2891.
protein-SERINE/THREONINE kinases [STE] ❚
enzyme activity (% of control)
100
50
0
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
staurosporine
SP600125
U0126
SB202190
Cerep
services
Receptors
MST1 kinase (STK4)
Ref. 2585
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (Sf9 cells)
Substrate ATP + Ulight-FLGFTYVAP
(200 nM)
Measured product phospho-Ulight-FLGFTYVAP
Detection method LANCE
Reference
staurosporine (IC 50 : 14.5 nM)
Ura, S. et al. (2001) Proc. Natl. Acad. Sci. USA, 98: 10148-10153.
Ion
channels
Transporters
MST2 kinase
Ref. 2761
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-ARTKQTARKSTGGKAPRKQLAGCG
(100 nM)
Measured product phospho-Ulight-ARTKQTARKSTGGKAPRKQL
AGCG
Detection method LANCE
Reference staurosporine (IC 50 : 13 nM)
Lee, K.K. et al. (2001) J. Biol. Chem., 276: 19276-19285.
Kinases
Epigenetic &
DNA-related
enzymes
MST3 kinase
Ref. 2748
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 5 nM)
Huang, C.Y. et al. (2002) J. Biol. Chem., 277: 34367-34374.
Other
enzymes
Specialized
cellular
assays
MST4 kinase
Ref. 3366
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Comprehensive kinase profile
Source
Substrate
human recombinant
ATP + Ulight-PKC (50 nM)
Measured product phospho-Ulight-PKC
Detection method LANCE
Reference
staurosporine (IC 50 : 5.7 nM)
Qian, Z. et al. (2001) J. Biol. Chem., 276: 22439-22445.
Standard
profiles
Testing
conditions
NIK
Ref. 2325
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (Sf9 cells)
Substrate ATP + biotinyl-βAβAβAAGAGKRREILSRRPSYRK
(30 nM)
Measured product phospho-biotinyl-βAβAβAAGAGKRREILSRRPS
YRK
Detection method HTRF
Reference
Ro-318220 (IC 50 : 120 nM)
Park, G.Y. et al. (2006) J. Biol. Chem., 281: 18684-18690.
Ordering
information
Assay list
& index

148 in vitro pharmacology 2011 catalog
❚ protein-SERINE/THREONINE kinases [STE]
PAK1
Ref. 1934
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + biotinyl-tyrosine hydroxylase-derived
peptide (40 nM)
Measured product phospho-biotinyl-tyrosine hydroxylasederived
peptide
Detection method HTRF
Reference
staurosporine (IC 50 : 9 nM)
Yang, Z. et al. (2004) Clin. Cancer. Res., 10: 658-667.
enzyme activity (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
staurosporine
Ro-318220
K252a
H-89
-3
PAK2
Ref. 2932
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Comprehensive kinase profile
Source
human recombinant (Sf9 cells)
Substrate ATP + Ulight-RRRSLLE
(50 nM)
Measured product phospho-Ulight-RRRSLLE
Detection method LANCE
Reference
-10
staurosporine (IC 50 : 21 nM)
Wu, H. and Wang, Z-X. (2003) J. Biol. Chem., 278: 41768-41778.
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7 -6 -5 -4 -3
-8 -7 -6 -5 -4
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7 -6 -5
PAK4
Ref. 3363
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + Ulight-RRRSLLE
(50 nM)
Measured product phospho-Ulight-RRRSLLE
Detection method LANCE
Reference
staurosporine (IC 50 : 77.5 nM)
Arias-Romero, L.E. and Chernoff, J. (2008) Biol. Cell., 100: 97-108.
TAOK2 (TAO1)
Ref. 2586
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Organ safety profile
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-FLGFTYVAP
(40 nM)
Measured product phospho-Ulight-FLGFTYVAP
Detection method LANCE
Reference
staurosporine (IC 50 : 23 nM)
Hutchison, M. et al. (1998) J. Biol. Chem., 273: 28625-28632.
selected cerep assays
❚ Biochemical kinase assays
Kinase assays are enzymatic assays mostly using activated kinases. Those are usually full length kinase or cytoplasmic domain of RTK.
Assays are designed to be as close as possible to ATP and substrate Km.
The technology used to measure substrate phosphorylation is TR-FRET (HTRF ® or LANCE ® ). A few assays are cascade of activation.
❚ Cellular kinase assays
In order to complement our existing biochemical assay platform, we have implemented cellular kinase assays. These assays allow to
confirm inhibitors activity in a relevant cellular background and profile their selectivity against multiple signaling pathways.
- Cellular kinase phosphorylation assays
Cellular kinase phosphorylation assays are developed using AlphaScreen ® Surefire ® assay kits. The assays are optimized for directly
measuring kinase activation following treatment of cells with activators of signaling pathways.
- Cellular tyrosine kinase receptor activity assays
We have demonstrated that the impedance-based technology can be used to monitor the activity of the main tyrosine kinase receptor
families. These label-free assays allow the identification of inhibitors targeting either the ligand binding domain or the kinase domain.
These assays can be developed in virtually any cancer cell lines or primary cells. As an example, we have developed and validated
the EGFR cellular assay in the following cancer cell lines: A431, HELA and MDA-MB-231.
❚ Binding kinase assays
See page 107.

149
❚ protein-SERINE/THREONINE kinases [TKL]
Cerep
services
ALK4 (ACVR1B)
Ref. 3268
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-DNA topoisomerase 2a
(50 nM)
Measured product phospho-Ulight-DNA topoisomerase 2a
Detection method LANCE
Reference
staurosporine (IC 50 : 148 nM)
Laping, N.J. et al.(2002) Mol. Pharmacol., 62: 58-64.
Receptors
Ion
channels
BMPR1A kinase (ALK3)
Ref. 2762
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-ARTKQTARKSTGGKAPRKQLAGCG
(25 nM)
Measured product phospho-Ulight-ARTKQTARKSTGGKAPRKQL
AGCG
Detection method LANCE
Reference staurosporine (IC 50 : 148 nM)
Zhou, X.P. et al. (2001) Am. J. Hum. Genet., 69: 704-711.
Transporters
Kinases
B-raf kinase
Ref. 3294
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + inactive MEK1
(15 nM)
Measured product phospho-inactive MEK1
Detection method LANCE
Reference
Raf-1 inhibitor (IC 50 : 213 nM)
Kupcho, K.R. et al.(2008) Curr. Chem. Genomics., 1: 43-53.
Epigenetic &
DNA-related
enzymes
Other
enzymes
DLK1 (MAP3K12)
Ref. 2620
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 2.36 nM)
Robitaille, H. et al. (2005) J. Biol. Chem., 280: 12732-12741.
Specialized
cellular
assays
Standard
profiles
IRAK1
Ref. 1968
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + Ulight-FLGFTYVAP
(200 nM)
Measured product phospho-Ulight-FLGFTYVAP
Detection method LANCE
Reference
staurosporine (IC 50 : 43.5 nM)
Huang, Y. et al. (2004) J. Biol. Chem., 279: 51697-51703.
Testing
conditions
Ordering
information
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Assay developed in 2010 New assay conditions and/or assay converted from HTRF ® to LANCEUltra ®
Human Q Standard turnaround time
Assay list
& index

150 in vitro pharmacology 2011 catalog
❚ protein-SERINE/THREONINE kinases [TKL]
IRAK4
Ref. 2933
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + Ulight-FLGFTYVAP
(50 nM)
Measured product phospho-Ulight-FLGFTYVAP
Detection method LANCE
Reference staurosporine (IC 50 : 32 nM)
Li, S. et al. (2002) Proc. Natl. Acad. Sci. U S A., 99: 5567-5572.
LIMK1
Ref. 2934
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (Sf21 cells)
Substrate ATP + Ulight-RRRSLLE
(50 nM)
Measured product phospho-Ulight-RRRSLLE
Detection method LANCE
Reference
staurosporine (IC 50 : 59 nM)
Scott, R.W. and Olson, M.F. (2007) J. Mol. Med., 85: 555-568.
LRRK2
Ref. 3177
Q 3 weeks
Source
human recombinant (insect cells)
Substrate ATP + Ulight-RRRSLLE
(50 nM)
Measured product phospho-Ulight-RRRSLLE
Detection method LANCE
Reference
H-89 (IC 50 : 30 nM)
Greggio, E. et al. (2008) J. Biol. Chem., 283: 16906-16914.
MLK1
Ref. 2935
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-FLGFTYVAP
(400 nM)
Measured product phospho-Ulight-FLGFTYVAP
Detection method LANCE
Reference
staurosporine (IC 50 : 21.5 nM)
Maroney, A.C. et al. (2001) Biochem. J., 276: 25302-25308.
MLK2 (MAP3K10)
Ref. 2326
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + Ulight-ARTKQTARKSTGGKAPRKQLAGCG
(25 nM)
Measured product phospho-Ulight-ARTKQTARKSTGGKAPRKQL
AGCG
Detection method LANCE
Reference
staurosporine (IC 50 : 79 nM)
Liu, Y.F. et al. (2000) J. Biol. Chem., 275: 19035-19040.
RAF-1 kinase
Ref. 2936
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Organ safety profile
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-ARTKQTARKSTGGKAPRKQLAGCG
(50 nM)
Measured product phospho-Ulight-ARTKQTARKSTGGKAPRKQL
AGCG
Detection method LANCE
Reference staurosporine (IC 50 : 94 nM)
Force, T. et al. (1994) Proc. Natl. Acad. Sci. USA., 91: 1270-1274.

151
RAF-1/MEK1
Ref. 1703
Q 3 weeks
RIPK2
Ref. 2763
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + inactive MEK1
(200 nM)
Measured product phospho-ERK 2
Detection method HTRF
Reference
staurosporine (IC 50 : 150 nM)
Force, T. et al. (1994) Proc. Natl. Acad. Sci. USA, 91: 1270-1274.
Source
human recombinant
Substrate ATP + Ulight-ARTKQTARKSTGGKAPRKQLAGCG
-9 -8 -7 -6 -5 -4
(25 nM)
Measured product phospho-Ulight-ARTKQTARKSTGGKAPRKQL
AGCG
Detection method LANCE
Reference staurosporine (IC 50 : 150 nM)
McCarthy, J.V. et al. (1998) J. Biol. Chem., 273: 16968-16975.
-10
protein-SERINE/THREONINE kinases [TKL] ❚
enzyme activity (% of control)
100
50
0
-11
-10
-9 -8 -7 -6 -5 -4
log [drug] (M)
-10 -9 -8 -7 -6 -5 -4
-9 -8 -7 -6 -5 -4
-8 -7 -6 -5 -4
-10 -9 -8 -7 -6 -5
-10 -9 -8 -7 -6 -5
-3
staurosporine
ZM336372
PD98059
U0126
Cerep
services
Receptors
Ion
channels
Transporters
TAK1-TAB1 (MAP3K7)
Ref. 3017
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-FLGFTYVAP
(200 nM)
Measured product phospho-Ulight-FLGFTYVAP
Detection method LANCE
Reference
staurosporine (IC 50 : 95 nM)
Safwat, N. et al. (2005) Endocrinol., 146: 4814-4824.
Kinases
Epigenetic &
DNA-related
enzymes
❚ other kinases
Other
enzymes
AurA/Aur2 kinase
Ref. 2885
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Comprehensive kinase profile
Source
human recombinant (Sf21 cells)
Substrate ATP + Ulight-RRRSLLE
(100 nM)
Measured product phospho-Ulight-RRRSLLE
Detection method LANCE
Reference
staurosporine (IC 50 : 10 nM)
Sun, C. et al. (2004) J. Biomol. Screen., 9: 391-397.
Specialized
cellular
assays
Standard
profiles
AurB/Aur1 kinase
Ref. 1841
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + biotinyl-PLK-derived peptide
(50 nM)
Measured product phospho-biotinyl-PLK-derived peptide
Detection method HTRF
Reference
staurosporine (IC 50 : 46 nM)
Bishop, J.D. and Schumacher, J.M. (2002) J. Biol. Chem., 277: 27577-27580.
enzyme activity (% of control)
100
50
staurosporine
H-89
Ro-318220
0
KT5720
-8 -7 -6 -5 -9 -4
log [drug] (M)
Testing
conditions
Ordering
information
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
-10 -9 -8 -7 -6 -5 -4
-10 -9 -8 -7 -6 -5 -4
-8 -7 -6 -5 -4
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Assay developed in 2010 New assay conditions and/or assay converted from HTRF ® to LANCEUltra ®
Human Q Standard turnaround time
Assay list
& index

152 in vitro pharmacology 2011 catalog
❚ other kinases
AurC/Aur3 kinase
Ref. 1842
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + biotinyl-PLK-derived peptide
(200 nM)
Measured product phospho-biotinyl-PLK-derived peptide
Detection method HTRF
Reference
staurosporine (IC 50 : 45.8 nM)
Li, X. et al. (2004) J. Biol. Chem., 279: 47201-47211.
enzyme activity (% of control)
100
50
0
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
staurosporine
H-89
Ro-318220
KT5720
CDC7/ASK
Ref. 2764
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-ARTKQTARKSTGGKAPRKQLAGCG
(50 nM)
Measured product phospho-Ulight-ARTKQTARKSTGGKAPRKQL
AGCG
Detection method LANCE
Reference staurosporine (IC 50 : 271 nM)
Montagnoli, A. et al. (2008) Nat. Chem. Biol., 4: 357-365.
-10 -9 -8 -7 -6 -5 -4
-8 -7 -6 -5 -4
-9 -8 -7 -6 -5 -4
IKKa
Ref. 2937
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (Sf21 cells)
Substrate ATP + Ulight-IkappaB-alpha
(100 nM)
Measured product phospho-Ulight-IkappaB-alpha
Detection method LANCE
Reference
staurosporine (IC 50 : 60 nM)
Khai Huynh, Q. et al. (2000) J. Biol. Chem., 275: 25883-25891.
IKKb
Ref. 2938
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (Sf21 cells)
Substrate ATP + Ulight-IkappaB-alpha
(100 nM)
Measured product phospho-Ulight-IkappaB-alpha
Detection method LANCE
Reference
staurosporine (IC 50 : 500 nM)
Khai Huynh, Q. et al. (2000) J. Biol. Chem., 275: 25883-25891.
IKKe (IKBKE)
Ref. 2587
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (Sf9 cells)
Substrate ATP + Ulight-FLGFTYVAP
(40 nM)
Measured product phospho-Ulight-FLGFTYVAP
Detection method LANCE
Reference
staurosporine (IC 50 : 4.9 nM)
Eddy, S.F. et al. (2005) Cancer Res., 65: 11375-11383.
MOS kinase
Ref. 2765
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-DEKTDDED
(75 nM)
Measured product phospho-Ulight-DEKTDDED
Detection method LANCE
Reference
staurosporine (IC 50 : 74.3 nM)
Robertson, S.C. and Donoghue, D.J. (1996) Mol. Cell. Biol., 16: 3472-3479.

153
other kinases ❚
MYT1 kinase
Ref. 2521
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 8.8 nM)
Yee, K.S.Y. and Yu, V.C. (1998) J. Biol. Chem., 273: 5366-5374.
Cerep
services
Receptors
NEK1
Ref. 1931
Q 3 weeks
Included in:
Organ safety profile
Source
human recombinant (insect cells)
Substrate ATP + biotinyl-KEAKEKRQEQIAKRRRLSSLRA
STSKSGGSQK (200 nM)
Measured product phospho-biotinyl-KEAKEKRQEQIAKRRRLSSL
RASTSKSGGSQK
Detection method HTRF
Reference
staurosporine (IC 50 : 51.6 nM)
Fry, A.M. et al. (1995) J. Biol. Chem., 270: 12899-12905.
enzyme activity (% of control)
100
50
staurosporine
Ro-318220
H-89
0
K252a
-8 -7 -6 -4
-9 -5
log [drug] (M)
Ion
channels
Transporters
NEK2
Ref. 2939
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + Ulight-FLGFTYVAP
(50 nM)
Measured product phospho-Ulight-FLGFTYVAP
Detection method LANCE
Reference
staurosporine (IC 50 : 1.5 µM)
Fry, A.M. et al. (1995) J. Biol. Chem., 270: 12899-12905.
-9 -8 -7 -6 -5 -4
-10 -9 -8 -7 -6 -5 -4
-10 -9 -8 -7 -6 -5 -4
Kinases
Epigenetic &
DNA-related
enzymes
NEK4
Ref. 2950
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + Ulight-FLGFTYVAP
(40 nM)
Measured product phospho-Ulight-FLGFTYVAP
Detection method LANCE
Reference
staurosporine (IC 50 : 70 nM)
Hayashi, K. et al. (1999) Biochem. Biophys. Res. Commun., 264: 449-456.
Other
enzymes
Specialized
cellular
assays
NEK6
Ref. 1933
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + Ulight-FLGFTYVAP
(40 nM)
Measured product phospho-Ulight-FLGFTYVAP
Detection method LANCE
Reference
Raf-1 inhibitor (IC 50 : 8.5 µM)
Minoguchi, S. et al. (2003) Biochem. Biophys. Res. Com., 301: 899-906.
Standard
profiles
Testing
conditions
NEK7
Ref. 2588
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (Sf9 cells)
Substrate ATP + Ulight-FLGFTYVAP
(200 nM)
Measured product phospho-Ulight-FLGFTYVAP
Detection method LANCE
Reference
Raf-1 inhibitor (IC 50 : 26 µM)
Minoguchi, S. et al. (2003) Biochem. Biophys. Res. Com., 301: 899-906.
Ordering
information
Assay list
& index

154 in vitro pharmacology 2011 catalog
❚ other kinases
PEK (EIF2AK3)
Ref. 2589
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-FLGFTYVAP
(40 nM)
Measured product phospho-Ulight-FLGFTYVAP
Detection method LANCE
Reference
staurosporine (IC 50 : 2.28 µM)
Wek, R.C. et al. (2006) Bioch. Soc. Trans., 34: part 1.
PKR (EIF2AK2)
Ref. 2522
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-ARTKQTARKSTGGKAPRKQLAGCG
(25 nM)
Measured product phospho-Ulight-ARTKQTARKSTGGKAPRKQL
AGCG
Detection method LANCE
Reference
staurosporine (IC 50 : 420 nM)
Kim, S.H. et al. (2000) Oncogene, 19: 3086-3094.
PLK1
Ref. 2049
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-FLGFTYVAP
(40 nM)
Measured product phospho-Ulight-FLGFTYVAP
Detection method LANCE
Reference
staurosporine (IC 50 : 427 nM)
Golsteyn, R.M. et al. (1995) J. Cell. Biol., 129: 1617-1628.
PLK2
Ref. 2766
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-FLGFTYVAP
(200 nM)
Measured product phospho-Ulight-FLGFTYVAP
Detection method LANCE
Reference
staurosporine (IC 50 : 355 nM)
Inglis, K.J. et al. (2009) J. Biol. Chem., 284: 2598-2602.
PLK3
Ref. 2793
Q 3 weeks
Source
human recombinant
Substrate ATP + Ulight-CGSGSGRPRTSSFAEG
(50 µM)
Measured product phospho-Ulight-CGSGSGRPRTSSFAEG
Detection method LANCE
Reference
wortmannin (IC 50 : 130 nM)
Liu, Y. et al. (2007) J. Biol. Chem., 282: 2505-2511.
PLK4
Ref. 2749
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 13 nM)
Liu, Y. et al. (2007) J. Biol. Chem., 282: 2505-2511.

155
other kinases ❚
TBK1
Ref. 3347
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (Sf9 cells)
Substrate ATP + Ulight-FLGFTYVAP
(200 nM)
Measured product phospho-Ulight-FLGFTYVAP
Detection method LANCE
Reference
staurosporine (IC 50 : 16 nM)
Clark K. et al.(2009) J. Biol. Chem., 284: 14136-14146.
Cerep
services
Receptors
TTK
Ref. 2767
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-ARTKQTARKSTGGKAPRKQLAGCG
(25 nM)
Measured product phospho-Ulight-ARTKQTARKSTGGKAPRKQL
AGCG
Detection method LANCE
Reference
staurosporine (IC 50 : 400 nM)
Mills, G.B. et al. (1992) J. Biol. Chem., 267: 16000-16006.
Ion
channels
Transporters
ULK1
Ref. 3346
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (Sf9 cells)
Substrate ATP + Ulight-FLGFTYVAP
(200 nM)
Measured product phospho-Ulight-FLGFTYVAP
Detection method LANCE
Reference
staurosporine (IC 50 : 24 nM)
Jung, C.H. et al.(2009) Mol. Bio. Cell., 20: 1992-2003.
Kinases
Epigenetic &
DNA-related
enzymes
ULK2
Ref. 3348
Q 3 weeks
Source
human recombinant (Sf21 cells)
Substrate ATP + Ulight-FLGFTYVAP
(150 nM)
Measured product phospho-Ulight-FLGFTYVAP
Detection method LANCE
Reference
staurosporine (IC 50 : 6.4 nM)
Jung, C.H. et al.(2009) Mol. Bio. Cell., 20: 1992-2003.
Other
enzymes
Specialized
cellular
assays
Wee1 kinase
Ref. 2940
Q 3 weeks
Included in:
Comprehensive kinase profile
WNK2
Ref. 2768
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + Ulight-ARTKQTARKSTGGKAPRKQLAGCG
(25 nM)
Measured product phospho-Ulight-ARTKQTARKSTGGKAPRKQL
AGCG
Detection method LANCE
Reference staurosporine (IC 50 : 150 nM)
Yoshida, T. et al. (2004) Annal. Oncol., 15: 252-256.
Source
human recombinant
Substrate ATP + Ulight-ARTKQTARKSTGGKAPRKQLAGCG
(50 nM)
Measured product phospho-Ulight-ARTKQTARKSTGGKAPRKQL
AGCG
Detection method LANCE
Reference
staurosporine (IC 50 : 455 nM)
Richardson, C. and Alessi, D.R. (2008) J. Cell. Sci., 121: 3293-3304.
Standard
profiles
Testing
conditions
Ordering
information
Assay list
& index

156 in vitro pharmacology 2011 catalog
❚ other kinases
WNK3
Ref. 2114
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-ARTKQTARKSTGGKAPRKQLAGCG
(75 nM)
Measured product phospho-Ulight-ARTKQTARKSTGGKAPRKQL
AGCG
Detection method LANCE
Reference
staurosporine (IC 50 : 3.15 µM)
Rinehart, J. et al. (2005) Proc. Natl. Acad. Sci. USA, 102: 16777-16782.
WNK4
Ref. 2633
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-ARTKQTARKSTGGKAPRKQLAGCG
(25 nM)
Measured product phospho-Ulight-ARTKQTARKSTGGKAPRKQL
AGCG
Detection method LANCE
Reference
staurosporine (IC 50 : 235 nM)
Vitari, A.C. et al. (2005) Biochem. J., 391: 17-24.
❚ atypical kinases
mTOR kinase (FRAP1)
Ref. 2941
Q 3 weeks
Source
human recombinant (insect cells)
Substrate ATP + Ulight-FLGFTYVAP
(40 nM)
Measured product phospho-Ulight-FLGFTYVAP
Detection method LANCE
Reference
PI-103 (IC 50 : 129 nM)
Aoki, M. et al. (2001) Proc. Natl. Acad. Sci. USA, 98: 136-141.
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Assay developed in 2010 New assay conditions and/or assay converted from HTRF ® to LANCEUltra ®
Human Q Standard turnaround time

157
Cerep
services
Epigenetic
& DNA-related enzymes
Receptors
Ion
channels
Epigenetics describes a stably heritable change in phenotype or gene expression in an organism or cell, resulting from changes in a chromosome
that is not caused by a change in DNA sequence. The epigenetic regulation of gene transcription is a key biological determinant of cellular
differentiation. There are three distinct classes of epigenetic information that can be stably inherited over cell divisions: DNA methylation, non
coding RNAs, and histone modifications. DNA methylation is the best understood and the most extensively studied epigenetic mechanism.
Histone modification includes acetylation/deacetylation, phosphorylation, ubiquitination and methylation/demethylation.
Cerep has developed a large panel of histone deacetylases (HDAC). HDACs remove the acetyl groups from the lysine residues leading to
the formation of a condensed and transcriptionally silenced chromatin. HDAC inhibitors block this action, thereby affecting gene expression.
Different DNA methylase enzymes are under development and will be available soon.
Classical genetic includes the DNA replication and DNA repair enzymes. Both families of enzyme are involved in mitosis and ensure that exact
copies of the DNA in chromosomes are passed on to daughter cells. To carry out gene expression, and to replicate chromosomes, a cell must
control the coiling and uncoiling of DNA, around DNA itself and around histones. This is accomplished with different types of enzymes such as
topoisomerases. Topoisomerases are critical for maintaining normal DNA topography and Topoisomerase inhibitors cause breaks in the DNA
strand leading to cell death.
Different classes of epigenetic enzymes have been demonstrated to have strong disease association and are currently being targeted for small
molecule inhibition in cancer therapy. Mutation in genes critical to cellular growth and survival can also cause and promote cancer. Another
class of enzymes called kinesins, are also interesting as anticancer agents, as they are present in actively dividing cells only during mitosis.
Cerep has developed Eg5 and CENP-E which help chromosomes align and separate during mitosis.
The assays in this section allow elucidation of compounds activity on a number of enzymes involved in epigenetics and DNA function. Extensive
research is aimed at discovering small molecule inhibitors against them for therapeutic use.
❚ For further information, please contact us ar sales@cerep.com
Transporters
Kinases
Epigenetic &
DNA-related
enzymes
Other
enzymes
❚ DNA repair & mitotic enzymes
Specialized
cellular
assays
CENP-E
Ref. 2150
Q 3 weeks
Included in:
Non-kinase enzyme profile
Diversity profile
Organ safety profile
Source
human recombinant (E. coli)
Substrate
ATP (100 µM)
Measured product inorganic phosphate
Detection method photometry
Reference
rose bengal (IC 50 : 1.3 µM)
Goldstein, L.S.B. (1993) An. Rev. Genetic, 27: 319-351.
enzyme activity (% of control)
100
50
0
-9 -8 -7 -6 -5
log [drug] (M)
rose bengal
Standard
profiles
Testing
conditions
DNA polymerase I
Ref. 2348
Q 6 weeks
Source
bacterial recombinant (E. coli)
Substrate
[ 3 H]TTP (300 nM)
Measured product [ 3 H]TTP incorporation
Detection method scintillation counting
Reference
rifampicin (IC 50 : 9.3 µM)
Tuske, S. et al. (2000) J. Biol. Chem., 275: 23759-23768.
-10 -9 -8 -7 -6 -5 -4 -3
-12 -11 -10 -9 -8 -7 -6 -5 -4
-10 -9 -8 -7 -6
-10 -7 -9 -8 -6 -5 -4
-11 -10 -6 -5
-12 -9 -8 -7
Ordering
information
Assay list
& index

158 in vitro pharmacology 2011 catalog
❚ dna repair & mitotic enzymes
DNA polymerase b
Ref. 2445
Q 3 weeks
Included in:
Organ safety profile
Source
human recombinant (E. coli)
Substrate
[ 3 H]TTP (50 µM)
Measured product [ 3 H]TTP incorporation
Detection method scintillation counting
Reference
rifampicin (IC 50 : 12 µM)
Tuske, S. et al. (2000) J. Biol. Chem., 275: 23759-23768.
Eg5
Ref. 2151
Q 3 weeks
Included in:
Non-kinase enzyme profile
Diversity profile
Organ safety profile
Source
human recombinant
Substrate
ATP (50 µM)
Measured product inorganic phosphate
Detection method photometry
Reference
S-trityl-L-cysteine (IC 50 : 365 nM)
Goldstein, L.S.B. (1993) An. Rev. Genetic, 27: 319-351.
enzyme activity (% of control)
100
50
S-trityl-L-cysteine
trans 24
dimethylenastron
0
monastrol
-10 -9 -8 -7 -6 -5 -4
-11
log [drug] (M)
topoisomerase II
Ref. 2430
[Custom offer]
Please contact us at:
customresearch@cerep.com
Source
human recombinant
Substrate
supercoiled pN01 plasmid DNA substrate
(25 µg/mL)
Measured product triplex formation (substrate/oligonucleotide)
Detection method fluorimetry
Reference
XK469 (IC 50 :90 µM)
Maxwell, A. et al. (2006) Nucleic Acids Res., 34: 1-7.
-10 -9 -8 -7 -6 -5 -4 -3
-12 -11 -10 -9 -8 -7 -6 -5 -4
-10 -9 -8 -7 -6
-10 -7 -9 -8 -6 -5 -4
-11 -6 -12 -10 -5
-9 -8 -7
❚ HDACs
HDAC1
Ref. 2491
Q 3 weeks
Source
human recombinant
Substrate
fluorogenic HDAC substrate (20 µM)
Measured product fluoro-lysine
Detection method fluorimetry
Reference
trichostatin A (IC 50 : 7.2 nM)
Strahl, B.D. and Allis, C.D. (2000) Nature, 403: 41-45.
HDAC2
Ref. 2492
Q 3 weeks
Source
human recombinant
Substrate
fluorogenic HDAC substrate (20 µM)
Measured product fluoro-lysine
Detection method fluorimetry
Reference
trichostatin A (IC 50 : 45 nM)
Strahl, B.D. and Allis, C.D. (2000) Nature, 403: 41-45.
α
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Assay developed in 2010 New assay conditions Human Q Standard turnaround time

159
HDACs ❚
HDAC3
Ref. 2083
Q 3 weeks
Included in:
Non-kinase enzyme profile
Diversity profile
Organ safety profile
Source
human recombinant
Substrate
fluorogenic HDAC substrate (50 µM)
Measured product fluoro-lysine
Detection method fluorimetry
Reference
trichostatin A (IC 50 : 5 nM)
Strahl, B.D. and Allis, C.D. (2000) Nature, 403: 41-45.
enzyme activity (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
trichostatin A
scriptaid
sodium butyrate
α-compound 8
Cerep
services
Receptors
HDAC4
Ref. 2493
Q 3 weeks
Included in:
Non-kinase enzyme profile
Diversity profile
Organ safety profile
Source
human recombinant
Substrate
fluorogenic HDAC substrate class 2a
(20 µM)
Measured product fluoro-lysine
Detection method fluorimetry
Reference
trichostatin A (IC 50 : 3.3 µM)
Strahl, B.D. and Allis, C.D. (2000) Nature, 403: 41-45.
-10 -9 -8 -7 -6 -5 -4 -3
-12 -11 -10 -9 -8 -7 -6 -5 -4
-10 -9 -8 -7 -6
-10 -7 -9 -8 -6 -5 -4
-12 -11 -6 -5
-10 -9 -8 -7
α
Ion
channels
Transporters
HDAC5
Ref. 2494
Q 3 weeks
Source
human recombinant
Substrate
fluorogenic HDAC substrate class 2a (20 µM)
Measured product fluoro-lysine
Detection method fluorimetry
Reference
trichostatin A (IC 50 : 1.3 µM)
Strahl, B.D. and Allis, C.D. (2000) Nature, 403: 41-45.
α
Kinases
Epigenetic &
DNA-related
enzymes
HDAC6
Ref. 2495
Q 3 weeks
Included in:
Non-kinase enzyme profile
Diversity profile
Organ safety profile
Source
human recombinant
Substrate
fluorogenic HDAC substrate (25 µM)
Measured product fluoro-lysine
Detection method fluorimetry
Reference
trichostatin A (IC 50 : 30 nM)
Strahl, B.D. and Allis, C.D. (2000) Nature, 403: 41-45.
α
Other
enzymes
Specialized
cellular
assays
HDAC7
Source
Substrate
Measured product
Detection method
human recombinant
fluorogenic HDAC substrate class 2a
(50 µM)
fluoro-lysine
fluorimetry
α
Standard
profiles
Ref. 2610
Q 3 weeks
Reference
trichostatin A (IC 50 : 2.1 µM)
Strahl, B.D. and Allis, C.D. (2000) Nature, 403: 41-45.
Testing
conditions
HDAC8
Ref. 2247
Q 3 weeks
Source
human recombinant
Substrate
fluorogenic HDAC substrate (400 µM)
Measured product fluoro-lysine
Detection method fluorimetry
Reference
trichostatin A (IC 50 : 400 nM)
Strahl, B.D. and Allis, C.D. (2000) Nature, 403: 41-45.
enzyme activity (% of control)
100
50
trichostatin A
sriptaid
sodium butyrate
0
α-compound 8
-10 -9 -8 -7 -6 -5 -4
-11
log [drug] (M)
Ordering
information
Assay list
& index
-10 -9 -8 -7 -6 -5 -4 -3

160 in vitro pharmacology 2011 catalog
❚ hdacs
HDAC9
Source
Substrate
Measured product
Detection method
human recombinant
fluorogenic HDAC substrate class 2a
(50 µM)
fluoro-lysine
fluorimetry
α
Ref. 2611
Q 3 weeks
Reference
trichostatin A (IC 50 : 3 µM)
Strahl, B.D. and Allis, C.D. (2000) Nature, 403: 41-45.
HDAC10
Ref. 2662
Q 3 weeks
Source
human recombinant
Substrate
fluorogenic HDAC substrate (20 µM)
Measured product fluoro-lysine
Detection method fluorimetry
Reference
trichostatin A (IC 50 : 13 nM)
Strahl, B.D. and Allis, C.D. (2000) Nature, 403: 41-45.
α
HDAC11
Ref. 2663
Q 3 weeks
Included in:
Non-kinase enzyme profile
Diversity profile
Organ safety profile
Source
human recombinant
Substrate
fluorogenic HDAC substrate class 2a
(20 µM)
Measured product fluoro-lysine
Detection method fluorimetry
Reference
scriptaid (IC 50 : 94 µM)
Strahl, B.D. and Allis, C.D. (2000) Nature, 403: 41-45.
α
sirtuin 1 (activator effect)
Source
human recombinant (E. coli)
Substrate
fluorogenic HDAC substrate (200 µM)
Measured product fluoro-lysine
Detection method fluorimetry
Reference
resveratrol (EC 50 : 50 µM)
Ref. 2991
Q 3 weeks
Michan, S. and Sinclair, D. (2007) Biochem. J., 404: 1-13.
sirtuin 1(inhibitor effect)
Ref. 2581
Q 3 weeks
Included in:
Non-kinase enzyme profile
Diversity profile
Organ safety profile
Source
Substrate
Measured product
Detection method
Reference
human recombinant (E. coli)
fluorogenic HDAC substrate (200 µM)
fluoro-lysine
fluorimetry
suramin (IC 50 : 4.5 µM)
Michan, S. and Sinclair, D. (2007) Biochem. J., 404: 1-13.
sirtuin 2
Ref. 2582
Q 3 weeks
Included in:
Non-kinase enzyme profile
Diversity profile
Organ safety profile
Source
human recombinant (E. coli)
Substrate
fluoro-lysine sirtuin 2 deacetylase substrate
(150 µM)
Measured product fluoro-lysine
Detection method fluorimetry
Reference
suramin (IC 50 : 26 µM)
Michan, S. and Sinclair, D. (2007) Biochem. J., 404: 1-13.

161
HDACs ❚
sirtuin 3
Source
Substrate
Measured product
Detection method
human recombinant (E. coli)
fluoro-lysine sirtuin 2 deacetylase substrate
(20 µM)
fluoro-lysine
fluorimetry
Cerep
services
Ref. 2583
Q 3 weeks
Reference
niacinamide (IC 50 : 31 µM)
Michan, S. and Sinclair, D. (2007) Biochem. J., 404: 1-13.
Receptors
Ion
channels
Transporters
Kinases
Epigenetic &
DNA-related
enzymes
Other
enzymes
Specialized
cellular
assays
Standard
profiles
Testing
conditions
Ordering
information
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Assay developed in 2010 New assay conditions Human Q Standard turnaround time
Assay list
& index

162 in vitro pharmacology 2011 catalog
❚ notes
❚ see also ADME-Tox & PK 2011 catalog
ADME-Tox & PK
2011 CATALOG
IN VITRO ADME
Solution properties
Drug absorption/drug transport
Drug metabolism
Drug-drug interactions
IN VITRO TOXICITY
Cardiac toxicity
Cytotoxicity
Genetic toxicity
IN VIVO PK/BIOANALYTICAL
In vivo PK
Bioanalytical
ASSAY SELECTION GUIDE
STANDARD PROFILES
APPLICATION NOTES

163
Cerep
services
Other enzymes
Receptors
Ion
channels
❚ Phosphatases
Transporters
Reversibility of protein tyrosine residue phosphorylation is an important factor in the intra-cellular signalling as phosphorylation induces
conformational changes, creates docking sites for other proteins and causes intracellular relocation. This reversibility relies on the co-ordinated
actions of protein tyrosine kinases and protein tyrosine phosphatases (PTPs).
Protein tyrosine phosphatases are divided in receptor PTPs (rPTPs) and non receptor PTPs (nrPTPs), the dual specificity PTP (dsPTPs) and the
low molecular PTP families. They are involved in cell-substrate adhesion, cell-cell adhesion and insulin signalling as described in Protein
tyrosine phospshatase end signaling, Stoker, A.S. (2005), J. Endocrinol., 185: 19-33.
In this context, Cerep has designed a high throughput profiling platform to determine the inhibitory activity of compounds on the phosphates
superfamily. The robustness, reproducibility and relevance of this platform were determined by screening a panel of commercially available
reference inhibitors in three independent experiments.
Kinases
Epigenetic &
DNA-related
enzymes
phosphatase PP1a
Ref. 2656
Q 3 weeks
Source
human recombinant (E. coli)
Substrate
DIFMUP (250 µM)
Measured product DIFMU
Detection method fluorimetry
Reference
LR-microcystin (IC 50 : 9 nM)
Honkanen, R.E. et al. (1990) J. Biol. Chem., 265: 19401-19404.
Other
enzymes
Specialized
cellular
assays
phosphatase 1B (PTP1B)
Ref. 2593
Q 3 weeks
Included in:
Non-kinase enzyme profile
Diversity profile
Organ safety profile
Source
Substrate
Measured product
Detection method
Reference
human recombinant (E. coli)
DIFMUP (100 µM)
DIFMU
fluorimetry
Welte, S. et al. (2005) Anal. Biochem., 338: 32-38.
ammonium molybdate (IC 50 : 420 nM)
Standard
profiles
Testing
conditions
phosphatase 2A (PP2A)
Source
human recombinant
Substrate
DIFMUP (100 µM)
Measured product DIFMU
Detection method fluorimetry
Ref. 2584
Reference
LR-microcystin (IC 50 : 8.7 nM)
Q 3 weeks
Fontal, O.I. et al. (1999) Anal. Bioch., 269: 289-296.
Ordering
information
Assay list
& index

164 in vitro pharmacology 2011 catalog
❚ phosphatases
phosphatase 2B
Source
Substrate
Measured product
Detection method
bovine brain
pNPP (10 mM)
pNP
photometry
enzyme activity (% of control)
100
50
Ref. 0365
Q 3 weeks
Reference
trifluoperazine (IC 50 : 37 µM)
Pallen, C.J. and Wang, J.H. (1984) J. Biol. Chem., 259: 6134-6141.
0
trifluoperazine
-7 -6 -5 -4 -3
log [drug] (M)
phosphatase CD45
Ref. 2594
Q 3 weeks
Source
human recombinant (yeast)
Substrate
DIFMUP (100 µM)
Measured product DIFMU
Detection method fluorimetry
Reference
ammonium molybdate (IC 50 : 60 nM)
Welte, S. et al. (2005) Anal. Biochem., 338: 32-38.
phosphatase CDC25A
Ref. 2561
Q 3 weeks
Included in:
Non-kinase enzyme profile
Diversity profile
Organ safety profile
Source
Substrate
Measured product
Detection method
Reference
human recombinant (E. coli)
OMFP (20 µM)
OMF
fluorimetry
NSC 663284 (IC 50 : 350 nM)
Tierno, M.B. et al. (2007) Nat. Protoc., 2: 1134-1144.
phosphatase CDC25B
Source
human recombinant (E. coli)
Substrate
OMFP (20 µM)
Measured product OMF
Detection method fluorimetry
Ref. 2541
Reference
NSC 663284 (IC 50 : 500 nM)
Q 3 weeks
Tierno, M.B. et al. (2007) Nat. Protoc., 2: 1134-1144.
phosphatase CDC25C
Source
human recombinant (E. coli)
Substrate
OMFP (20 µM)
Measured product OMF
Detection method fluorimetry
Ref. 2562
Reference
NSC 663284 (IC 50 : 410 nM)
Q 3 weeks
Tierno, M.B. et al. (2007) Nat. Protoc., 2: 1134-1144.
phosphatase DEP1 (PTPRJ)
Source
human recombinant (E. coli)
Substrate
DIFMUP (150 µM)
Measured product DIFMU
Detection method fluorimetry
Ref. 2801
Reference
ammonium molybdate (IC 50 : 240 nM)
Q 3 weeks
Welte, S. et al. (2005) Anal. biochem., 338: 32-38.

165
phosphatases ❚
phosphatase LAR (PTPRF)
Source
Substrate
Measured product
Detection method
human recombinant (E. coli)
DIFMUP (150 µM)
DIFMU
fluorimetry
Cerep
services
Ref. 2803
Q 3 weeks
Reference
ammonium molybdate (IC 50 : 300 nM)
Welte, S. et al. (2005) Anal. biochem., 338: 32-38.
Receptors
phosphatase MEG1 (PTPN4)
Source
human recombinant (E. coli)
Substrate
DIFMUP (30 µM)
Measured product DIFMU
Detection method fluorimetry
Ref. 2807
Reference
ammonium molybdate (IC 50 : 800 nM)
Q 3 weeks
Welte, S. et al. (2005) Anal. biochem., 338: 32-38.
phosphatase MEG2 (PTPN9)
Source
human recombinant (E. coli)
Substrate
DIFMUP (150 µM)
Measured product DIFMU
Detection method fluorimetry
Ref. 2808
Reference
ammonium molybdate (IC 50 : 310 nM)
Q 3 weeks
Welte, S. et al. (2005) Anal. biochem., 338: 32-38.
Ion
channels
Transporters
Kinases
Epigenetic &
DNA-related
enzymes
phosphatase MKP1
Ref. 2652
Q 3 weeks
Source
human recombinant
Substrate
DIFMUP (100 µM)
Measured product DIFMU
Detection method fluorimetry
Reference
NSC 663284 (IC 50 : 8.2 µM)
Lazo, J.S. et al. (2007) J. Pharmacol. Exp. Ther., 322: 940-947.
Other
enzymes
Specialized
cellular
assays
phosphatase MKP2
Ref. 2653
Q 3 weeks
Source
human recombinant
Substrate
DIFMUP (100 µM)
Measured product DIFMU
Detection method fluorimetry
Reference
NSC 663284 (IC 50 : 35.5 µM)
Chen, P. et al. (2001) J. Biol. Chem., 27: 29440-29449.
Standard
profiles
Testing
conditions
phosphatase MKP3
Ref. 2654
Q 3 weeks
Source
human recombinant
Substrate
DIFMUP (100 µM)
Measured product DIFMU
Detection method fluorimetry
Reference
NSC 663284 (IC 50 : 5.2 µM)
Fjeld, C.C. et al. (2000) J. Biol. Chem., 275: 6749-6757.
Ordering
information
Assay list
& index

166 in vitro pharmacology 2011 catalog
❚ phosphatases
phosphatase MKP6
Ref. 2655
Q 3 weeks
Source
human recombinant
Substrate
DIFMUP (100 µM)
Measured product DIFMU
Detection method fluorimetry
Reference
NSC 663284 (IC 50 : 18.5 µM)
Marti, F. et al. (2001) J. Immunol., 166: 197-206.
phosphatase PEST (PTPN12)
Source
human recombinant (E. coli)
Substrate
DIFMUP (150 µM)
Measured product DIFMU
Detection method fluorimetry
Ref. 2809
Reference
ammonium molybdate (IC 50 : 440 nM)
Q 3 weeks
Welte, S. et al. (2005) Anal. biochem., 338: 32-38.
phosphatase PTPb (PTPRB)
Source
human recombinant (E. coli)
Substrate
DIFMUP (60 µM)
Measured product DIFMU
Detection method fluorimetry
Ref. 2802
Reference
ammonium molybdate (IC 50 : 123 nM)
Q 3 weeks
Welte, S. et al. (2005) Anal. biochem., 338: 32-38.
phosphatase PTPg (PTPRG)
Source
human recombinant (E. coli)
Substrate
DIFMUP (100 µM)
Measured product DIFMU
Detection method fluorimetry
Ref. 2804
Reference
ammonium molybdate (IC 50 : 680 nM)
Q 3 weeks
Welte, S. et al. (2005) Anal. biochem., 338: 32-38.
phosphatase PTPµ (PTPRM)
Source
human recombinant (E. coli)
Substrate
DIFMUP (150 µM)
Measured product DIFMU
Detection method fluorimetry
Ref. 2805
Reference
ammonium molybdate (IC 50 : 200 nM)
Q 3 weeks
Welte, S. et al. (2005) Anal. biochem., 338: 32-38.
phosphatase SHP1 (PTPN6)
Source
human recombinant (E. coli)
Substrate
DIFMUP (100 µM)
Measured product DIFMU
Detection method fluorimetry
Ref. 2597
Reference
ammonium molybdate (IC 50 : 3.2 µM)
Q 3 weeks
Welte, S. et al. (2005) Anal. Biochem., 338: 32-38.

167
phosphatase SHP2 (PTPN11)
Source
human recombinant
Substrate
DIFMUP (100 µM)
Measured product DIFMU
Detection method fluorimetry
Ref. 2533
Reference
ammonium molybdate (IC 50 : 160 nM)
Q 3 weeks
Welte, S. et al. (2005) Anal. Biochem., 338: 32-38.
phosphatase TC-PTP (PTPN2)
Source
human recombinant (E. coli)
Substrate
DIFMUP (30 µM)
Measured product DIFMU
Detection method fluorimetry
Ref. 2806
Reference
ammonium molybdate (IC 50 : 700 nM)
Q 3 weeks
Welte, S. et al. (2005) Anal. biochem., 338: 32-38.
phosphatase VHR (DUSP3)
Source
human recombinant
Substrate
DIFMUP (100 µM)
Measured product DIFMU
Detection method fluorimetry
Ref. 2598
Reference
ammonium molybdate (IC 50 : 11.5 µM)
Q 3 weeks
Denu, J.M. and Dixon, J.E. (1995) Proc. Natl. Acad. Sci. USA, 92: 5910-5914.
❚ Proteases
phosphatases ❚
Cerep
services
Receptors
Ion
channels
Transporters
Kinases
Epigenetic &
DNA-related
enzymes
Other
enzymes
cathepsin G
❚ Serine protease
Ref. 0179
Q 4 weeks
Source
human leukocytes
Substrate
N-SAAPF-pNa (1 mM)
Measured product pNa
Detection method photometry
Reference
3’,4’dichloroisocoumarin (IC 50 : 60 µM)
Nakajima, K. and Powers, J. C. (1979) J. Biol. Chem., 254: 4027-4032.
enzyme activity (% of control)
100
50
3',4'dichloroisocoumarin
0
PMSF
-7 -6 -5 -4 -3
log [drug] (M)
Specialized
cellular
assays
Standard
profiles
dipeptidyl peptidase IV (DPP-IV)
Source
human recombiant
Substrate
GP-AMC, fluorogenic substrate (40 µM)
Measured product aminomethyl coumarin
❚ Serine protease
Detection method fluorimetry
Ref. 2942
Reference
K579 (IC 50 : 3.7 nM)
Q 3 weeks
Takasaki, K. et al. (2004) Eur. J. Pharmacol., 486: 335-342.
Testing
conditions
Ordering
information
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Assay developed in 2010 New assay conditions Human Q Standard turnaround time
Assay list
& index

168 in vitro pharmacology 2011 catalog
❚ proteases [serine proteases]
elastase
❚ Serine protease
Ref. 0183
Q 3 weeks
Included in:
Non-kinase enzyme profile
Organ safety profile
Source
Substrate
Measured product
Detection method
Reference
human leukocytes
MeOSAAPV-pNa (0.1 mM)
pNa
photometry
3’,4’dichloroisocoumarin (IC 50 : 392 nM)
Adeyemi, E.O. et al. (1990) J. Pharm. Pharmacol., 42: 487-490.
enzyme activity (% of control)
100
50
0
-8 -7 -6 -5 -4 -3
log [drug] (M)
3',4'dichloroisocoumarin
PMSF
NDGA
HNE (human neutrophil elastase)
Source
human serum
Substrate
elastin fluorescein (1 mg)
Measured product fluorescein
❚ Serine protease
Detection method fluorimetry
Ref. 0562
Reference
3’,4’dichloroisocoumarin (IC 50 : 520 nM)
Q 4 weeks
McGillivray, D. H. et al. (1981) Clin. Chim. Acta., 111: 289-294.
enzyme activity (% of control)
100
50
3',4'dichloroisocoumarin
0
PMSF
-11 -10 -9 -8 -7 -6 -5 -4 -3 -2
log [drug] (M)
kallikrein
❚ Serine protease
Ref. 0791
Q 4 weeks
Included in:
Organ safety profile
Source
human plasma
Substrate
HDPFR-pNa (50 µM)
Measured product pNa
Detection method photometry
Reference
soybean trypsin inhibitor (IC 50 : 6 nM)
Nagase, H and Barrett, A.J. (1981) Biochem. J., 193: 187-192.
tryptase
❚ Serine protease
Ref. 0512
Q 3 weeks
Included in:
Non-kinase enzyme profile
Organ safety profile
Source
human lung
Substrate
N-p-Tosyl-GPR-pNa (0.1 mM)
Measured product pNa
Detection method photometry
Reference
leupeptin (IC 50 : 1 µM)
Schwartz, L.B. and Bradford, T.R. (1986) J. Biol. Chem., 261: 7372-7379.
caspase-1
100
❚ Cysteine protease
Ref. 3251
Q 3 weeks
Source
human recombinant (E. coli)
Substrate
benzyloxycarbonyl-YVAD-AFC (7.5 µM)
Measured product AFC
Detection method fluorimetry
Reference
Ac-YVAD-CHO (IC 50 : 20 nM)
Margolin, N. et al.(1997) J. Biol. Chem., 272: 7223-7228.
enzyme activity (% of control)
50
0
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
Ac-YVAD-CHO
Ac-DEVD-CHO
Ac-LEHD-CHO
Ac-IETD-CHO
caspase-2
❚ Cysteine protease
Ref. 0681
Q 6 weeks
Source
human recombinant (E. coli)
Substrate
benzyloxycarbonyl-VDVAD-AFC (10 µM)
Measured product AFC
Detection method fluorimetry
Reference
Ac-VDVAD-CHO (IC 50 : 130 nM)
Talanian, R.V. et al. (1997) J. Biol. Chem., 272: 9677-9682.
-10 -9 -8 -7 -6 -5 -4 -3
-11
-10 -9 -8 -7 -6 -5 -4 -3
-12 -11 -10 -9 -8 -7 -6 -5 -4
-11 -10 -9 -8 -7 -6 -5 -4 -3 -2
-10 -9 -8 -7 -6
-10 -9 -8 -7 -6 -5
-4
-12 -11 -10 -9
-8 -7 -6 -5 -4 -3
-12 -11 -10 -9 -8 -7 -6 -5
-11
-10 -9 -8 -7 -6 -5 -4

169
caspase-3
❚ Cysteine protease
Ref. 0774
Q 3 weeks
Included in:
Non-kinase enzyme profile
BioPrint ® profile
Organ safety profile
Source
human recombinant (E. coli)
Substrate
benzyloxycarbonyl-DEVD-AFC (3.6 µM)
Measured product AFC
Detection method fluorimetry
Reference
Ac-DEVD-CHO (IC 50 : 1.6 nM)
Mittl, P.R.E. et al. (1997) J. Biol. Chem., 272: 6539-6547.
proteases [cysteine proteases] ❚
enzyme activity (% of control)
100
50
Ac-DEVD-CHO
Ac-DMQD-CHO
0
Ac-YVAD-CHO
-12 -11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
Cerep
services
Receptors
caspase-6
❚ Cysteine protease
Ref. 0908
Q 4 weeks
Included in:
Organ safety profile
Source
human recombinant (E. coli)
Substrate
benzyloxycarbonyl-VEID-AFC (10 µM)
Measured product AFC
Detection method fluorimetry
Reference
Ac-VEID-CHO (IC 50 : 31 nM)
Talanian, R.V. et al. (1997) J. Biol. Chem., 272: 9677-9682.
enzyme activity (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
Ac-VEID-CHO
Ac-DEVD-CHO
Ac-YVAD-CHO
Ion
channels
Transporters
caspase-7
❚ Cysteine protease
Ref. 0909
Q 6 weeks
Source
human recombinant (E. coli)
Substrate
benzyloxycarbonyl-DEVD-AFC (30 µM)
Measured product AFC
Detection method fluorimetry
Reference
Ac-DEVD-CHO (IC 50 : 10 nM)
Talanian, R.V. et al. (1997) J. Biol. Chem., 272: 9677-9682.
enzyme activity (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
Ac-DEVD-CHO
Ac-VEID-CHO
Ac-YVAD-CHO
Kinases
Epigenetic &
DNA-related
enzymes
caspase-8
❚ Cysteine protease
Ref. 0668
Q 3 weeks
Included in:
Non-kinase enzyme profile
Organ safety profile
Source
human recombinant (E. coli)
Substrate
benzyloxycarbonyl-IETD-AFC (10 µM)
Measured product AFC
Detection method fluorimetry
Reference
Ac-IETD-CHO (IC 50 : 29 nM)
Karahashi, H. and Amano, F. (2000) Biol. Pharm. Bull., 23: 140-144.
enzyme activity (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5
log [drug] (M)
Ac-IETD-CHO
Ac-VEID-CHO
Ac-DEVD-CHO
Other
enzymes
Specialized
cellular
assays
caspase-9
❚ Cysteine protease
Ref. 0675
Q 3 weeks
Included in:
BioPrint ® profile
Organ safety profile
Source
human recombinant (E. coli)
Substrate
Acetyl-LEHD-AFC (25 µM)
Measured product AFC
Detection method fluorimetry
Reference
Ac-LEHD-CHO (IC 50 : 200 nM)
Thornberry, N.A. et al. (1997) J. Biol. Chem., 272: 17907-17911.
Standard
profiles
Testing
conditions
caspase-10
❚ Cysteine protease
Ref. 0910
Q 4 weeks
Source
human recombinant (E. coli)
Substrate
Acetyl-LEHD-AFC (80 µM)
Measured product AFC
Detection method fluorimetry
Reference
Ac-LEHD-CHO (IC 50 : 240 nM)
Thornberry, N.A. et al. (1997) J. Biol. Chem., 272: 17907-17911.
Ordering
information
Assay list
& index

170 in vitro pharmacology 2011 catalog
❚ proteases [cysteine proteases]
cathepsin B
❚ Cysteine protease
Ref. 0178
Q 3 weeks
Source
human placenta
Substrate
Z-RR-pNa (0.3 mM)
Measured product pNa
Detection method photometry
Reference
leupeptin (IC 50 : 17.7 nM)
Barrett, A.J. and Kirschke, H. (1981) Meth. Enzymol., 80: 535-561
enzyme activity (% of control)
100
50
0
-9 -8 -7 -6 -5 -4
log [drug] (M)
leupeptin
3',4' dichloroisocoumarin
cathepsin H
❚ Cysteine protease
Ref. 0801
Q 6 weeks
Source
human liver
Substrate
H-R-AMC (20 µM)
Measured product AMC
Detection method fluorimetry
Reference
leupeptin (IC 50 : 7.3 µM)
Barrett, A.J. and Kirschke, H. (1981) Meth. Enzymol., 80: 535-561.
enzyme activity (% of control)
100
50
0
leupeptin
E-64
cathepsin
inhibitor III
-10 -9 -8 -7 -6 -5 -4 -3
log [drug] (M)
cathepsin L
❚ Cysteine protease
Ref. 0802
Q 3 weeks
Included in:
Non-kinase enzyme profile
Organ safety profile
Source
human liver
Substrate
Z-FR-AMC (15 µM)
Measured product AMC
Detection method fluorimetry
Reference
leupeptin (IC 50 : 1.9 nM)
Barrett, A.J. and Kirschke, H. (1981) Meth. Enzymol., 80: 535-561.
enzyme activity (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5
log [drug] (M)
leupeptin
cathepsin
inhibitor II
cathepsin
inhibitor III
cathepsin X
❚ Cysteine protease
Ref. 0931
Q 4 weeks
Included in:
Organ safety profile
Source
human recombinant (NS0 cells)
Substrate
Mca-RPPGFSAFK(Dnp)-OH (10 µM)
Measured product Mca-peptides
Detection method fluorimetry
Reference
leupeptin (IC 50 : 240 nM)
Therrien, C. et al. (2001) Biochemistry, 40: 2702-2711.
BACE-1 (β-secretase)
❚ Aspartic protease
Ref. 0701
Q 3 weeks
Included in:
Non-kinase enzyme profile
BioPrint ® profile
Organ safety profile
Source
human recombinant (murine cells)
Substrate
Mca-SEVNLDAEFRK(Dnp)-RR-NH 2 (6 µM)
Measured product Mca-SEVNL-NH 2
Detection method fluorimetry
Reference
OM 99-2 (IC 50 : 110 nM)
Ermolieff, J. et al. (2000) Biochemistry, 39: 12450-12456.
enzyme activity (% of control)
100
50
0
-10 -9 -8 -7 -6 -5
log [drug] (M)
OM 99-2
APP β-secretase
inhibitor
cathepsin D
❚ Aspartic protease
Ref. 0650
Q 3 weeks
Included in:
Non-kinase enzyme profile
Organ safety profile
Source
human liver
Substrate
Moc-Ac-GKPIFFRLK(DNP)-D-Arg-NH 2 (8 µM)
Measured product Moc-Ac-GKPIF
Detection method fluorimetry
Reference
pepstatin A (IC 50 : 1.9 nM)
Yasuda, Y. et al. (1999) J. Biochem., 125: 1137-1143.
enzyme activity (% of control)
100
50
0
-13-12 -11-10 -9 -8 -7 -6 -5 -4 -3 -2
log [drug] (M)
pepstatin
leupeptin
A

171
proteases [aspartic proteases] ❚
cathepsin E
❚ Aspartic protease
Ref. 1001
Q 4 weeks
Included in:
Organ safety profile
Source
mouse recombinant (NS0 cells)
Substrate
Mca-PLGL-Dpa-AR-NH 2 (6 µM)
Measured product Mca-peptides
Detection method fluorimetry
Reference
pepstatin A (IC 50 : 2.6 nM)
Yasuda, Y. et al. (1999) J. Biochem., 125: 1137-1143.
Cerep
services
Receptors
HIV-1 protease
❚ Aspartic protease
Ref. 0346
Q 3 weeks
Included in:
Non-kinase enzyme profile
BioPrint ® profile
Source
human recombinant (E. coli)
Substrate
antranilyl-HIV (75 µM)
Measured product N-terminal tripeptide
Detection method fluorimetry
Reference
pepstatin A (IC 50 : 3 µM)
Toth, M.V. and Marshall, G.R. (1990) Int. J. Protein Res., 36: 544-550.
enzyme activity (% of control)
100
50
0
-8 -7 -6 -5 -4 -3
log [drug] (M)
pepstatin A
warfarin
Ion
channels
Transporters
ACE
❚ Metalloprotease
Ref. 0979
Q 3 weeks
Included in:
Non-kinase enzyme profile
BioPrint ® profile
Organ safety profile
Source
human recombinant (murine cells)
Substrate
Mca-RPPGFSAFK(DNP)-OH (10 µM)
Measured product Mca-peptides
Detection method fluorimetry
Reference
captopril (IC 50 : 3.1 nM)
Hoorn, C.M. and Roth, R.A. (1993) Brit. J. Pharmacol., 110: 597-602.
Kinases
Epigenetic &
DNA-related
enzymes
ACE
❚ metalloprotease
tissue
Ref. 0302
Q 4 weeks
Source
rabbit aorta
Agonist angiotensin-I (pD 2 = 7.9)
Antagonist captopril (pA 2 = 8.7)
Test concentrations
[Solvent] must be kept ≤ 0.1%
3 concentrations, n=2 (2 tissues) for both
activities
Kuroda, K. et al. (1990) Arzneim.-Forsch. Drug Res., 40: 968-973.
tension (% of max.)
100
50
0
-10 -9 -8 -7
log [agonist] (M)
captopril
none
1 nM
3 nM
10 nM
Other
enzymes
Specialized
cellular
assays
ACE-2
❚ metalloprotease
Ref. 1954
Q 3 weeks
Included in:
Non-kinase enzyme profile
BioPrint ® profile
Organ safety profile
Source
Substrate
Measured product
Detection method
Reference
human recombinant (murine cells)
Mca-YVADPAK(DNP)-OH (10 µM)
Mca-peptides
fluorimetry
AC-GG-26-NH 2 (IC 50 : 400 nM)
Huang, L. et al. (2003) J. Biol. Chem., 278: 15532-15540.
enzyme activity (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4 -3 -2
log [drug] (M)
AC-GG-26-NH 2
captopril
EDTA
chloro-2-
benzene
Standard
profiles
Testing
conditions
ECE-1
❚ metalloprotease
Ref. 0184
Q 3 weeks
Included in:
Non-kinase enzyme profile
Organ safety profile
Source
human recombinant (NSO cells)
Substrate
ECE-1 fluorescent substrate (15 µM)
Measured product Mca-RPPGFSA
Detection method fluorimetry
Reference
phosphoramidon (IC 50 : 31 nM)
Ahn, K. et al. (1998) Arch. Biochem. Biophys., 359: 258-268.
enzyme activity (% of control)
100
50
0
-10 -9 -8 -7 -6 -5 -4 -3
log [drug] (M)
phosphoramidon
phenanthroline
thiorphan
captopril
Ordering
information
Assay list
& index

172 in vitro pharmacology 2011 catalog
❚ proteases [metalloproteases]
ECE-1
❚ metalloprotease
tissue
Ref. 0313
Q 4 weeks
Source
rabbit saphenous artery
Agonist big endothelin-1 (pD 2 = 8.5)
Antagonist phosphoramidon (pA 2 = 8)
Test concentrations
[Solvent] must be kept ≤ 0.1%
3 concentrations, n=2 (2 tissues)
for both activities
Auguet, M. et al. (1992) Eur. J. Pharmacol., 224: 101-102.
tension (% of max.)
100
50
0
-9 -8 -7
log [agonist] (M)
phosphoramidon
none
0.01 µM
0.1 µM
1 µM
MMP-1
❚ metalloprotease
Ref. 0510
Q 3 weeks
Included in:
Non-kinase enzyme profile
BioPrint ® profile
Organ safety profile
Source
human recombinant (E. coli)
Substrate DNP-P-Cha-GC(Me)-HAK(n-Me-Abz)-NH 2
(10 µM)
Measured product Cys(Me)-HAK(n-Me-Abz)-NH 2
Detection method
Reference
fluorimetry
GM6001 (IC 50 : 1.9 nM)
Bickett, D.A. et al. (1993) Anal. Biochem., 212: 58-64.
enzyme activity (% of control)
100
50
0
-12 -11 -10 -9 -8 -7
log [drug] (M)
GM 6001
TIMP-1
TIMP-2
MMP-2
❚ metalloprotease
Ref. 0489
Q 3 weeks
Included in:
BioPrint ® profile
Source
human recombinant
Substrate
NFF-2 (10 µM)
Measured product Mca-RPKPYA
Detection method fluorimetry
Reference
GM6001 (IC 50 : 1.6 nM)
Nagase, N. et al. (1994) J. Biol. Chem., 269: 20952-20957.
enzyme activity (% of control)
100
50
0
-11 -10 -9 -8 -7
log [drug] (M)
GM 6001
TIMP-2
TIMP-1
MMP-3
❚ metalloprotease
Ref. 0490
Q 3 weeks
Included in:
Non-kinase enzyme profile
Source
human recombinant
Substrate
NFF-2 (10 µM)
Measured product Mca-RPKPYA
Detection method fluorimetry
Reference
GM6001 (IC 50 : 35 nM)
Nagase, N. et al. (1994) J. Biol. Chem., 269: 20952-20957.
enzyme activity (% of control)
100
50
GM 6001
0
TIMP-1
TIMP-2
-12 -11 -10 -9 -8 -7 -6
log [drug] (M)
MMP-7
❚ metalloprotease
Ref. 0502
Q 3 weeks
Source
human recombinant (E. coli)
Substrate
MMP-2/MMP-7 substrate (5 µM)
Measured product Mca-PLG
Detection method fluorimetry
Reference
GM6001 (IC 50 : 11 nM)
Quesada, A.R. et al. (1997) Clin. Exp. Metastasis, 15: 26-32.
MMP-8
❚ metalloprotease
Ref. 0643
Q 6 weeks
Source
human neutrophils
Substrate
Mca-P-Cha-G-Nva-HA-Dpa-NH 2 (1 µM)
Measured product Mca-P-Cha-G
Detection method fluorimetry
Reference
GM6001 (IC 50 : 0.3 nM)
Knauper, V. et al. (1996) J. Biol. Chem., 271: 1544-1550.

173
proteases [metalloproteases] ❚
MMP-9
❚ metalloprotease
Ref. 0491
Q 3 weeks
Included in:
Non-kinase enzyme profile
BioPrint ® profile
Source
human recombinant
Substrate
NFF-2 (10 µM)
Measured product Mca-RPKPYA
Detection method fluorimetry
Reference
GM6001 (IC 50 : 1.1 nM)
Nagase, N. et al. (1994) J. Biol. Chem., 269: 20952-20957.
enzyme activity (% of control)
100
50
0
-12 -11 -10 -9 -8 -7
log [drug] (M)
GM 6001
TIMP-1
TIMP-2
Cerep
services
Receptors
MMP-12
❚ metalloprotease
Ref. 0511
Q 6 weeks
Source
Substrate
Measured product
Detection method
Reference
human recombinant
MMP fluorescent substrate (10 µM)
Dnp-AG
fluorimetry
GM6001 (IC 50 : 0.75 nM)
Hiller, O. et al. (2000) J. Biol. Chem., 275: 33008-33013.
enzyme activity (% of control)
100
-10 -9 -8 -7 -6 -5 -4
50
-11 -10 -9 -8 -7 -6
GM 6001
NNGH
0
TIMP-1
-12 -11 -10 -9 -8 -7 -6
log [drug] (M)
Ion
channels
Transporters
MMP-13
❚ metalloprotease
Ref. 0632
Q 6 weeks
Source
Substrate
Measured product
Detection method
Reference
human recombinant
(Spodoptera frugiperda)
MMP-13 substrate (2 µM)
Mca-P-Cha-G
fluorimetry
GM6001 (IC 50 : 0.31 nM)
Knauper, V. et al. (1996) J. Biol. Chem., 271: 1544-1550.
-10 -9 -8 -7 -6 -5 -4
-11 -10 -9 -8 -7 -6
-12 -11 -10 -6
-9 -8 -7
Kinases
Epigenetic &
DNA-related
enzymes
MT1-MMP (MMP-14)
❚ metalloprotease
Ref. 0670
Q 3 weeks
Source
human recombinant
Substrate
MMP-14 substrate (2 µM)
Measured product Mca-PLA
Detection method fluorimetry
Reference
GM6001 (IC 50 : 3.1 nM)
Mucha, A. et al. (1998) J. Biol. Chem., 273: 2763-2768.
Other
enzymes
Specialized
cellular
assays
neutral endopeptidase
❚ metalloprotease
Ref. 0509
Q 3 weeks
Included in:
Non-kinase enzyme profile
BioPrint ® profile
Organ safety profile
Source
Substrate
Measured product
Detection method
Reference
HUV-EC-C cells
DAGNPG (50 µM)
Dansyl-D-AG
fluorimetry
thiorphan (IC 50 : 0.94 nM)
Graf, K. et al. (1998) Basic Res. Cardiol., 93: 11-17.
Standard
profiles
Testing
conditions
TACE
❚ metalloprotease
Ref. 0702
Q 3 weeks
Included in:
Non-kinase enzyme profile
Organ safety profile
Source
human recombinant (insect cells)
Substrate
TACE substrate II (4 µM)
Measured product Mca-PLAQA
Detection method fluorimetry
Reference
GM6001 (IC 50 : 40 nM)
Van Dyk, D.E. et al. (1997) Bioorg. Med. Chem. Lett., 7: 1219-1224.
enzyme activity (% of control)
100
50
0
-11 -10 -9 -8 -7 -6
log [drug] (M)
GM 6001
Ordering
information
Assay list
& index

174 in vitro pharmacology 2011 catalog
❚ Phosphodiesterases
Cyclic nucleotide phosphodiesterases (PDEs), ubiquitously distributed in mammalian tissues, play a major role in cell signaling by hydrolyzing
cAMP and/or cGMP. Due to their diversity and specific distribution at cellular and subcellular levels, PDEs can selectively regulate various
cellular functions. Increased understanding of their function at the cell and molecular level provides an impetus for the development of
isoenzyme selective inhibitors for the treatment of various diseases. Examples are PDE3 inhibitors for congestive heart failure, PDE4 inhibitors
for inflammatory airways disease and the most well known, inhibitor for erectile dysfunction (Viagra).
As PDEs are expressed in a variety of tissues, selectivity is a prerequisite for a therapeutically applicable PDE inhibitor. As an example, high
selectivity for PDE5 inhibitors is important for treatment of erectile dysfunction to minimize the possibility of side effects that arise as a result
of inhibition of other PDEs. Possible side effects include heart rate increase and vasodilation that are attributed to inhibition of PDE1 and
PDE3, or blue-green vision disturbances that are attributed to inhibition of PDE6.
In this context, Cerep has designed a high throughput profiling platform to determine the inhibitory activity and selectivity of compounds
on the PDE superfamily
The robustness, reproducibility and relevance of this platform was determined by screening a broad panel of commercially available reference
inhibitors and known clinical drugs in three independent experiments. Poster available upon request.
❚ For cellular phosphodiesterase assays, please contact us at customresarch@cerep.com
PDE1B
Ref. 2431
Q 3 weeks
Included in:
Diversity profile
Organ safety profile
PDE high-throughput profile
Source
human recombinant (Sf9 cells)
Substrate
cGMP (240 nM)
Measured product residual cGMP
Detection method HTRF
Reference
calmidazolium (IC 50 : 2.2 µM)
Bender, A.T. and Beavo, J.A. (2006) Pharmacol. Rev., 58: 488-520.
PDE2A
Ref. 2426
Q 3 weeks
Included in:
Non-kinase enzyme profile
Diversity profile
BioPrint ® profile
Organ safety profile
PDE high-throughput profile
Source
human recombinant (Sf9 cells)
Substrate
cAMP (40 nM)
Measured product residual cAMP
Detection method HTRF
Reference
EHNA (IC 50 : 1.56 µM)
Bender, A.T. and Beavo, J.A. (2006) Pharmacol. Rev., 58: 488-520.
PDE3A
Ref. 2432
Q 3 weeks
Included in:
Non-kinase enzyme profile
Diversity profile
Organ safety profile
PDE high-throughput profile
Source
human recombinant (Sf9 cells)
Substrate
cAMP (40 nM)
Measured product residual cAMP
Detection method HTRF
Reference
milrinone (IC 50 : 270 nM)
Bender, A.T. and Beavo, J.A. (2006) Pharmacol. Rev., 58: 488-520.
enzyme activity (% of control)
100
50
0
-12 -11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
milrinone
cilostamide
trequinsin
rolipram
PDE3B
Ref. 2705
Q 3 weeks
Included in:
BioPrint ® profile
PDE high-throughput profile
Source
human recombinant (Sf9 cells)
Substrate
cAMP (40 nM)
Measured product residual cAMP
Detection method HTRF
Reference
milrinone (IC 50 : 510 nM)
Bender, A.T. and Beavo, J.A. (2006) Pharmacol. Rev., 58: 488-520.
-10 -9 -8 -7 -6 -5 -4 -3
-12 -11 -10 -9 -8 -7 -6 -5 -4
-10 -9 -8 -7 -6
-10 -7 -9 -8 -6 -5 -4
-12 -11 -10 -6 -5
-9 -8 -7

phosphodiesterases ❚
175
PDE4A 1A
Ref. 2342
Q 3 weeks
Included in:
Organ safety profile
PDE high-throughput profile
Source
human recombinant (Sf9 cells)
Substrate
cAMP (40 nM)
Measured product residual cAMP
Detection method HTRF
Reference
rolipram (IC 50 : 77 nM)
Saldou, N. et al. (1998) Cell signal., 10: 427-440.
Cerep
services
Receptors
PDE4B 1
Ref. 2413
Q 3 weeks
Included in:
Organ safety profile
PDE high-throughput profile
Source
human recombinant (Sf9 cells)
Substrate
cAMP (40 nM)
Measured product residual cAMP
Detection method HTRF
Reference
rolipram (IC 50 : 46 nM)
Saldou, N. et al. (1998) Cell signal., 10: 427-440.
Ion
channels
Transporters
PDE4D 2
Ref. 2434
Q 3 weeks
Included in:
Non-kinase enzyme profile
Diversity profile
BioPrint ® profile
Organ safety profile
PDE high-throughput profile
Source
human recombinant (Sf9 cells)
Substrate
cAMP (40 nM)
Measured product residual cAMP
Detection method HTRF
Reference
rolipram (IC 50 : 48 nM)
Saldou, N. et al. (1998) Cell signal., 10: 427-440.
Kinases
Epigenetic &
DNA-related
enzymes
PDE5 (non-selective)
Ref. 0204
Q 3 weeks
Included in:
Non-kinase enzyme profile
Diversity profile
BioPrint ® profile
Organ safety profile
PDE high-throughput profile
Source
human platelets
Substrate
[ 3 H]cGMP + cGMP (1 µM)
Measured product [ 3 H]5'GMP
Detection method scintillation counting
Reference
dipyridamole (IC 50 : 700 nM)
Weishaar, R.E. et al. (1986) Biochem. Pharmacol., 35: 787-800.
Other
enzymes
Specialized
cellular
assays
PDE6 (non-selective)
Ref. 0478
Q 3 weeks
Included in:
Non-kinase enzyme profile
BioPrint ® profile
PDE high-throughput profile
Source
bovine retina
Substrate
[ 3 H]cGMP + cGMP (2 µM)
Measured product [ 3 H]5’GMP
Detection method scintillation counting
Reference
zaprinast (IC 50 : 212 nM)
Ballard, A. S. et al. (1998) J. Urol., 159: 2164-2171.
enzyme activity (% of control)
100
50
zaprinast
dipyridamole
IBMX
0
milrinone
-8 -7 -6 -5 -4
-9
log [drug] (M)
Standard
profiles
Testing
conditions
PDE7A
Ref. 2351
Q 3 weeks
Included in:
Organ safety profile
PDE high-throughput profile
Source
human recombinant (Sf9 cells)
Substrate
cAMP (40 nM)
Measured product residual cAMP
Detection method HTRF
Reference
BRL 50481 (IC 50 : 617 nM)
Smith, S.J. et al. (2004) Mol. Pharm., 66: 1679-1689
-10 -9 -8 -7 -6 -5 -4
-11 -10 -9 -8 -7 -6
-12 -11 -10 -6
-9 -8 -7
Ordering
information
Assay list
& index

176 in vitro pharmacology 2011 catalog
❚ phosphodiesterases
PDE8A
Ref. 2355
Q 3 weeks
Included in:
PDE high-throughput profile
Source
human recombinant (Sf9 cells)
Substrate
cAMP (40 nM)
Measured product residual cAMP
Detection method HTRF
Reference
dipyridamole (IC 50 : 10.68 µM)
Fisher, D.A. et al. (1998) Biochem., 246: 570-577.
PDE10A 1
Ref. 2357
Q 3 weeks
Included in:
Organ safety profile
PDE high-throughput profile
Source
human recombinant (Sf9 cells)
Substrate
cAMP (40 nM)
Measured product residual cAMP
Detection method HTRF
Reference
papaverine (IC 50 : 88 nM)
Soderling, S.H. et al. (1999) Proc. Natl. Acad. Sci. USA, 96: 7071-7076.
PDE11A 4
Ref. 2358
Q 3 weeks
Included in:
PDE high-throughput profile
Source
human recombinant (Sf9 cells)
Substrate
cAMP (40 nM)
Measured product residual cAMP
Detection method HTRF
Reference
dipyridamole (IC 50 : 830 nM)
Fawcett, L. et al. (2000) Proc. Natl. Acad. Sci. USA, 97: 3702-3707.
rolipram - antagonist radioligand
Source
mouse brain
Ligand
[ 3 H]rolipram (1 nM)
Kd
1 nM
Non specific rolipram (10 µM)
binding
Reference
rolipram (IC 50 : 0.98 nM)
Ref. 0379
Q 3 weeks
Duplantier, A.J. et al. (1996) J. Med. Chem., 39: 120-125.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5
log [drug] (M)
rolipram
Ro 20-1724
diazepam
❚ No synthases
-10 -9 -8 -7 -6 -5 -4
-11 -10 -9 -8 -7 -6
inducible NOS
-12 -11 -10 -9 -8 -7 -6
Ref. 3185
Q 3 weeks
Included in:
Non-kinase enzyme profile
BioPrint ® profile
Organ safety profile
Source
mouse recombinant (E. coli)
Substrate
L-arginine (200 µM)
Measured product
-
NO 2
Detection method photometry
Reference
1400W (IC 50 : 20 nM)
Tayeh, M. A. and Marletta, M.A. (1989) J. Biol. Chem., 264: 19654-19658.
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Assay developed in 2010 New assay conditions Human Q Standard turnaround time

177
no synthases ❚
inducible NOS
cellul ar
Ref. 0194
[Custom offer]
Please contact us at:
customresearch@cerep.com
Source
constitutive NOS (cerebellar)
Ref. 0198
[Custom offer]
Please contact us at:
customresearch@cerep.com
RAW 264-7 cells
Stimulant
LPS (0.1 µg/mL) + IFN-γ (50 U/mL)
Substrate
endogenous arginine
Measured product
-
NO 2
Detection method photometry
Reference
1400W (IC 50 : 400 nM)
[Solvent] must be kept ≤ 0.3%
Estrada, C. et al. (1992) Biochem. Biophys. Res. Commun., 186: 475-482.
❚ Whole cell assay to test inhibitors of induction and activity of NOS
Source
Substrate
Measured product
Detection method
Reference
rat cerebellum
[ 3 H]arginine (28 nM) + arginine (400 nM)
[ 3 H]citrulline
scintillation counting
L-NMMA (IC 50 : 370 nM)
Bredt, D.S. and Snyder, S.H. (1990) Proc. Natl. Acad. Sci. USA, 87: 682-685.
enzyme activity (% of control)
100
50
0
-8 -7 -6 -5 -4 -3
log [drug] (M)
L-NMMA
L-NAME
L-arginine
aminoguanidine
Cerep
services
Receptors
Ion
channels
Transporters
constitutive NOS (endothelial)
Source
HUV-EC-C
Substrate
[ 3 H]arginine (28 nM) + arginine (50 nM)
Measured product [ 3 H]citrulline
Detection method scintillation counting
Ref. 0197
Reference
L-NMMA (IC 50 : 300 nM)
Q 3 weeks
Pollock, J.S. et al. (1991) Proc. Natl. Acad. Sci. USA, 88: 10480-10484.
enzyme activity (% of control)
100
-10 -9 -8 -7 -6 -5 -4
50
-11 -10 -9 -8 -7 -6
-12 -11 -10 -6
-9 -8 -7
L-NMMA
L-arginine
L-NAME
0
aminoguanidine
-8 -7 -6 -5 -4 -3
log [drug] (M)
Kinases
Epigenetic &
DNA-related
enzymes
-10 -9 -8 -7 -6 -5 -4
-10 -8 -7 -6
-11 -9
Other
enzymes
-12 -11 -10 -9 -8 -7 -6
❚ Arachidonic acid metabolism
Specialized
cellular
assays
5-lipoxygenase
❚ lipoxygenase
Ref. 0772
Q 3 weeks
Included in:
Non-kinase enzyme profile
Diversity profile
Source
human recombinant (Sf9 cells) (cytosol)
Substrate
arachidonic acid (25 µM)
Measured product rhodamine 123
Detection method fluorimetry
Reference
NDGA (IC 50 : 400 nM)
Pufahl, R.A. et al. (2007) Anal. biochem., 364: 204-212.
Standard
profiles
Testing
conditions
12-lipoxygenase
❚ lipoxygenase
Ref. 0883
Q 3 weeks
Included in:
Non-kinase enzyme profile
Source
human platelets
Substrate
arachidonic acid (6 µM)
Measured product ferric oxidation of xylenol orange
Detection method photometry
Reference
NDGA (IC 50 : 1.2 µM)
Waslidge, N.B. and Hayes, D.J. (1995) Anal. biochem., 231: 354-358.
enzyme activity (% of control)
100
50
0
NDGA
baicalein
-8 -7 -6 -5
-9
log [drug] (M)
Ordering
information
Assay list
& index

178 in vitro pharmacology 2011 catalog
❚ arachidonic acid metabolism
15-lipoxygenase
Source
soybean
Substrate
arachidonic acid (35 µM)
❚ lipoxygenase
Measured product ferric oxidation of xylenol orange
Ref. 0190
Detection method photometry
Q 3 weeks
Reference
NDGA (IC 50 : 1.1 µM)
Included in:
Organ safety profile
Waslidge, N.B. and Hayes, D.J. (1995) Anal. biochem., 231: 354-358.
enzyme activity (% of control)
100
50
0
-8 -7 -6 -5 -4
log [drug] (M)
NDGA
COX 1
❚ cyclooxigenase
Ref. 0726
Q 3 weeks
Included in:
Non-kinase enzyme profile
BioPrint ® profile
Source
Substrate
Measured product PGE 2
Detection method EIA
Reference
human recombinant (Sf9 cells)
arachidonic acid (4 µM)
diclofenac (IC 50 : 13 nM)
Glaser, K. et al. (1995) Eur. J. Pharmacol., 281: 107-111.
enzyme activity (% of control)
100
-10 -9 -8 -7 -6 -5 -4
50
-11 -10 -9 -8 -7 -6
-12 -11 -10 -7 -6
-9 -8
diclofenac
0
sulindac
indomethacine
-11 -10 -9 -8 -7 -6 -5
log [drug] (M)
COX 2
❚ cyclooxigenase
Ref. 0727
Q 3 weeks
Included in:
Non-kinase enzyme profile
BioPrint ® profile
Organ safety profile
Source
human recombinant (Sf9 cells)
Substrate
arachidonic acid (2 µM)
Measured product PGE 2
Detection method EIA
Reference
NS398 (IC 50 : 68 nM)
Glaser, K. et al. (1995) Eur. J. Pharmacol., 281: 107-111.
enzyme activity (% of control)
100
-10 -9 -8 -7 -6 -5 -4
50 -11 -10 -9 -8 -7 -6
-12 -11 -10 -6
-9 -8 -7
NS 398
diclofenac
rofecoxib
0
indomethacine
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
sPLA 2 (Type V)
❚ phospholipase
Ref. 3176
Q 3 weeks
Included in:
Non-kinase enzyme profile
Organ safety profile
Source
Substrate
Measured product
Detection method
human recombinant (E. coli)
diheptanoyl thio-PC (250 µM)
heptanoyl thio-PC
photometry
Reference
oleyloxyethyl phosphorylcholine
(IC 50 : 20 µM)
Tiege, U.J. et al. (2005) J. Lipid. Res., 46: 1604-1614.
sPLA 2 (bee venom type III)
❚ phospholipase
Ref. 2999
Q 3 weeks
Source
Substrate
Measured product
Detection method
Reference
bee venom
diheptanoyl thio-PC (250 µM)
heptanoyl thio-PC
photometry
oleyloxyethyl phosphorylcholine
(IC 50 : 5.7 µM)
Tiege, U.J. et al. (2005) J. Lipid. Res., 46: 1604-1614.
TXA 2 synthetase
❚ TXA 2 synthetase
Ref. 0564
Q 3 weeks
Source
human platelets
Substrate
PGH 2 (10 µM)
Measured product TXB 2
Detection method EIA
Reference
furegrelate (IC 50 : 6 nM)
Wade, M.L. and Fitzpatrick, F.A. (1997) Arch. Biochem. Biophys., 347: 174-180.
enzyme activity (% of control)
100
50
0
furegrelate
-9 -8 -7 -6 -5
-11 -10
log [drug] (M)

179
❚ Monoamine & neurotransmitter synthesis
& metabolism
Cerep
services
Receptors
acetylcholinesterase
Ref. 0363
Q 3 weeks
Included in:
Non-kinase enzyme profile
Diversity profile
BioPrint ® profile
Organ safety profile
Source
human recombinant (HEK-293 cells)
Substrate
AMTCh (50 µM)
Measured product thio-conjugate
Detection method photometry
Reference
neostigmine (IC 50 : 35 nM)
[Solvent] must be kept ≤ 0.1%
Ellman, G.L. et al. (1961) Biochem. Pharmacol., 7: 88-95.
enzyme activity (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
neostigmine
physostigmine
tacrine
darepezil
Ion
channels
Transporters
COMT (catechol-O-methyl transferase)
Ref. 0457
Q 3 weeks
Included in:
Diversity profile
BioPrint ® profile
Organ safety profile
Source
Substrate
Measured product
Detection method
Reference
porcine liver
esculetin (1 µM)
scopoletin
fluorimetry
Ro 41-0960 (IC 50 : 30 nM)
Muller-Enoch, D. et al. (1976) Z. Naturforsch., 31: 280-284.
-10 -9 -8 -7 -6 -5 -4
-11 -10 -9 -8 -7 -6
-12 -11 -10 -6
-9 -8 -7
Kinases
Epigenetic &
DNA-related
enzymes
GABA transaminase
Ref. 0461
Q 3 weeks
Included in:
Diversity profile
Organ safety profile
Source
rat brain
Substrate
GABA (9 mM) + α-ketoglutarate (9 mM)
Measured product succinic semialdehyde
Detection method fluorimetry
Reference
AoAA (IC 50 : 200 nM)
Lösher, W. (1981) J. Neurochem., 36: 1521-1527.
enzyme activity (% of control)
100
50
AoAA
γ-acetylenic
0
GABA
-9 -8 -7 -6 -5 -4 -3
log [drug] (M)
Other
enzymes
Specialized
cellular
assays
HNMT (histamine N-methyl transferase)
Source
rat kidney
Substrate
[ 14 C]S-adenosyl-L-methionin (4 µM)
+ histamine (300 µM)
Ref. 0463
Measured product [ 14 C]histamine
Q 6 weeks
Detection method scintillation counting
Included in:
Reference
SKF-91488 (IC 50 : 34 µM)
Organ safety profile
De Santi C. et al. (1998) Xenobiotica, 28: 571-577.
enzyme activity (% of control)
100
-10 -9 -8 -7 -6 -5 -4
50
-11 -10 -9 -8 -7 -6
-12 -11 -10 -6
-9 -8 -7
SKF-91488
0
-7 -6 -5 -4 -3
log [drug] (M)
Standard
profiles
Testing
conditions
MAO-A
Ref. 0191
Q 3 weeks
Included in:
Non-kinase enzyme profile
Diversity profile
Organ safety profile
Source
human placenta
Substrate
kynuramine (0.15 mM)
Measured product 4-OHquinoline
Detection method photometry
Reference
clorgyline (IC 50 : 37 nM)
Weyler, W. and Salach, J.I. (1985) J. Biol. Chem., 260: 13199-13207.
-10 -9 -8 -7 -6 -5 -4
-11 -10 -9 -8 -7 -6
-12 -11 -10 -6
-9 -8 -7
Ordering
information
Assay list
& index

180 in vitro pharmacology 2011 catalog
❚ monoamine & neurotransmitter synthesis & metabolism
MAO-A - antagonist radioligand
Source
rat cerebral cortex
Ligand
[ 3 H]Ro 41-1049 (10 nM)
binding
Kd
14 nM
Ref. 0443
Non specific clorgyline (1 µM)
Q 3 weeks
Reference
clorgyline (IC 50 : 1.1 nM)
Included in:
BioPrint ® profile
Cesura, A.M. et al. (1990) Mol. Pharmacol., 37: 358-366.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
clorgyline
Ro 41-1049
(R)-deprenyl
Ro 16-6491
MAO-B
Ref. 0621
Q 3 weeks
Included in:
Non-kinase enzyme profile
Diversity profile
Organ safety profile
Source
human platelets
Substrate
benzylamine (0.5 mM)
Measured product benzaldehyde
Detection method photometry
Reference
deprenyl (IC 50 : 33 nM)
Uebelhack, R. et al. (1998) Pharmacopsychiat., 31: 187-192.
enzyme activity (% of control)
100
-10 -9 -8 -7 -6 -5 -4
50
-11 -10 -9 -8 -7 -6
-12 -11 -10 -6
-9 -8 -7
deprenyl
0
Ro-166491
clorgyline
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
MAO-B - antagonist radioligand
Source
rat cerebral cortex
Ligand
[ 3 H]Ro 19-6327 (15 nM)
Kd
19 nM
Non specific (R)-deprenyl (10 µM)
binding
Reference
(R)-deprenyl (IC 50 : 19 nM)
Ref. 0444
Q 3 weeks
Cesura, A.M. et al. (1989) Eur. J. Pharmacol., 162: 457-465.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
(R)-deprenyl
clorgyline
Ro 41-1049
Ro 16-6491
PNMT (phenylethanolamine N-methyltransferase)
Ref. 0464
Q 6 weeks
Included in:
Diversity profile
Organ safety profile
Source
Substrate
Measured product
Detection method
Reference
bovine adrenal medulla
[ 14 C]SAM (4 µM) + normetanephrine (28 mM)
[ 14 C]metanephrine
scintillation counting
LY 78335 (IC 50 : 42 µM)
Betito, K. et al. (1993) Eur. J. Pharmacol., 238: 273-282.
enzyme activity (% of control)
100
50
-10 -9 -8 -7 -6 -5 -4
-11 -10 -9 -8 -7 -6
-12 -11 -10 -9 -8 -7 -6
0
-9 -8 -7 -6 -5 -4 -3
log [drug] (M)
LY 78335
SKF64139
tyrosine hydroxylase
Ref. 0214
Q 3 weeks
Included in:
Diversity profile
Organ safety profile
Source
rat striatum
Substrate
[ 3 H]tyrosine (10 µM)
Measured product [ 3 H]H 2 O
Detection method scintillation counting
Reference
3-iodo L-tyrosine (IC 50 : 740 nM)
Nagatsu, T. et al. (1964) Anal. Biochem., 9: 122-126.
enzyme activity (% of control)
100
-10 -9 -8 -7 -6 -5 -4
50
-11 -10 -9 -8 -7 -6
-12 -11 -10 -6
-9 -8 -7
3-iodo L-tyrosine
methyl L-tyrosine
0
fusaric acid
-9 -8 -7 -6 -5 -4 -3
log [drug] (M)
-10 -9 -8 -7 -6 -5 -4
-11 -10 -9 -8 -7 -6
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
-12 -11 -10 -9 -8 -7 -6
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Assay developed in 2010 New assay conditions Human Q Standard turnaround time

181
Cerep
services
❚ Transduction signal enzymes
adenylyl cyclase (activator effect)
❚ cyclase
cellul ar
Ref. 3002
Q 3 weeks
Included in:
Diversity profile
Source
Stimulant
Measured product
Detection method
Reference
adenylyl cyclase (inhibitor effect)
❚ cyclase
cellul ar
Ref. 3003
Q 3 weeks
CHO cells
none (100 µM forskolin for control)
cAMP
HTRF
forskolin (EC 50 :11000 nM)
Johnson, R.A et al.(1997) J. Biol. Chem., 272: 8962-8966.
❚ This model should be used to test adenylyl cyclase stimulating drugs
Source
Stimulant
Measured product
Detection method
Reference
guanylyl cyclase (activator effect)
❚ cyclase
Ref. 3004
Q 3 weeks
Included in:
Diversity profile
BioPrint ® profile
CHO cells
forskolin (20 µM)
cAMP
HTRF
2'5'-dd-3'-AMP-bis (t-Bu-SATE)
(IC 50 :320 nM)
Johnson, R.A et al.(1997) J. Biol. Chem., 272: 8962-8966.
❚ This model should be used to test adenylyl cyclase inhibitors
Source
Substrate
Stimulant
Measured product
Detection method
Reference
guanylyl cyclase (inhibitor effect)
❚ cyclase
Ref. 3005
Q 3 weeks
IP 3 - agonist radioligand
❚ inositol phosphate
binding
Ref. 0083
Q 3 weeks
human recombinant
GTP (10 µM)
none (100 µM SNP for control)
cGMP
HTRF
sodium nitroprusside (EC 50 : 8.5 µM)
Lee, Y.-C. et al. (2000) Proc. Natl. Acad. Sci. USA, 20: 10763-10768.
❚ This model should be used to test guanylyl cyclase stimulating drugs
Source
Substrate
Stimulant
Measured product
Detection method
Reference
human recombinant
GTP (10 µM)
SNP(20 µM)
cGMP
HTRF
NS-2028 (IC 50 : 88 nM)
Lee, Y.-C. et al. (2000) Proc. Natl. Acad. Sci. USA, 20: 10763-10768.
❚ This model should be used to test guanylyl cyclase inhibitors
Source
Ligand
Kd
Non specific
Reference
rat cerebellum
[ 3 H]D-(1,4,5)IP 3 (0.5 nM)
11 nM
D-(1,4,5)IP 3 (1 µM)
D-(1,4,5)IP 3 (IC 50 : 23 nM)
Worley, P.F. et al. (1987) J. Biol. Chem., 262: 12132-12136.
enzyme activity (% of control)
100
50
0
-7 -6 -5 -4
log [drug] (M)
-8 -7 -6 -5 -4 -3
sodium
nitroprusside
Receptors
Ion
channels
Transporters
Kinases
Epigenetic &
DNA-related
enzymes
Other
enzymes
Specialized
cellular
assays
Standard
profiles
Testing
conditions
Ordering
information
Assay list
& index

182 in vitro pharmacology 2011 catalog
❚ transduction signal enzymes
PLC
❚ phospholipase c
Source
Substrate
Measured product
Detection method
Bacillus cereus
glycero-phosphoethanolamine (GPE)
(100 nM)
diacylglycerol (DAG)
fluorimetry
Ref. 2837
Q 3 weeks
Reference
D609 (IC 50 : 5.2 µM)
Amtmann, E. (1996) Drugs Exp. Clin. Res., 22: 287-294.
❚ ATPases
ATPase (Na + /K + )
Ref. 2009
Q 3 weeks
Included in:
Diversity profile
BioPrint ® profile
Source
porcine cerebral cortex
Substrate
ATP (2 mM)
Measured product Pi
Detection method photometry
Reference
ouabain (IC 50 : 215 nM)
Fiske, C.M. and Subbarow, Y. (1925) J. Biol. Chem., 66: 375-400.
enzyme activity (% of control)
100
50
ouabain
melittin
0
buffalin
-9 -8 -7 -6 -5 -4
log [drug] (M)
ATPase (H + /K + )
Ref. 0445
Q 4 weeks
Source
rabbit stomach fundus
Substrate
pNPP (2 mM)
Measured product pNP
Detection method photometry
Reference
omeprazole (IC 50 : 2.4 µM)
Dantzig, H. et al. (1991) Biochem. Pharmacol., 42: 2019-2026.
-10 -9 -8 -7 -6 -5 -4
-11 -10 -9 -8 -7 -6
-12 -11 -10 -6
-9 -8 -7
❚ Miscellaneous enzymes
acetyl CoA synthetase
Source
yeast
Substrate
[ 14 C]acetate (50 µM)
Measured product [ 14 C]acetyl CoA
Detection method scintillation counting
Reference
p-HMB (IC 50 : 350 µM)
Ref. 0388
Q 4 weeks
Focke, M. et al. (1990) FEBS Lett., 261: 106-108.
enzyme activity (% of control)
100
50
0
-5 -3
-4
log [drug] (M)
p-HMB
arginase 1
Ref. 3117
Q 3 weeks
Source
human recombinant (E. coli)
Substrate
thioarginine (1 mM)
Measured product thiol group
Detection method photometry
Reference
BEC (IC 50 : 850 nM)
Han, S. and Viola, R.E. (2001) Anal. Biochem., 295: 117-119.
-10 -9 -8 -7 -6 -5 -4
-11 -10 -9 -8 -7 -6
-12 -11 -10 -6
-9 -8 -7

183
miscellaneous enzymes ❚
carbonic anhydrase II
Ref. 2572
Q 3 weeks
Source
human erythrocytes
Substrate
4-nitrophenyl acetate (450 µM)
Measured product 4-nitrophenol
Detection method photometry
Reference
acetazolamide (IC 50 : 29 nM)
Iyer, R. et al. (2006) J. Biomol. Screen., 11: 782-791.
Cerep
services
Receptors
FAAH (fatty acid amide hydrolase)
Source
human recombinant (Sf21 cells)
Substrate
AMC arachidonoyl amide (20 µM)
Measured product 7-amino-4-methyl coumarin
Detection method Fluorimetry
Ref. 2960
Reference
URB597 (IC 50 :90 nM)
Q 3 weeks
Vandevoorde, S. (2008) Curr. Top. Med. Chem., 8: 247-267.
Ion
channels
Transporters
HMG-CoA reductase
Ref. 0187
Q 6 weeks
Source
Syrian hamster recombinant (E. coli)
Substrate
Measured product
Detection method
Reference
HMG-CoA (130 µM)
mevalonate
photometry
mevastatin (IC 50 : 4.7 µM)
Omhumar, R.V. et al. (1994) J. Biol. Chem., 269: 6810-6814.
enzyme activity (% of control)
100
50
0
-7 -6 -5 -4
log [drug] (M)
mevastatin
Kinases
Epigenetic &
DNA-related
enzymes
myeloperoxidase
Ref. 0193
Q inquire
Source
human leukocytes
Substrate
guaiacol (80 mM)
Measured product tetraguaiacol
Detection method photometry
Reference
NDGA (IC 50 : 5.1 µM)
Desser, R.K. et al. (1972) Arch. Biochem. Biophys., 148: 452-465.
-10 -9 -8 -7 -6
-10 -9 -6 -8 -7 -5 -4
-11 -10 -9 -8 -7 -6
-12 -11 -10 -6
-9 -8 -7
100
0
Other
enzymes
Specialized
cellular
assays
tubulin
Ref. 3274
Q 3 weeks
Source
porcine brain
Substrate
GTP (1 mM)
Measured comp. microtubules polymerisation
Detection method fluorimetry
Reference
vinblastine (IC 50 :1200 nM)
Bonne, D et al.(1985) J. Biol. Chem., 260: 2819-2825.
Standard
profiles
Testing
conditions
xanthine oxidase/superoxide O 2
–
scavenging
Ref. 0276
Q 3 weeks
Included in:
BioPrint ® profile
Source
purified xanthine oxidase from bovine milk
Substrate
Measured product
Detection method
Reference
hypoxanthine (10 µM)
O 2
–
+ uric acid
photometry
allopurinol (IC 50 : 2.37 µM)
McCord, J.K. and Fridovich, I. (1969) J. Biol. Chem., 244: 6049-6055.
Ordering
information
Assay list
& index

184 in vitro pharmacology 2011 catalog
❚ notes
❚ see also ADME-Tox & PK 2011 catalog
ADME-Tox & PK
2011 CATALOG
IN VITRO ADME
Solution properties
Drug absorption/drug transport
Drug metabolism
Drug-drug interactions
IN VITRO TOXICITY
Cardiac toxicity
Cytotoxicity
Genetic toxicity
IN VIVO PK/BIOANALYTICAL
In vivo PK
Bioanalytical
ASSAY SELECTION GUIDE
STANDARD PROFILES
APPLICATION NOTES

185
Specialized
cellular assays
The specialized cellular assays listed in this section are displayed as part of our custom offer.
Cerep offers a more flexible approach around these targets to better fit the client's needs in terms of choice of technology, assay customization,
workplan and turnaround time.
❚ For further information, please contact us at customresearch@cerep.com.
Cerep
services
Receptors
Ion
channels
❚ Monomamine & neurotransmitter release
Transporters
dopamine release (activator effect)
cellul ar
Ref. 0450
[CUSTOM OFFER]
Source
Tracer
Control
Measured product
Detection method
rat striatum synaptosomes
[ 3 H]DA
amphetamine (1 mM)
[ 3 H]DA release from synaptosomes
scintillation counting
Reference
amphetamine (EC 50 : 1 µM)
Bondiolotti, G.P. et al. (1995) Biochem. Pharmacol., 50: 97-102.
DA release (% of control)
100
50
0
-9 -8 -7 -6 -5 -4 -3
log [drug] (M)
amphetamine
Kinases
Epigenetic &
DNA-related
enzymes
norepinephrine release (activator effect)
cellul ar
Ref. 0460
[CUSTOM OFFER]
Source
Tracer
Control
Measured product
Detection method
Reference
rat hypothalamus synaptosomes
[ 3 H]NE
amitriptyline (1 mM)
[ 3 H]NE release from synaptosomes
scintillation counting
amitriptyline (EC 50 : 59 µM)
Yamagushi, T. et al. (1998) Neuropharmacol., 37: 1169-1176.
Other
enzymes
Specialized
cellular
assays
histamine release (activator effect)
Source
human blood
Control
compound A23187 (20 µM)
Measured product histamine
Detection method EIA
cellul ar
Reference
A23187 (EC 50 : 2.5 µM)
Ref. 0404
Q 4 weeks
[Solvent] must be kept ≤ 0.3%
Nolte, H. and Stahlskov, P. (1988) Agents Actions , 23: 173-176.
Standard
profiles
Testing
conditions
histamine release (inhibitor effect)
cellul ar
Source
Stimulant
Measured product
Detection method
Reference
human blood
A23187 (10 µM)
histamine
EIA
cyclosporin A (IC 50 : 280 nM)
Ordering
information
Ref. 0409
[CUSTOM OFFER]
[Solvent] must be kept ≤ 0.3%
Nolte, H. and Stahlskov, P. (1988) Agents Actions , 23: 173-176.
Assay list
& index

186 in vitro pharmacology 2011 catalog
❚ monoamine & neurotransmitter release
5-HT release (activator effect)
cellul ar
Ref. 0459
[CUSTOM OFFER]
Source
Tracer
Control
Measured product
Detection method
Reference
rat brain synaptosomes
[ 3 H]5-HT
fenfluramine (0.1 mM)
[ 3 H]5-HT release from synaptosomes
scintillation counting
fenfluramine (EC 50 : 470 nM)
Bonanno, G. et al. (1994) J. Neurochem., 63: 1163-1166.
5-HT release (inhibitor effect)
100
cellul ar
Ref. 0286
[CUSTOM OFFER]
Source
rat mast cells
Tracer
[ 3 H]5-HT (0.2 µCi)
Stimulant
compound 48/80 (0.1 µg/mL)
Measured product 5-HT (endogenous)
Detection method scintillation counting
Reference
SCG (IC 50 : 4 µM)
[Solvent] must be kept ≤ 0.1%
Theoharides, T.C. et al. (1985) Biochem. Pharmacol., 34: 1389-1398.
5-HT release (% of control)
50
0
-7 -6 -5 -4 -3
log [drug] (M)
SGC
❚ Ion transport systems
Ca 2+ - ATPase pump
cellul ar
Ref. 0216
[CUSTOM OFFER]
Source
rat liver membrane vesicles
Substrate
ATP (1 mM)
Tracer
45 Ca (0.1 µCi)
Measured product
45 Ca uptake
Detection method scintillation counting
Reference
thapsigargin (IC 50 : 400 nM)
Jean, T. and Klee, C.B. (1986) J. Biol. Chem., 261: 16414-16420.
45 Ca uptake (% of control)
100
50
0
-8 -7 -6 -5
log [drug] (M)
thapsigargin
Na + /K + - ATPase pump
100
cellul ar
Ref. 0221
[CUSTOM OFFER]
Source
A7r5 cells
Substrate
endogenous ATP
Tracer
86 Rb (0.1 µCi)
Measured product
86 Rb uptake
Detection method scintillation counting
Reference
ouabain (IC 50 : 200 µM)
[Solvent] must be kept ≤ 0.3%
Chassande, O. et al. (1988) Eur. J. Biochem., 171: 425-433.
86 Rb uptake (% of control)
50
0
-6 -5 -4 -3
log [drug] (M)
ouabain
Na + /Ca 2+ antiport
cellul ar
Ref. 0222
[CUSTOM OFFER]
Source
bovine heart membrane vesicles
Tracer
45 Ca (0.5 µCi)
Measured product
45 Ca uptake
Detection method scintillation counting
Reference
2’,4’ dichlorobenzamil (IC 50 : 20 µM)
Slaughter, R.S. et al. (1988) Biochemistry, 27: 2403-2409.

187
ion transport systems ❚
Na + /H + antiport
cellul ar
Ref. 0223
[CUSTOM OFFER]
Source
A7r5 cells
Tracer
22 Na (0.4 µCi)
Measured product
22 Na uptake
Detection method scintillation counting
Reference
EIPA (IC 50 : 50 nM)
Jean, T. et al. (1986) Eur. J. Biochem., 160: 211-219.
Cerep
services
Receptors
Na + /K + /Cl – cotransport
100
cellul ar
Ref. 0224
[CUSTOM OFFER]
Source
Tracer
Measured product
Detection method
Reference
A7r5 cells
86 Rb (0.2 µCi)
86 Rb uptake
scintillation counting
bumetanide (IC 50 : 1 µM)
Chassande, O. et al. (1988) Eur. J. Biochem., 171: 425-433.
86 Rb uptake (% of control)
50
0
-8 -7 -6 -5 -4
log [drug] (M)
bumetanide
furosemide
Ion
channels
Transporters
❚ Arachidonic acid metabolite secretion
Kinases
LTB 4 secretion (inhibitor effect)
cellul ar
Ref. 0243
[CUSTOM OFFER]
Source
differentiated HL-60 cells
Stimulant
A23187 (5 µM)
Measured product LTB 4
Detection method EIA
Reference
[Solvent] must be kept ≤ 0.3%
NDGA (IC 50 : 470 nM)
Bennett, C.F. et al. (1993) Biochem. J., 289: 33-39.
LTB 4 secretion (% of control)
100
50
0
-8 -7 -6 -5 -4
log [drug] (M)
NDGA
zileuton
phenidone
ETYA
Epigenetic &
DNA-related
enzymes
Other
enzymes
LTC 4 secretion (inhibitor effect)
cellul ar
Ref. 0395
[CUSTOM OFFER]
Source
differentiated HL-60 cells
Stimulant
A23187 (5 µM)
Measured product LTC 4
Detection method
Reference
EIA
PMA (IC 50 : 5 nM)
Bennett, C.F. et al. (1993) Biochem. J., 289: 33-39.
LTC 4 secretion (% of control)
100
50
0
PMA
NDGA
-10 -9 -8 -7 -6 -5
log [drug] (M)
Specialized
cellular
assays
Standard
profiles
PGE 2 secretion (inhibitor effect)
cellul ar
Ref. 0238
[CUSTOM OFFER]
Source
differentiated HL-60 cells
Stimulant
A23187 (5 µM)
Measured product PGE 2
Detection method EIA
Reference
indomethacin (IC 50 : 4 nM)
[Solvent] must be kept ≤ 0.3%
Honda, A. et al. (1990) Biochem. J., 272: 259-262.
PGE2 secretion (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5 -4 -3
log [drug] (M)
indomethacin
diclofenac
ibuprofen
acetylsalicylic
acid
Testing
conditions
Ordering
information
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Human Q Standard turnaround time [CUSTOM OFFER] Please contact us at: customresearch@cerep.com
Assay list
& index

188 in vitro pharmacology 2011 catalog
❚ arachidonic acid metabolite secretion
PGI 2 secretion
cellul ar
Ref. 0240 Activator effect
Ref. 0241 Inhibitor effect
[CUSTOM OFFER]
Source
TXB 2 secretion (inhibitor effect)
cellul ar
Ref. 2006
[CUSTOM OFFER]
HUV-EC-C
Measured product 6ketoPGF 1α
Detection method EIA
Activator effect Control thrombin (0.3 U/mL)
Reference thrombin (EC 50 : 0.04 U/mL)
Inhibitor effect Stimulant human thrombin (0.3 U/mL)
Reference indomethacin (IC 50 : 8.6 nM)
Zavoico, G.B. et al. (1989) J. Immunol., 142: 3993-3999.
❚ This model should be used to test pro-inflammatory drugs.
Source
differentiated HL-60
Stimulant
A23187 (5 µM)
Measured product TXB 2
Detection method EIA
Reference
indomethacin (IC 50 : 4.7 nM)
[Solvent] must be kept ≤ 0.1%
Zaitsu, M. et al. (2002) Prost. Leuk. Essent. Fatty Acids, 67: 405-410.
[Solvent] must be kept 0.1%
❚ Chemokine secretion
IL-8 secretion (inhibitor effect)
cellul ar
Ref. 0272
[CUSTOM OFFER]
Source
PBMC
Stimulant
LPS (1 µg/mL)
Measured product IL-8
Detection method EIA
Reference
dexamethasone (IC 50 : 8.4 nM)
[Solvent] must be kept ≤ 0.1%
Schindler, R. et al. (1990) Blood, 75: 40-47.
❚ Cytokine secretion
IFN-g secretion (inhibitor effect)
cellul ar
Ref. 0368
[CUSTOM OFFER]
Source
Stimulant
Measured product
PBMC
PHA (2 µg/mL)
IFN-γ
Detection method EIA
Reference
dexamethasone (IC 50 : 3.5 nM)
[Solvent] must be kept ≤ 0.1%
Andre, F. et al. (1996) Allergy, 51: 350-355.
IFN-γ secretion (% of control)
100
50
0
-10 -9 -8 -7 -6 -5
log [drug] (M)
dexamethasone
IL-1β secretion (inhibitor effect)
cellul ar
Ref. 0262
[CUSTOM OFFER]
Source
Stimulant
Measured product
PBMC
LPS (1 µg/mL)
IL-1β
Detection method EIA
Reference
cycloheximide (IC 50 : 230 nM)
[Solvent] must be kept ≤ 0.1%
Schindler, R. et al. (1990) Blood, 75: 40-47.
IL-1β secretion (% of control)
100
50
0
-9 -8 -7 -6 -5
log [drug] (M)
cycloheximide

189
cytokine secretion ❚
IL-2 secretion (inhibitor effect)
cellul ar
Ref. 0263
[CUSTOM OFFER]
Source
Stimulant
Measured product
PBMC
PHA (20 µg/mL)
IL-2
Detection method EIA
Reference
dexamethasone (IC 50 : 9 nM)
[Solvent] must be kept ≤ 0.1%
Konno, S. et al. (1994) Eur. J. Pharmacol., 264: 265-268.
IL-2 secretion (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5
log [drug] (M)
dexamethasone
Cerep
services
Receptors
IL-4 secretion (inhibitor effect)
cellul ar
Ref. 0264
[CUSTOM OFFER]
Source
PBMC
Stimulant
ConA (20 µg/mL)
Measured product IL-4
Detection method EIA
Reference
dexamethasone (IC 50 : 4.8 nM)
[Solvent] must be kept ≤ 0.1%
Endo, H. et al. (1993) Int. Arch. Allergy Immunol., 101: 425-430.
IL-4 secretion (% of control)
100
50
0
-10 -9 -8 -7 -6
log [drug] (M)
dexamethasone
Ion
channels
Transporters
IL-5 secretion (inhibitor effect)
cellul ar
Ref. 0265
[CUSTOM OFFER]
Source
PBMC
Stimulant
ConA (20 µg/mL)
Measured product IL-5
Detection method EIA
Reference
dexamethasone (IC 50 : 2.4 nM)
[Solvent] must be kept ≤ 0.1%
Endo, H. et al. (1993) Int. Arch. Allergy Immunol., 101: 425-430.
IL-5 secretion (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5
log [drug] (M)
dexamethasone
Kinases
Epigenetic &
DNA-related
enzymes
IL-6 secretion (inhibitor effect)
cellul ar
Ref. 0269
[CUSTOM OFFER]
Source
PBMC
Stimulant
LPS (1 µg/mL)
Measured product IL-6
Detection method EIA
Reference
dexamethasone (IC 50 : 5 nM)
[Solvent] must be kept ≤ 0.1%
Schingler, R. et al. (1990) Blood, 75: 40-47.
IL-6 secretion (% of control)
100
50
0
-10 -9 -8 -7 -6
log [drug] (M)
dexamethasone
Other
enzymes
Specialized
cellular
assays
IL-10 secretion (inhibitor effect)
cellul ar
Ref. 0273
[CUSTOM OFFER]
Source
PBMC
Stimulant
PHA (3 µg/mL)
Measured product IL-10
Detection method EIA
Reference
dexamethasone (IC 50 : 15 nM)
[Solvent] must be kept ≤ 0.1%
Rigano, R. et al. (1995) Clin. Exp. Immunol., 99: 433-439.
IL-10 secretion (% of control)
100
50
0
-10 -9 -8 -7 -6
log [drug] (M)
dexamethasone
Standard
profiles
Testing
conditions
TNF-α secretion (inhibitor effect)
cellul ar
Ref. 0259
[CUSTOM OFFER]
Source
Stimulant
Measured product
PBMC
LPS (1 µg/mL)
TNF-α
Detection method EIA
Reference
dexamethasone (IC 50 : 6 nM)
[Solvent] must be kept ≤ 0.1%
Schindler, R. et al. (1990) Blood, 75: 40-47.
TNFα secretion (% of control)
100
50
0
-10 -9 -8 -7 -6
log [drug] (M)
dexamethasone
Ordering
information
Assay list
& index

190 in vitro pharmacology 2011 catalog
❚ Free radical secretion
superoxide O 2
–
secretion
cellul ar
Source
Substrate
Stimulant
Measured product
Detection method
differentiated HL-60 cells
cytochrome C (19 µM)
PMA (30 nM)
-
O 2 (cytochrome C reduction)
photometry
Ref. 0275
[CUSTOM OFFER]
Reference
diphenyleneiodonium (IC 50 : 380 nM)
Lorico, A. et al. (1986) Biochem. Pharmacol., 35: 2443-2445.
H 2 O 2 secretion
cellul ar
Ref. 0277
[CUSTOM OFFER]
Source
differentiated HL-60 cells
Substrate
scopoletin (4 µM)
Stimulant
PMA (19 nM)
Measured product H 2 O 2 (scopoletin oxidation)
Detection method fluorimetry
Reference
catalase (IC 50 : 220 U/mL)
Root, R.K. et al. (1975) J. Clin. Invest., 55: 945-955.
H 2O2 secretion (% of control)
100
50
0
1 10 100 1000 10000
log [drug] (U/mL)
catalase
H 2 O 2 scavenging
cellul ar
Ref. 0278
[CUSTOM OFFER]
Source
cell free system
Substrate
scopoletin (4 µM)
Stimulant
H 2 O 2 (2 µM)
Measured product scopoletin oxidation
Detection method fluorimetry
Reference
catalase (IC 50 : 27 U/mL)
Root, R.K. et al. (1975) J. Clin. Invest., 55: 945-955.
H 2 O 2 scavenging (% of control)
100
50
0
0 1 10 100 1000
log [drug] (U/mL)
catalase
lipid peroxidation
cellul ar
Ref. 0279
[CUSTOM OFFER]
Source
rat liver microsomes
Substrate
ascorbic acid (0.1 mM)
Measured product malonaldehyde
Detection method photometry
Reference
N-propyl gallate (IC 50 : 2.4 µM)
Aruoma, O.I. et al. (1990) Free Rad. Res. Commun., 10: 143-157.
malonaldehyde production (% of control)
100
50
0
-7 -6 -5 -4
log [drug] (M)
N-propyl gallate
ebselen
trolox
❚ Cell adhesion
expression of endothelial adhesion proteins (ICAM1/VCAM-1)
cellul ar
Ref. 0244
[CUSTOM OFFER]
Source
resting U-937 cells to stimulated HUVEC
Stimulant
LPS (1 µg/mL)
Measured product ICAM1/VCAM-1 mediated adhesion
Detection method fluorimetry
Reference
NDGA (IC 50 : 10 µM)
[Solvent] must be kept ≤ 0.3%
Staunton, D.E. et al. (1989) Nature, 339: 61-64.

191
expression of endothelial adhesion proteins (ELAM-1)
cellul ar
Ref. 0245
[CUSTOM OFFER]
Source
Stimulant
Measured product
Detection method
Reference
[Solvent] must be kept ≤ 0.1%
resting HL-60 cells to stimulated HUVEC
TNF-α (3 ng/mL)
ELAM-1 mediated adhesion
fluorimetry
NDGA (IC 50 : 18 µM)
Vaporciyan, A.A. et al. (1993) J. Immunol. Met., 159: 93-100.
expression of endothelial adhesion proteins (VCAM-1)
cellul ar
Ref. 0246
[CUSTOM OFFER]
Source
resting Ramos cells to stimulated HUVEC
Stimulant
TNF-α (1 ng/mL) + IL-4 (500 U/mL)
Measured product VCAM-1 mediated adhesion
Detection method fluorimetry
Reference
cycloheximide (IC 50 : 2 µM)
[Solvent] must be kept ≤ 0.1%
Kapiotis, S. et al. (1994) Circulatory Shock, 43: 18-25.
activation of monocyte adhesion proteins (U-937/HUVEC)
cellul ar
Ref. 0247
[CUSTOM OFFER]
Source
stimulated U-937 cells to resting HUVEC
Stimulant
PMA (100 nM)
Measured product activation of U-937 adhesion molecules
Detection method fluorimetry
Reference
staurosporine (IC 50 : 230 nM)
[Solvent] must be kept ≤ 0.1%
Cavender, D.E. et al. (1991) J. Leuk. Biol., 49: 566-578.
adhesion (% of control)
adhesion (% of control)
cell adhesion ❚
100
50
cycloheximide
0
-7 -6 -5
log [drug] (M)
100
50
0
staurosporine
-8 -7 -6
log [drug] (M)
Cerep
services
Receptors
Ion
channels
Transporters
Kinases
Epigenetic &
DNA-related
enzymes
activation of monocyte adhesion proteins (matrix proteins)
cellul ar
Ref. 0249
[CUSTOM OFFER]
Source
stimulated U-937 cells to extracellular
matrix proteins (collagen + fibronectin)
Stimulant
PMA (100 nM)
Measured product activation of U-937 adhesion molecules
Detection method fluorimetry
Reference staurosporine (IC 50 : 160 nM)
[Solvent] must be kept ≤ 0.1%
Cavender, D.E. et al. (1991) J. Leuk. Biol., 49: 566-578.
adhesion (% of control)
100
50
0
-8 -7 -6 -5
log [drug] (M)
staurosporine
Other
enzymes
Specialized
cellular
assays
activation of granulocyte adhesion proteins (HL-60/HUVEC)
cellul ar
Ref. 0248
[CUSTOM OFFER]
Source
stimulated HL-60 cells to resting HUVEC
Stimulant
PMA (100 nM)
Measured product activation of HL-60 adhesion molecules
Detection method fluorimetry
Reference
staurosporine (IC 50 : 540 nM)
[Solvent] must be kept ≤ 0.1%
Cavender, D.E. et al. (1991) J. Leuk. Biol., 49: 566-578.
adhesion (% of control)
100
50
0
-8 -7 -6
log [drug] (M)
staurosporine
Standard
profiles
Testing
conditions
Ordering
information
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Human Q Standard turnaround time [CUSTOM OFFER] Please contact us at: customresearch@cerep.com
Assay list
& index

192 in vitro pharmacology 2011 catalog
❚ Cell migration
PDGF-stimulated A7r5 migration
1. 5
cellul ar
Ref. 0250
[CUSTOM OFFER]
Source
A7r5 cells
Stimulant
PDGF-BB (100 ng/mL)
Measured product cells stained with crystal violet
Detection method photometry
Reference
tyrphostin 9 (5 µM)
Koyama, N. et al. (1994) Circ. Res., 75: 682-691.
absorbance at 550 nm
1. 0
0. 5
0. 0
- + + + + PDGF 100 ng/mL
- - 2x10 -7 2x10 -6 5x10 -6 Tyrphostin 9 (M)
PDGF-stimulated AoSMC migration
2. 0
cellul ar
Ref. 0344
[CUSTOM OFFER]
Source
AoSMC
Stimulant
PDGF-BB (100 ng/mL)
Measured product cells stained with crystal violet
Detection method photometry
Reference
tyrphostin 9 (5 µM)
Koyama, N. et al. (1994) Circ. Res., 75: 682-691
absorbance at 550 nm
1. 5
1. 0
0. 5
0. 0
- + + + + + PDGF 100 ng/mL
- -
2x10 -7
2x10 -6
5x10 -6
10 -5
Tyrphostin 9 (M)
❚ Cell proliferation
serum-stimulated A7r5 proliferation
cellul ar
Ref. 0251
[CUSTOM OFFER]
Source
A7r5 cells
Stimulant FCS (10 %)
Measured product BrdU incorporation
Detection method
Reference
EIA
nitrendipine (IC 50 : 52 µM)
Handler, J.A. et al. (1990) J. Biol. Chem., 265: 3669-3673.
[ 3 H]BrdU incorporation (% of control)
100
50
0
-7 -6 -5 -4
log [drug] (M)
nitrendipine
PDGF-stimulated A7r5 proliferation
cellul ar
Ref. 0352
[CUSTOM OFFER]
Source
Stimulant
Tracer
Measured product
A7r5 cells
PDGF-BB (50 ng/mL)
[ 3 H]TMD (0.25 µCi)
[ 3 H]TMD incorporation
Detection method scintillation counting
Reference tyrphostin 9
Koyama, N. et al. (1994) Circ. Res., 75: 682-691.
[ 3 H]TMD incorporation (dpm)
15000
10000
5000
0
- +
tyrphostin
3x10 -7
nitrendipine
10 -5
verapamil
3x10 -5
EGF-stimulated A-431 proliferation
cellul ar
Ref. 0252
[CUSTOM OFFER]
Source
A-431 cells
Stimulant
EGF (1 ng/mL)
Tracer
[ 3 H]TMD (0.05 µCi)
Measured product [ 3 H]TMD incorporation
Detection method scintillation counting
Reference
staurosporine (IC 50 : 3 nM)
[Solvent] must be kept ≤ 0.1%
Handler, J.A. et al. (1990) J. Biol. Chem., 265: 3669-3673.
[ 3 H]TMD incorporation (dpm)
100
50
0
-10
-9 -8
log [drug] (M)
staurosporine

193
PDGF-stimulated Balb/c 3T3 proliferation
cellul ar
Ref. 0253
[CUSTOM OFFER]
Source
Stimulant
Tracer
Measured product
Detection method
Balb/c 3T3 cells
PDGF-BB (3 ng/mL)
[ 3 H]TMD (1 µCi)
[ 3 H]TMD incorporation
scintillation counting
Reference
cycloheximide (IC 50 : 100 nM)
Handler, J.A. et al. (1990) J. Biol. Chem., 265: 3669-3673.
[ 3 H]TMD incorporation (dpm)
cell proliferation ❚
100
50
0
cycloheximide
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
Cerep
services
Receptors
VEGF-stimulated HUV-EC-C proliferation
cellul ar
Ref. 0937
[CUSTOM OFFER]
Source
HUV-EC-C cells
Stimulant
VEGF (10 nM)
Tracer
[ 3 H]TMD (0.2 µCi)
Measured product [ 3 H]TMD incorporation
Detection method scintillation counting
Reference
TNFα (IC 50 : 4.4 pM)
[Solvent] must be kept ≤ 0.1%
Mauerhoff, T. et al. (1994) Tumori, 80: 301-305.
[ 3 H]TMD incorporation (dpm)
100
50
0
-50
-14 -13 -12 -11 -10 -9 -8 -7 -6 -5 -4
log [drug] (M)
TNFα
staurosporine
Ion
channels
Transporters
PHA-stimulated PBMC proliferation
cellul ar
Ref. 0254
[CUSTOM OFFER]
Source
PBMC
Stimulant PHA (2 µg/mL)
Tracer
[ 3 H]TMD (1 µCi)
Measured product [ 3 H]TMD incorporation
Detection method scintillation counting
Reference
staurosporine (IC 50 : 19 nM)
[Solvent] must be kept ≤ 0.1%
Gougerot-Pocidalo, M.A. et al. (1988) Immunology, 64: 281-288.
[ 3 H]TMD incorporation (% of control)
100
50
0
staurosporine
-10 -9 -8 -7 -6
log [drug] (M)
Kinases
Epigenetic &
DNA-related
enzymes
❚ Cell viability
Other
enzymes
cell viability
Source
U-937, HUVEC, PBMC, THP-1, A7r5,
HL-60 or SK-N-SH cells
Substrate
MTT (0.5 mg/mL)
Measured product formazan
Detection method photometry
cellul ar
0
Reference
erythromycin or PMA
erythromycin
0.1 0.3 1.0
Ref. 0274
n To be combined with secretion assays
[erythromycin] (mg/mL)-24h incubation
[CUSTOM OFFER]
Mosmann, T. (1983) J. Immunol. Met., 65: 55-63.
❚ Cellular models such as human primary hepatocytes, and other technology such alamarBlue are available: see ADME-Tox & PK 2011 catalog
PBMC viability (% of viable cells)
100
50
Specialized
cellular
assays
Standard
profiles
Testing
conditions
Ordering
information
For further details and updated information on assays:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
Human Q Standard turnaround time [CUSTOM OFFER] Please contact us at: customresearch@cerep.com
Assay list
& index

194 in vitro pharmacology 2011 catalog

195
cerep
Standard
profiles
ExpresS profile
High-Throughput profile
ExpresS Diversity Kinase profile
Cellular functional profile
PDE high-throughput profile
Non-kinase enzyme profile
Diversity profile
BioPrint ® profile
Organ safety profile
Comprehensive kinase profile
ADME-Tox Option I [Bioavailability]
ADME-Tox Option II [Lead selection/prioritization]
Genotoxicity profile
CYP drug-drug interaction profile
P-gp mediated drug-drug interaction profile
p. 196
p. 196
p. 196
p. 197
p. 197
p. 197
p. 197
p. 197
p. 198
p. 198
p. 199
p. 199
p. 199
p. 199
p. 200
Sample size p. 201

196 in vitro pharmacology 2011 catalog
CEREP
standard profiles
At January 1, 2011, Cerep offers 15 standard profiles. While some, extensively used by many of our customers, remain the
same as in 2010, others have evolved to include widely requested assays.
Compared to 2010:
Two new profiles have been created, the Cellular functional GPCR profile, designed to identify potential off-target activities
early in the drug discovery process, and the PDE High-throughput profile, designed to determine the inhibitory activity and
selectivity of compounds on the PDE superfamily.
The ADME-Tox Option II [Lead Selection/Prioritization] profile, has been expanded to incorporate a complete panel of
CYP isozymes for evaluation of a compound’s CYP inhibition potential.
❚ ExpresS profile [55 binding assays]
Ref. P1
Suggested testing: 10 µM (n=2)
Q 5 business days
The ExpresS Profile is a fast turnaround selectivity/specificity profile drawn from the Highthroughput
profile (see below). The majority of the 55 binding assays in the ExpresSProfile panel
are human recombinant receptors.
With a one week turnaround time, the ExpresS Profile greatly accelerates the "risk assessment"
of lead compounds.
❚ High-throughput profile [80 binding assays]
Ref. P3
Suggested testing: 10 µM (n=2)
Q 2 weeks
The High-throughput profile consists of a broad collection of 80 transmembrane and soluble
receptors, ion channels and monoamine transporters. It has been specifically designed to
provide information not only on potential limitations or liabilities of drug candidates, but also
for off-target activity identification.
Used either for risk assessment, selectivity/specificity, or for identification of new activities,
the high-throughput profile is a rapid and cost effective way of prioritizing the most promising
compounds in hit-to-lead selection process.
Cellular functional GPCR assays are available on 66 % of the assays in this profile.
❚ ExpresS DIVERSITY KINASE profile [48 enzyme assays]
Ref. P10
Suggested testing: 10 µM (n=2)
Q 5 business days
(Starting on Monday: Compounds
must be received at Cerep France
site on Friday before noon.)
The ExpresS Diversity kinase profile is a fast turnaround profile containing 48 biochemical kinase
assays. The assays were selected taking into consideration the diversity of assay families and the
automation level of each assay to maintain the one week turnaround time. As Kinase-inhibitory
compounds often interact with a spectrum of kinases, identification of those with improved selectivity
is essential. This need can be supported by rapid profiling of your libraries on ExpresS Diversity
kinase profile.
All assays are part of the Comprehensive kinase profile (See page 198).
For list of assays included in standard profiles and updated information:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
New profile Profile/module changed as compared to 2010: please go to www.cerep.com Q Standard turnaround time

197
❚ Cellular functional GPCR profile [30 targets]
Ref. P27
Suggested testing: 10 µM (n=2)
Q 10 business days
(Starting on Monday: Compounds
must be received at Cerep France
site on Friday before noon.)
The Cellular Functional GPCR profile – 30 targets – is a fast turnaround time panel covering
a selection of diverse and information rich GPCR targets. This profile is designed to identify
potential off-target activities early in the drug discovery process. Targets were selected taking
into account market demand, and according to statistical correlations between compound pharmacological
profiles and Adverse Drug Reactions (ADRs), identified within Cerep’s proprietary
BioPrint ® database.
The assay protocols are designed to detect agonist, and antagonist activities of compounds.
For those who would like to evaluate earlier in the drug discovery process both affinity and
functional activity of compounds, all corresponding binding assays of the targets in this
profile are available at Cerep. Clients may request Cerep’s advice on when to use binding,
functional, or both approaches according to target(s) of interest.
The assays for each target can be customized to identify inverse agonists or allosteric
modulators (not included in this profile): please contact us at sales@cerep.com.
Cerep
services
Receptors
Ion
channels
❚ PDE High-throughput profile [13 assays]
Ref. P23
Suggested testing: 10 µM (n=2)
Q 3 weeks
The PDE High-throughput profile is designed to determine the inhibitory activity and selectivity
of compounds on the PDE superfamily. The robustness, reproducibility and relevance of
this 13 enzyme assay profile were validated by determining the potency and selectivity of a
broad panel of commercially available reference inhibitors and known clinical drugs in three
independent experiments (poster available on the website).
For Cellular phosphodiesterase assays, please contact us at customresarch@cerep.com
Transporters
Kinases
❚ Non-KINASE enzyme profile [40 assays]
Ref. P7
Suggested testing: 10 µM (n=2)
Q 3 weeks
The Non-kinase enzyme profile includes 40 robust and diverse enzymes broadly chosen
among various enzyme families with a particular focus on specific enzymes involved in cell
cycle regulation. Due to its diversity, this profile allows an optimal assessment of enzymatic
specificity of drug candidates.
Epigenetic &
DNA-related
enzymes
Other
enzymes
❚ Diversity profile [72 binding & 27 enzyme assays]
Ref. P9
Suggested testing: 10 µM (n=2)
Q 3 weeks
The Diversity profile is composed of 72 binding and 27 enzyme assays. The binding assay
panel is broadly defined with roughly an equal number of selective, central and peripheral
therapeutically relevant targets. The enzyme assay panel includes the most representative targets
from diverse enzyme families with a particular focus on phosphatases and specific enzymes
involved in cell cycle regulation.
This profile is designed for the optimal assessment of the “biological diversity” or early discovery
compounds.
Specialized
cellular
assays
Standard
profiles
❚ BioPrint ® profile [159 assays]
Full profile (159 assays)
Ref. P22
BioPrint ® in vitro
pharmacology profile
(139 assays)
Suggested testing: 10 µM (n=2)
Ref. P22-p
The BioPrint ® profile includes the assays used to explore the properties of about 2,450 BioPrint ®
compounds, establishing individual Pharma-ADME fingerprints for each compound.
The BioPrint ® profile is mainly based on target diversity and includes today 105 binding assays
(GPCRs, nuclear and other receptors, ion channels and transporters), 34 enzyme assays
(including 10 kinases, 10 proteases and 5 PDEs), as well as 20 ADME-Tox assays (Solubility,
Absorption, Metabolism and CYP-mediated drug-drug interaction). More than 70% are human
targets.
The 159 assays of this profile represent a rationalized panel from a larger assay collection in
the database, selected for highest information content.
Testing
conditions
Ordering
information
Q 3 weeks
BioPrint ® services – Drug profile interpretation & Target profile design – are now part of
our custom offer. For further information, please contact us at customresearch@cerep.com.
Assay list
& index

198 in vitro pharmacology 2011 catalog
❚ Cerep standard profiles
❚ Organ safety profile [270 assays]
full panel (271 assays)
Ref. P26
Suggested testing: 10 µM (n=2)
Q 4 weeks
(Starting on Monday: Compounds
must be received at Cerep France
site on Friday before noon.)
MODULES
Module 1 Ref. P26-m1
Module 2 Ref. P26-m2
Module 3
Module 4
Module 5
Q inquire
Ref. P26-m3
Ref. P26-m4
Ref. P26-m5
This Organ safety profile is inspired from the ICH guidelines S7A: Safety pharmacology studies
for human pharmaceuticals. The ICH S7A is into effect from June 2001 and is applied to new
chemical and biological entities, including biotechnology driven products and may be applied
to marketed pharmaceuticals when appropriate.
Safety pharmacology studies investigate the potential undesirable pharmacodynamic effects
of chemicals or pharmaceutical compounds on vital organs or systems which are essential for
sustaining life. The ICH Safety Expert Working Group has developed a hierarchy of organ
systems with respect to their life supporting functions. The most important functions are those
of the cardiovascular, respiratory or central nervous systems. Drug induced effects on these
systems should be investigated prior to the first administration of substances to humans. Other
organ systems (e.g. the renal or gastrointestinal system), the functions of which can transiently
be disrupted by adverse pharmacodynamic effects without causing irreversible harm, are of
less immediate investigative concern (S. Whitebread et al., (2005), DDT, 10:1421-1433 –
R. Porsolt et al., (2005), Drug. Dev. Res., 64:83-89).
The objective of safety pharmacology studies are: (1) To identify undesirable pharmacodynamic
properties of a substance that may have relevance to its human safety, (2) To evaluate adverse
pharmacodynamic and/or pathophysiological effects of a substance observed in toxicology
and/or clinical studies and (3) To investigate the mechanism of the adverse pharmacodynamic
effects observed and/or suspected. (CPMP/ICH/39/00)
This Organ safety profile (full panel) serves as a complementary tool, to ADME and toxicology
profiling, to select compounds for the in vitro to in vivo transition. It contains 5 modules (Each
module can be purchased separately):
1 Ubiquitous targets (15 assays): Due to their expression in the nucleus, these targets are mainly
involved in the cell cycle.
2 Regulatory-oriented targets (5 assays): These targets, adapted to high throughput screening
mode, are recommended by various regulatory guidelines.
3 Brain panel (221 assays): These targets are expressed in brain.
4 Heart panel (120 assays): These targets are expressed in heart.
5 Lung panel (124 assays): These targets are expressed in lung.
Targets expressed in more than one organ are included in multiple modules.
Rationale for the selection of the most appropriate test systems
Test systems include receptors, ion channels, transporters and enzymes (kinases and others).
Relevant test systems have been selected so that scientifically valid information can be derived.
Assays have been selected according to sensitivity and reproducibility of the test system.
Selected test systems are performed according to standardized processes.
Isoform specific assays as opposed to non-specific assays, have been used when available.
Isoforms have been selected on the basis of their pharmacology behavior (if the same, only
1isoform in the family has been selected).
The Full panel (5 modules/270 assays) is recommended to investigate the potential undesirable
pharmacodynamic effects of a substance on physiological functions.
❚ Comprehensive KINASE profile [218 assays]
Ref. P20
Suggested testing: 10 µM (n=2)
Q 3 weeks
(Starting on Monday: Compounds
must be received at Cerep France
site on Friday before noon.)
The Comprehensive kinase profile is a broad panel containing 218 biochemical kinase assays
taking into consideration the vast diversity of families.
With a 3 week-turnaround time, it allows clients to profile compounds across all major families
in the human kinome (Manning G. et al. (2002) Science, 298: 1912-1934.) and to better
understand the selectivity of their drug candidates.
Our kinases are developed using two technologies: HTRF ® and LANCE ® . A similar process as
both technologies are TR-FRET allows rapid turnaround-time and low cost for our high throughput
selectivity screening.
For list of assays included in standard profiles and updated information:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
New profile Profile/module changed as compared to 2010: please go to www.cerep.com Q Standard turnaround time

Cerep standard profiles ❚
199
Drug screening
❚ ADME-tox option i (bioavailability) profile [6 assays]
Ref. P12
Q 2 weeks
The ADME-Tox - Option I [Bioavailability] profile provides useful compound bioavailability
information.
This profile combined with the ADME-Tox profile-option II and with pharmacology profiling data
will help optimize drug candidate selection.
Cerep
services
Receptors
Ion
channels
❚ ADME-tox option Ii (lead selection/prioritization) profile [13 assays]
Ref. P13
Q 2 weeks
The ADME-Tox - Option II [Lead selection/Prioritization] profile has been expanded from 8 to
13 assays. It focuses on early safety evaluation by providing drug-drug interaction, cytotoxicity
and cardiotoxicity information.
This profile combined with the ADME-Tox profile-option I and with pharmacology profiling data
is a rapid cost-effective way for prioritizing drug candidates.
Transporters
Kinases
❚ Genotoxicity profile [11 assays]
Ref.
Q 2 weeks
P14
For early genetic toxicity assessment, this profile includes the Ames fluctuation assay, evaluating
the mutagenic potential of chemicals and the in vitro micronucleus assay in CHO-K1 cells complementing
the Ames test in the evaluation of genotoxic effects like chromosomal damage.
Epigenetic &
DNA-related
enzymes
Drug development
The following CYP-based drug-drug interaction profile and P-gp mediated drug-drug interaction profile have been designed following
the latest FDA draft guidance 1 . These profiles comprise several modules, which can be purchased as a full panel or by module.
❚ CYP-based drug-drug interaction profile [23 assays]
FULL panel
Ref. P19
Q 3 weeks
MODULES
Module 1 Ref. P19-m1
Q 2 weeks
Module 2 Ref. P19-m2
Q 2 weeks
Module 3
Q 3 weeks
Ref. P19-m3
These assays will answer the questions in lines 177-197 of the FDA guidance: whether a test
compound is metabolized by and/or inhibits/induces any of these CYPs. Negative findings
from this profile could eliminate the need for later clinical investigations (however, the negative
finding should be interpreted in context, e.g. if in vivo concentration of a test compound is
greater than 10 µM, our negative finding in CYP inhibition at 10 µM may not eliminate the
need for further in vivo study).
The CYP-based drug-drug interaction profile contains 3 modules:
1 CYP phenotyping (10 assays): Human recombinant CYPs are used to evaluate whether the
test compound is specifically metabolized by one or more of the isozymes tested.
2 CYP inhibition (10 assays): Using unique, CYP specific substrates, the test compound is
evaluated for its ability to inhibit one or more of the isozymes tested within the context of a
human liver microsome matrix.
3 CYP induction (3 assays): Test concentrations used are defined around Cmax. The CYP1A,
CYP2B6, and CYP3A enzyme activities are measured in hepatocytes derived from three
different human donors to address the donor variability.
Other
enzymes
Specialized
cellular
assays
Standard
profiles
Testing
conditions
Ordering
information
1 FDA/CBER guidance for Industry on Drug Interaction Studies - Study Design, Data Analysis, and Implications for Dosing and Labeling; available on the internet at http://www.fda.gov/cber/
gdlns/interactstud.htm
Assay list
& index

200 in vitro pharmacology 2011 catalog
❚ Cerep standard profiles
❚ P-gp mediated drug-drug interaction profile [14 assays]
FULL panel
Ref. P21
Q 4 weeks
MODULES
Module 1 Ref. P21-m1
Q 4 weeks
Module 2 Ref. P21-m2
Q 4 weeks
P-glycoprotein (P-gp) is an efflux pump located in the intestine and blood-brain barrier among
other tissues. Compounds that are substrates for P-gp may be secreted back into the lumen of
the intestine. Additionally, compounds may be inhibitors of P-gp, and interfere with the efflux
of concurrently administered drugs, resulting in potentially toxic levels and severe side effects.
Compounds that are P-gp substrates may or may not inhibit P-gp activity. Similarly, compounds
that are P-gp inhibitors may or may not be substrates for P-gp.
The FDA draft guidance for industry on drug interaction studies addresses study design and data
analysis for evaluating P-gp substrates and inhibitors. It recommends the bi-directional transport
assay as the definitive assay for identifying P-gp substrates and inhibitors since this measures
drug efflux in a more direct manner than other methods.
The P-gp-mediated drug-drug interaction profile is a set of assays designed to comply with
the FDA draft guidance recommendations.
The P-gp mediated drug-drug interaction profile contains 2 modules:
1 P-gp substrate evaluation (12 assays):
Step I assays are designed to assess a compound's non-specific binding and determine the
efflux ratio and linear flux range.
Step II assays are designed to confirm whether the efflux activity is related to P-gp by including
P-gp inhibitors and to evaluate the concentration dependence of the test compound.
2 P-gp inhibitor evaluation (2 assays):
Assays are designed to determine the IC 50 value of the test compound.
For list of assays included in standard profiles and updated information:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
New profile Profile/module changed as compared to 2010: please go to www.cerep.com Q Standard turnaround time

Cerep standard profiles ❚
201
Sample size
❚ minimum compound amount (including IC 50 follow-up)
Cerep
services
Values are based on a molecular weight ≤ 500 g/mol and a typical testing concentration of 10 µM in duplicate (including a possible retest).
Screening
Weight
(pre-weighed)
Volume
(100% DMSO)
Screening + Follow up
with highest concentration at 10 µM 1
Weight
(pre-weighed)
Volume
(100% DMSO)
Number of assays
standard profiles
ExpresSProfile 55 1 mg 125 µL @ 10 mM 1.1 mg 220 µL @ 10 mM
High-Throughput profile 80 1 mg 170 µL @ 10 mM 1.4 mg 270 µL @ 10 mM
ExpresS Diversity kinase profile 48 1 mg 140 µL @ 10 mM 1 mg 190 µL @ 10 mM
Cellular functional GPCR profile 60 2 3.25 mg 650 µL @ 10 mM 10 mg 2000 µL @ 10 mM
PDE high-throughput profile 13 1mg 200 µL @ 10 mM 1.4 mg 275 µL @ 10 mM
Non-kinase enzyme profile 42 1 mg 185 µL @ 10 mM 1.5 mg 300 µL @ 10 mM
Diversity profile 101 1 mg 200 µL @ 10 mM 2 mg 400 µL @ 10 mM
BioPrint ® profile (Full profile) 159 3.4 mg 475 µL @ 10 mM 6.8 mg 1350 µL @ 10 mM
BioPrint ® in vitro pharmacology profile 139 1.4 mg 275 µL @ 10 mM 3.8 mg 750 µL @ 10 mM
Organ safety profile 270 3 9 mg 360 µL @ 50 mM 9 mg 360 µL@ 50 mM
Comprehensive kinase profile 218 2.5 mg 500 µL @ 10 mM 4.5 mg 850 µL @ 10 mM
ADME-Tox - Option I [Bioavailability] 6 1 - 2 mg 125 µL @ 10 mM inquire inquire
ADME-Tox - Option II [Lead selection/Prioritization] 13 1 - 2 mg 125 µL @ 10 mM inquire inquire
Genotoxicity profile 11 5 mg 200 µL @ 50 mM inquire inquire
CYP-based drug-drug interaction profile 23 3 10 mg – inquire –
P-gp mediated drug-drug interaction profile 14 3 20 mg – inquire –
1 Assuming ~10% of test in IC 50 . Usually, for 1 IC 50 : 30 µL @ 10 mM and + 25 µL @ 10 mM by additional IC 50 .
2 30 targets (agonist and antogonist effects)
3 Full panel. For compound amount needed for separate modules: please inquire
Receptors
Ion
channels
Transporters
Kinases
Epigenetic &
DNA-related
enzymes
For Screening + Follow-up sample sizes, with highest concentration at 100 µM:
Please go to www.cerep.com catalog online
Other
enzymes
Specialized
cellular
assays
Standard
profiles
Testing
conditions
Ordering
information
Assay list
& index

202 in vitro pharmacology 2011 catalog

203
testing
conditions
Binding, enzyme & cellular assays p. 204
Tissue assays p. 205

204 in vitro pharmacology 2011 catalog
testing
conditions
❚ binding, enzyme and cellular assays
❚ suggested testing
Primary screening at 1-10 µM in duplicate (2 wells), follow-up for IC 50 /Ki or EC 50 determination (8 concentrations in duplicate (16
wells) when compound displays more than 50% inhibition of control value or 50% stimulation relative to control.
For functional GPCR cellular assays: assessment of agonist and/or antagonist effects.
❚ sample size (including IC 50 /EC 50 follow-up studies)
See table page 209.
❚ requested compound information
To reduce the registration time and ensure that all the appropriate information is available to start the study in a shortest possible
timeframe, please use Cerep compound submission form 1 or MS Excel file 2 , and provide the following compound information:
Name (compound ID) / Batch # / Molecular weight 3 / Formula weight 4 / Stock concentration / Stock solvent / Quantity /
Unit 5 / Form / Storage conditions / Solubility, as well as Plate ID / plate position for compounds delivered in plates,
Comments 6 , and Quotation number.
NOTE: Impurity and colored compounds might affect the results (compound color information is mentioned in the study report).
General remarks:
- If compound(s) are supplied as a stock solution in plate(s) (preferred format for any submission of 10 or more compounds),
please leave columns 1 and 12 empty in a 96W plate. The 384W plate format is also acceptable with columns 1, 2,
23 and 24 empty. For any other plate format, please inquire.
- If compound(s) are not soluble in 100% DMSO, please provide any useful information concerning the solubility of the compound.
The following solvents are compatible with most of our assays: DMSO (Cerep standard), H 2 O, Methanol, Tris/HCl 10 mM pH 7.4.
- Organic solvents such as acetone, chloroform, ether, acetonitrile, tetrahydrofuran and trifluoroacetic acid are not recommended
as they will significantly affect the results from many in vitro assays, even at very low concentrations.
Customized handling procedure of compounds can be accommodated, please inquire for pricing conditions.
❚ protocol
A typical protocol for binding assays includes a minimum of 6-control wells (non-specific and total binding) with or without vehicle
for solvent-soluble compounds, plus an 8-point dose-response of the relevant reference compound.
The binding assays that are performed using an agonist radioligand are labeled as such in the assay description. This assay
design should pick more easily the test compounds that are agonists.
For radioligand binding assays, how should I choose between the agonist and the antagonist models when both are
available?
For some binding assays two models are available using either agonist or antagonist as radioligand.
G-protein-coupled receptors have both high-affinity and low-affinity states that are bound differently by agonists and antagonists.
Whereas the antagonists bind with an equal affinity to both affinity states, agonists bind poorly to the low affinity state
of the receptor. Therefore, it is advisable to use an antagonist radioligand to evaluate the binding of antagonists knowing
that this may fail to reveal the binding of agonists. On the other hand, an assay using an agonist radioligand is suitable to
evaluate both agonists and antagonists. The testing of a compound in both assays and the comparison of its competition
curves against each radioligand may provide information about its functional activity at the receptor.
A typical protocol for enzyme and all cellular assays includes a minimum of 6-control wells (background, and maximal signal
with and without vehicle) plus an 8-point dose-response of the relevant reference compound.
What kind of information cellular functional GPCR assays can bring about my compounds?
Most our cellular functional GPCR assays are designed to determine if compounds induce agonist-like and/or antagonist
activity.
Those assays also allow to detect allosteric modulators with a modified protocol. Please inquire.
Finally, 10 assays are specifically designed to detect inverse agonists. For other targets, please inquire
1 Cerep compound submission form will be emailed to you with your quotation. A copy can be requested from sales@cerep.com, or downloaded from Cerep website: www.
cerep.com/Catalog Online
2 Systematically required for studies of 10 compounds or more.
3 Molecular weight (MW) of free acid or base form.
4 Formula weight (FW) including salt form and/or hydrate form if applicable.
5 mg?, mL?
6 e.g. useful information such as sensitivity to light, stability or hygroscopicity issues.

205
The reference compound for each assay is listed in each assay description. The historical average IC 50 /EC 50 value is also
shown in each assay description.
Any of our assay protocols can be customized: Please inquire
❚ deliverables
Percent inhibition (mean of replicates), individual values as percent of control, EC 50 or IC 50 value (calculated from a minimum
5 concentration testing), Ki value for receptor binding assays (calculated using Cheng-Prussof equation, and the true Kd of the
membrane preparation used for the experiment), K Bapp for functional GPCR cellular assays, Hill coefficient (nH), and plotted
EC 50 or IC 50 curves.
NOTE: The Kd values mentioned in the catalog are indicative values only.
❚ data turnaround
Complete data set is typically available within 3 weeks, after receipt of the compounds at the testing site, for all the binding
assays and most of the enzyme assays (providing that we receive all available information to initiate the study). The cell-based
assays (including the functional assays) would require 3 to 6 weeks for data delivery.
Secure, password-protected data can be viewed on line as soon as they are produced, after scientific approval and QC-ed
by an experienced technician.
For majority of assays, ExpresScreen option (5 business day turnaround time) is available: please inquire.
Cerep
services
Receptors
Ion
channels
Transporters
❚ tissue assays
❚ suggested testing
Qualitative screening
Assessment of both agonism and antagonism at 3 concentrations in duplicate (2 tissues)
Suggested test concentrations: 1, 3 and 10 times the IC 50 /K i binding value
Catalog prices correspond to this combination.
Follow-up testing for quantitative determination of pharmacological parameters
EC 50 /pD 2 values of agonists at 6-8 concentrations in duplicate
IC 50 values of antagonists at 6-8 concentrations in duplicate
pA 2 or pD’ 2 values of antagonists at 3 concentrations, each at least in triplicate
Prices upon request.
❚ sample size (including IC 50 follow-up studies)
See information page 210.
❚ protocol
Agonism/antagonism assessment
The agonist activity is evaluated by exposing the tissues to increasing concentrations of the compounds. Where an agonistlike
response is obtained, the reference antagonist is tested against the highest test concentration to confirm the involvement
of the receptor studied in this response. A reference full agonist is used as a positive control.
The antagonist activity is evaluated by testing increasing concentrations of the compounds against a single concentration of
the reference agonist. A reference antagonist is used as a positive control.
EC 50 /pD 2 values for agonists, IC 50 values for antagonists and maximum responses (Emax)
Same protocols as above, with full concentration response curves.
pA 2 or pD’ 2 values for antagonists
Concentration-response curves to the reference full agonist are obtained in the absence (control) and in the presence of a
fixed concentration of the compound. The resulting changes in the agonist curves are used to determine a pA 2 value for
competitive antagonism (decrease in the pD 2 value of the agonist) or a pD’ 2 value for non-competitive antagonism (decrease
in the maximum response to the agonist).
Any of our assay protocols can be customized: Please inquire
❚ deliverables
Mean percent of control values, EC 50 /pD 2 , IC 50 , pA 2 or pD’ 2 values.
Concentration-response curves.
❚ data turnaround
Complete data set is typically available 4 weeks after receipt of the compound at the testing site.
Kinases
Epigenetic &
DNA-related
enzymes
Other
enzymes
Specialized
cellular
assays
Standard
profiles
Testing
conditions
Ordering
information
Assay list
& index

206 in vitro pharmacology 2011 catalog

207
ordering
information
Quotation request p. 208
Master service agreement p. 208
Requested compound information p. 208
Sample size p. 209
Shipment instructions p. 210
Study initiation p. 211
Turnaround time p. 211
Results reporting p. 211

208 in vitro pharmacology 2011 catalog
ordering
information
❚ quotation request
Email your request for a quotation to sales@cerep.com and copy our customer support teams:
In vitro pharmacology requests . customer.support@cerep.fr
ADME/PK-Tox requests . customersupportUS@cerep.com
Please detail your information including location, phone and fax #, the assays (and reference numbers) to be quoted, the number of
compounds for each assay and the number of concentrations for each compound. Standard quotations for catalog assays will be
returned to you by email within 48 hours maximum, and in most cases within 24 hours, of receipt at customer support. Customized
quotations will be returned within 5 business days.
Your quotation number becomes your study number.
Cerep Order form.xls document can be used to facilitate the quotation process, but is not required. A copy can be emailed to you,
request it from sales@cerep.com.
note: Please review your quotation carefully to ensure that it includes the assays, the test concentrations and other specifications
that concur with your request. We will try our best to interpret your inquiry, however, the quotation is what we will use to determine
how and what we perform, and once the assays have been launched in production, it will be due as per the quotation.
❚ Master service agreement
Simultaneous to quotation processing and if it is the first time you work with Cerep, we will prepare a Master Service Agreement
for your company and send it in an e-mail. This also serves as your confidentiality agreement.
Your legal counsel may have questions or propose changes. These must be reviewed by our in-house counsel at legal@cerep.fr.
Once the content has been agreed upon by both parties, fax a signed copy, and send two signed originals to Cerep legal department
who will have them signed, and will return one fully executed agreement to you.
Counsel - Legal department
Cerep - Le Bois l’Evêque - 86600 Celle l’Evescault - FRANCE
Tel +33 (0)5 49 89 30 00 - Fax +33 (0)5 49 43 21 70 - e-mail: legal@cerep.fr
❚ requested compound information
To reduce the registration time and ensure that all the appropriate information is available to start the study in a shortest possible
timeframe, please use Cerep compound submission form 1 or MS Excel file 2 , and provide the following compound information:
Name (compound ID) / Batch # / Molecular weight 3 / Formula weight 4 / Stock concentration / Stock solvent / Quantity /
Unit 5 / Form / Storage conditions / Solubility, as well as Plate ID / plate position for compounds delivered in plates, Comments
6 , and Quotation number.
NOTE: Impurity and colored compounds might affect the results (compound color information is mentioned in the study report).
General remarks:
- If compound(s) are supplied as a stock solution in plate(s) (preferred format for any submission of 10 or more compounds),
please leave columns 1 and 12 empty in a 96W plate. The 384W plate format is also acceptable with columns 1, 2, 23
and 24 empty. For any other plate format, please inquire.
- If compound(s) are not soluble in 100% DMSO, please provide any useful information concerning the solubility of the compound.
The following solvents are compatible with most of our assays: DMSO (Cerep standard), H 2 O, Methanol, Tris/HCl 10 mM
pH 7.4.
- Organic solvents such as acetone, chloroform, ether, acetonitrile (except for CYP assays), tetrahydrofuran and trifluoroacetic acid
are not recommended as they will significantly affect the results from many in vitro assays, even at very low concentrations.
1 Cerep compound submission form will be emailed to you with your quotation. A copy can be requested from sales@cerep.com, or downloaded from Cerep website: www.cerep.
com/Catalog Online
2 Systematically required for studies of 10 compounds or more.
3 Molecular weight (MW) of free acid or base form.
4 Formula weight (FW) including salt form and/or hydrate form if applicable.
5 mg?, mL?
6 e.g. useful information such as sensitivity to light, stability or hygroscopicity issues.

209
REQUESTED COMPOUND INFORMATION ❚
Remarks for ADME-Tox assays:
- Any study including mass spectrometry (MS) assays (such as stability, permeability, protein binding) requires both molecuular
weight (MW) and formula weight (FW) of each tested compound, even if they are the same. The FW is required to prepare
the stock solution of each compound at the correct concentration. The MW gives indication on which expected molecular ion
to look for in the LC-MS analysis of samples.
- Chemical structure or list of the ionizable groups is required for ionization constant (pKa) assay.
- Solubility information is useful and recommended for pKa and genotoxicity testing (due to high test concentrations).
Warning: Cerep will apply the standard solubilization process described in the flow chart below when compounds are received
at the testing site, unless special instructions are provided with the compounds.
Customized handling procedure of compounds can be accommodated, please inquire for pricing conditions.
Cerep
services
Receptors
cerep compound management process
Standard solubilization process
[diagram]
DMSO solvents are stored
under nitrogen to minimize
potential oxidation and water
absorption.
NOTE: Covaris: this device sends
acoustic energy waves from a
transducer that converges and
focuses on a small area. Covaris
processing of compounds is done
isothermally maintaining temperature
between 20 and 25°C.
Dedicated team
Daily dilutions in 100% fresh DMSO
Only 1 freeze/thaw cycle in standard
process to minimize precipitation
Constant concentration of solvent
in the assays
Cherry-picking and multiplexing
expertise
Customized handling procedure of
compounds upon request
POWDER
FORM
more
Weighing in a glass tube
Solubilization at 10 mM
in DMSO
Covaris processing
NO
Diluted down to 5 mM in DMSO
Covaris processing
NO
Diluted down to 1 mM in DMSO
Covaris processing
NO
less
YES
YES
YES
less
Solubilization in client's vial
(except for 1 dram glass vial)
Solubilization at 10 mM in DMSO
Vortexing 10 min
Solubilization in client's vial
(when in 1 dram glass vial)
Solubilization at 10 mM
in DMSO
Covaris processing
YES
Ready to be dispatched
in aliquots storage
at -20°C
Study interrupted - Client contacted
NO
Sonication
YES
NO
Diluted down to 5 mM in DMSO
Vortexing 10 min
YES
NO
Diluted down to 1 mM in DMSO
Vortexing 10 min
YES
NO
Ion
channels
Transporters
Kinases
Epigenetic &
DNA-related
enzymes
Other
enzymes
❚ sample size [minimum compound amount - including IC 50 /EC 50 follow-up studies]
❚
Binding, enzyme and cellular assays
Assuming a molecular weight ≤ 500 g/mol and a testing concentration of 10 µM in duplicate (including a possible retest).
Screening
Screening + Follow up
with highest concentration at 10 µM 1
Weight (pre-weighed) Volume (100% DMSO) Weight (pre-weighed) Volume (100% DMSO)
Individual binding, enzyme and cellular catalog assays
1 to 3 assays 1 mg 25 µL @ 10 mM 1 mg 60 µL @ 10 mM
4 to 5 assays 1 mg 35 µL @ 10 mM 1 mg 70 µL @ 10 mM
6 to 10 assays 1 mg 50 µL @ 10 mM 1 mg 100 µL @ 10 mM
11 to 15 assays 1 mg 65 µL @ 10 mM 1 mg 110 µL @ 10 mM
16 to 20 assays 1 mg 75 µL @ 10 mM 1 mg 125 µL @ 10 mM
21 to 40 assays 1 mg 100 µL @ 10 mM 1.5 mg 250 µL @ 10 mM
41 to 50 assays 1 mg 150 µL @ 10 mM 2 mg 275 µL @ 10 mM
51 to 70 assays 1.5 mg 225 µL @ 10 mM 2.5 mg 400 µL @ 10 mM
71 to 100 assays 2 mg 300 µL @ 10 mM 3 mg 550 µL @ 10 mM
101 to 135 assays 2 mg 350 µL @ 10 mM 4 mg 650 µL @ 10 mM
136 to 150 assays 2.5 mg 400 µL @ 10 mM 4 mg 750 µL @ 10 mM
151 to 200 assays 3 mg 500 µL @ 10 mM 5 mg 1000 µL @ 10 mM
201 to 250 assays 3.5 mg 600 µL @ 10 mM inquire inquire
1 Assuming ~10% of test in IC 50 . Usually, for 1 IC 50 : 30 µL @ 10 mM and + 25 µL @ 10 mM by additional IC 50 .
Specialized
cellular
assays
Standard
profiles
Testing
conditions
Ordering
information
Assay list
& index

210 in vitro pharmacology 2011 catalog
❚ sample size
❚
❚
tissue assays
For screening at 3 concentrations in duplicate (2 tissues) or follow-up: sufficient amount to prepare 150 µL of a 1000-fold
concentrated solution relative to the highest test concentration for each assay.
Maximum tolerable final DMSO concentration: 0.1%.
adme-tox assays
Assuming a molecular weight ≤ 500 g/mol and assays tested at default concentrations (including retest).
Weight (pre-weighed)
Volume (100% DMSO)
Individual adme-tox catalog assays
1 to 20 assays 1 - 2 mg 200 µL @ 10 mM (50 µL min)
1 to 10 IC 50 follow-up assays 1.5 - 2 mg 250 µL @ 10 mM (50 µL min)
Weights needed in addition to the general weight required for 1 to 20 ADME-Tox assays:
. pKa 3 x 1.5 mg –
. CYP1A, 2B6 & 3A induction (3 donors) 6 mg (2 mg/CYP) 120 µL @ 100 mM
. Ames (3 strains) 4 mg 800 µL @ 10 mM
. in vitro micronucleus 1 mg 40 µL @ 50 mM
. typical rat PK 1 25 mg –
. typical mouse PK (serial sampling) 1 10 mg –
. typical mouse PK (parallel sampling) 1 20 mg –
. typical rat BBB 2 15 mg –
. typical mouse BBB 2 10 mg –
. Plasma sample for quantitative bioanalysis – 100 µL
1 2 routes, 1 dose: 1 mg/kg for IV and 5 mg/kg for PO, n=3
2 1 route, 1 dose: 1 mg/kg for IV, 3 time points, n=3
❚
standard profiles
Values are based on a molecular weight ≤ 500 g/mol and a typical testing concentration of 10 µM in duplicate (including
a possible retest).
Screening
Weight
(pre-weighed)
Volume
(100% DMSO)
Screening + Follow up
with highest concentration at 10 µM 1
Weight
(pre-weighed)
Volume
(100% DMSO)
Number of assays
standard profiles
ExpresSProfile 55 1 mg 125 µL @ 10 mM 1.1 mg 220 µL @ 10 mM
High-Throughput profile 80 1 mg 170 µL @ 10 mM 1.4 mg 270 µL @ 10 mM
ExpresS Diversity kinase profile 48 1 mg 140 µL @ 10 mM 1 mg 190 µL @ 10 mM
Cellular functional GPCR profile 60 2 3.25 mg 650 µL @ 10 mM 10 mg 2000 µL @ 10 mM
PDE high-throughput profile 13 1mg 200 µL @ 10 mM 1.4 mg 275 µL @ 10 mM
Non-kinase enzyme profile 42 1 mg 185 µL @ 10 mM 1.5 mg 300 µL @ 10 mM
Diversity profile 101 1 mg 200 µL @ 10 mM 2 mg 400 µL @ 10 mM
BioPrint ® profile (Full profile) 159 3.4 mg 475 µL @ 10 mM 6.8 mg 1350 µL @ 10 mM
BioPrint ® in vitro pharmacology profile 139 1.4 mg 275 µL @ 10 mM 3.8 mg 750 µL @ 10 mM
Organ safety profile 270 3 9 mg 360 µL @ 50 mM 9 mg 360 µL@ 50 mM
Comprehensive kinase profile 218 2.5 mg 500 µL @ 10 mM 4.5 mg 850 µL @ 10 mM
ADME-Tox - Option I [Bioavailability] 6 1 - 2 mg 125 µL @ 10 mM inquire inquire
ADME-Tox - Option II [Lead selection/Prioritization] 13 1 - 2 mg 125 µL @ 10 mM inquire inquire
Genotoxicity profile 11 5 mg 200 µL @ 50 mM inquire inquire
CYP-based drug-drug interaction profile 23 3 10 mg – inquire –
P-gp mediated drug-drug interaction profile 14 3 20 mg – inquire –
1 Assuming ~10% of test in IC 50 . Usually, for 1 IC 50 : 30 µL @ 10 mM and + 25 µL @ 10 mM by additional IC 50 .
2 30 targets (agonist and antogonist effects)
3
Full panel. For compound amount needed for separate modules: please inquire
For Screening + Follow-up sample sizes, with highest concentration at 100 µM:
Please go to www.cerep.com catalog online
❚ shipment instructions
Please include study number (i.e. quotation number, see above Quotation request) on the shipping documents, and include the
Compound submission form or MS Excel file (see Requested compound information, page 5) and attach it to the compounds.
Form
- Dry powder, or
- 10 mM DMSO stock solution.

shipment instructions ❚
211
Format
- Securely closed vials, or
- Individual 2D barcode tubes, or
- Sealed 96-well plates (all SBS format standard plates are accepted): columns 1 and 12 empty and test compounds placed
in A2-H11 column-wise, or
- Sealed 384-well plates (all SBS format standard plates are accepted): columns 1, 2, 23 and 24 empty and test compounds
placed in A3-P22 column-wise.
For any other form and/or format: please inquire.
For frozen samples, please allow for enough dry ice to arrive frozen at Cerep site. In addition, it is very important to show on
documents and mark on package that compound(s) must be kept in dry ice during all the shipping period (from its collection to its
delivery at the Cerep site).
Compounds can be shipped 7 to any of the two sites below (Cerep will manage the compound transfer to the other testing site
when necessary):
Cerep
Attn: Compound receipt manager
Le Bois l’Evêque
86600 Celle l’Evescault - FRANCE
Tel. +33 (0)5 49 89 30 00
Cerep
Attn: Compound receipt manager
15318 NE 95th St
Redmond, WA 98052 - USA
Tel. +1 425 895 8666
Every shipment of compounds going through customs must include a commercial invoice.
For shipments going through US customs: a TSCA form (Toxic Substance Control Act) is required (templates are available upon request).
For customers located in China, compounds can be shipped to:
Cerep ( 西 海 珀 )
Attn: Compound receipt manager
上 海 张 江 高 科 技 区 爱 迪 生 路 326 号 302-1 室 (326 Aidisheng Road, B 302-1)
Zhangjiang High-Tech Park
Shanghai 201203 - CHINA
tel. +86 21 5132 0568
To assist Cerep in efficiently processing compounds upon receipt, the following information is helpful to ensure the appropriate
follow-up of shipment and streamlined initiation of the testing:
Advance notice of shipment to Cerep – e-mail: compoundreceipt@cerep.com
Shipment tracking number
Cerep
services
Receptors
Ion
channels
Transporters
Kinases
Epigenetic &
DNA-related
enzymes
❚ Study initiation
To initiate a study (following compound shipment): Fax your signed quotation or attach it to the e-mail accepting it 8 with purchase
order number, to:
For in vitro pharmacology assays: Customer support France: Fax +33 (0)5 49 43 21 70 – e-mail: customer.support@cerep.fr
For ADME/PK-Tox assays: Customer support USA: Fax +1 (425) 895 8668 – e-mail: customersupportUS@cerep.com
An acknowledgement of shipment receipt will be emailed to you when the shipment has arrived at the laboratory location.
Your signed quotation is your commitment that you wish us to run exactly the assays and the concentrations that are included in
the quotation. Please check it carefully.
Other
enzymes
Specialized
cellular
assays
❚ Turnaround time
The turnaround time indicated in the quotation starts the day following receipt of compounds at the Cerep testing site for compounds
received before 12:00 pm, unless otherwise specified with the client, and considering that the test compounds are received along
with all the necessary information to initiate the study (quotation acceptance and requested compound information). If received
after 12:00 pm, the study is initiated on the second day following receipt.
For majority of assays, ExpresScreen option (5 business day turnaround time) is available: please inquire.
❚ Results reporting
A Data Online account allowing visualization of the results as they are produced will be set-up when we receive your signed quotation
to initiate the study. Your user name and password will be faxed to you. Please modify them to ensure confidentiality.
Log on to https://www.cerep.com/secure to view your results that are posted as soon as validated. Daily updates are highlighted
with ”NEW” information since your last log-in and are listed first. You will have the option to convert the data to MS Excel format
and download it. Use the user name and password Demo to try out the site.
For details on DATA ONLINE, see page 9.
7 Preferred carriers: FedEx for room temperature and World Courier for dry ice shipment.
8 Your study will not begin until a signed quotation with purchase order # is received.
Standard
profiles
Testing
conditions
Ordering
information
Assay list
& index

212 in vitro pharmacology 2011 catalog

213
assay list
& index

214 in vitro pharmacology 2011 catalog BMPR1A kinase (ALK3) 149
❚ assay list & index
5-HT 1A 69
5-HT 1A - agonist radioligand 68
5-HT 1B 69
5-HT 1B - antagonist radioligand 69
5-HT 1D 69
5-HT 1D - agonist radioligand 69
5-HT 2A 70
5-HT 2A - agonist radioligand 70
5-HT 2A - antagonist radioligand 69
5-HT 2B 71
5-HT 2B - agonist radioligand 71
5-HT 2B - antagonist radioligand 70
5-HT 2C 71
5-HT 2C - agonist radioligand 71
5-HT 2C - antagonist radioligand 71
5-HT 3 90,101
5-HT 3 - antagonist radioligand 90,101
5-HT 4 72
5-HT 4e 72
5-HT 4e - antagonist radioligand 72
5-HT 5a - agonist radioligand 72
5-HT 6 72
5-HT 6 - agonist radioligand 72
5-HT 7 73
5-HT 7 - agonist radioligand 73
5-HT (non-selective)- agonist radioligand 68
5-HT release (activator effect) 186
5-HT release (inhibitor effect) 186
5-HT transporter - antagonist radioligand 105
5-HT uptake 105
5-lipoxygenase 177
12-lipoxygenase 177
15-lipoxygenase 178
[A]
A 1 13,14
A 1 - agonist radioligand 13
A 1 - antagonist radioligand 13
A 1 - inverse agonist effect 13
A 2A 14
A 2A - agonist effect 14
A 2A - agonist radioligand 14
A 2A - inverse agonist effect 14
A 2B 15
A 2B - antagonist radioligand 15
A 3 15
A 3 - agonist radioligand 15
Abl kinase 118
ACE 171
ACE-2 171
acetylcholinesterase 179
acetyl CoA synthetase 182
Ack 118
Activation of granulocyte adhesion proteins:
- HL-60/HUVEC 191
Activation of monocyte adhesion proteins:
- matrix proteins 191
- U-937/HUVEC 191
Adenosine 13,103
adenosine transporter - antago. radioligand 103
adenosine uptake 103
adenylyl cyclase (activator effect) 181
adenylyl cyclase (inhibitor effect) 181
ADME profiling (in vitro) 4
Adrenergic 16
AGC (protein-serine/threonine kinases) 137
agonism/antagonism assessment 205
agonist radioligand 204
Akt1/2 137
Akt1/PKBa 137
Akt2/PKBb 137
Akt3/PKBg 137
ALK 108
ALK4 (ACVR1B) 149
alpha 1A 16
alpha 1A - antagonist radioligand 16
alpha 1B 17
alpha 1B - antagonist radioligand 17
alpha 1D - antagonist radioligand 17
alpha 1 (non-selective) 16
alpha 1 (non-selective)- antagonist radioligand 16
alpha 2A 18
alpha 2A - agonist radioligand 18
alpha 2A - antagonist radioligand 18
alpha 2B 18
alpha 2B - antagonist radioligand 18
alpha 2C 19
alpha 2C - agonist radioligand 19
alpha 2C - antagonist radioligand 19
alpha 2 (non-selective) 18
alpha 2 (non-selective)- antagonist radioligand 17
AMPA - agonist radioligand 86,98
AMPKa 130
anandamide uptake 103
Angiotensin II 21
ANP - agonist radioligand 83
antagonist radioligand 204
Apelin 22
APJ (apelin) 22
APJ (apelin)- agonist radioligand 22
Arachidonic acid metabolism 177
Arachidonic acid metabolite secretion 187
AR - agonist radioligand 79
arginase 1 182
Arg kinase 118
ASK1 144
Aspartic proteases 170
Assay design & development 4
AT 1 21
AT 1 - antagonist radioligand 21
AT 2 - agonist radioligand 22
ATPase (H + /K + ) 182
ATPase (Na + /K + ) 182
ATPases 182
Atrial natriuretic peptide 83
Atypical kinases 156
AurA/Aur2 kinase 151
AurB/Aur1 kinase 151
AurC/Aur3 kinase 152
automated patch-clamp 94,96,97
Axl kinase 108
[B]
B 1 24
B 1 - agonist radioligand 24
B 2 25
B 2 - agonist radioligand 24
BACE-1 (β-secretase) 170
BB 1 23
BB 1 - agonist radioligand 22
BB 2 23
BB 2 - agonist radioligand 23
BB 3 23
BB 3 - agonist radioligand 23
BB (non-selective)- agonist radioligand 22
Benzodiazepine 83
beta 1 19,20
beta 1 - agonist radioligand 19
beta 1 - inverse agonist effect 19
beta 2 20
beta 2 - agonist radioligand 20
beta 2 - inverse agonist effect 20
beta 3 21
beta 3 - antagonist radioligand 20
binding assays 5,6,7,43,204,209
binding kinase assays 107
biochemical assays (tool-box) 6
biochemical kinase assays 107
BioPrint ® profile & services 7
BLK 118
BLT 1 (LTB 4 ) 44
BLT 1 (LTB 4 )- agonist radioligand 44
BMX (Etk) kinase 118
Bombesin 22
Bradykinin 24
B-raf kinase 149
Brk 119
BRSK1 130
BTK 119
BZD (central)- agonist radioligand 85,98
BZD (peripheral)- antagonist radioligand 83
[C]
c-kit kinase 108
c-Met kinase 108
c-Met kinase (HGFR) 108
C5a 31
C5a - agonist radioligand 31
Ca 2+ - ATPase pump 186
Ca 2+ channels 93,102
Ca 2+ - L 93
Ca 2+ - L (dihydropyridine site) - antagonist
radioligand 93
Ca 2+ - L (diltiazem site) (benzothiazepines)
- antagonist radioligand 93
Ca 2+ - L (verapamil site) (phenylalkylamine)
- antagonist radioligand 93
Ca 2+ - N - antagonist radioligand 94
Calcitonin 25
Calcitonin gene-related peptide 26
Calcium sensing 26
CaMK1a 130
CaMK1d 131
CaMK2a 131
CaMK2g 131
CaMK4 131
CaMK (protein-serine/threonine kinases) 130
Cannabinoid 27,103
CAR 80
carbonic anhydrase II 183
CAR - inverse agonist effect 80
CaS 26
caspase-1 168
caspase-2 168
caspase-3 169
caspase-6 169
caspase-7 169
caspase-8 169
caspase-9 169
caspase-10 169
cathepsin B 170
cathepsin D 170
cathepsin E 171
cathepsin G 167
cathepsin H 170
cathepsin L 170
cathepsin X 170
CB 1 27
CB 1 - agonist radioligand 27
CB 1 - inverse agonist effect 27
CB 2 28
CB 2 - agonist radioligand 27
CB 2 - inverse agonist effect 28
CCK 1 (CCK A ) 30
CCK 1 (CCK A )- agonist radioligand 30
CCK 2 (CCK B ) 31
CCK 2 (CCK B )- agonist radioligand 30
CCR1 28
CCR1 - agonist radioligand 28
CCR2 29
CCR2 - agonist radioligand 28
CCR3 29
CCR3 - agonist radioligand 29
CDC2/CDK1 (cycB) 124
CDC7/ASK 152
CDK2 (cycA) 124
CDK3 (cycE1) 124
CDK4 (cycD1) 124

215
CDK5/p35 124
CDK6 (cycD3) 125
CDK7/MAT1 (cycH) 125
CDK8 (cycC) 125
CDK9 (cycT1) 125
Cell adhesion 190
cell-based assay development (tool-box) 5
Cell migration 192
Cell proliferation 192
cellular assays 185,204,209
cellular functional GPCR assays 43
cellular kinase assays 107
Cell viability 193
cell viability 193
CENP-E 157
cerep services 4
CGRP 26
CGRP - agonist radioligand 26
Chemokines 28
Chemokine secretion 188
CHK1 131
CHK2 131
Cholecystokinin 30
Choline 103
choline transporter (CHT1)- antagonist
radioligand 103
CK1a 144
CK1e 144
CK2 (casein kinase 2) 125
CK1 (protein-serine/threonine kinases) 144
Class A Orphans 62
Cl - channel (GABA-gated)- antagonist
radioligand 86,98
CLK1 125
CLK2 126
CMGC (protein-serine/threonine kinases) 124
Complement 5a 31
Compound:
- form & format 210
- frozen samples 211
- requested information 208
- management process 209
- shipment 210
- submission form 208,210
Compound management 4
COMT (catechol-O-methyl transferase) 179
confidentiality (Master service agreement) 208
constitutive NOS (cerebellar) 177
constitutive NOS (endothelial) 177
Contacts (Cerep contacts) back cover
conventional patch-clamp 94,96,98
Corticotropin releasing factor 31
COT kinase (MAP3K8) 145
COX 1 178
COX 2 178
CRF 1 31
CRF 1 - agonist radioligand 31
CRF 2a 32
CRF 2a - agonist radioligand 32
CRIK 137
CSK 119
CT (calcitonin) 25
CT (calcitonin)- agonist radioligand 25
CTK 119
CTK (protein-tyrosine kinases) 118
customer support 208,211
custom offer 185
CXCR2 (IL-8B) 29
CXCR2 (IL-8B)- agonist radioligand 29
CXCR4 30
CXCR4 - agonist radioligand 29
Cyclases 181
CysLT 1 (LTD 4 ) 44
CysLT 1 (LTD 4 )- agonist radioligand 44
CysLT 2 (LTC 4 ) 45
CysLT 2 (LTC 4 )- agonist radioligand 44
Cysteine proteases 168
Cytokines 83
Cytokine secretion 188
[D]
D 1 32
D 1 - antagonist radioligand 32
D 2 33
D 2L - antagonist radioligand 33
D 2S 33
D 2S - agonist radioligand 33
D 2S - antagonist radioligand 33
D 3 34
D 3 - agonist radioligand 34
D 3 - antagonist radioligand 33
D 4.4 34
D 4.4 - antagonist radioligand 34
D 5 35
D 5 - agonist radioligand 34
D 5 - antagonist radioligand 34
DAPK1 132
DAPK2 132
data and reports 9
Data Online 9
Data Online account 211
data turnaround 205
DCAMKL1 132
DCAMKL2 132
DDR2 kinase 109
deliverables 205
delta 2 (DOP) 59
delta 2 (DOP)- agonist radioligand 59
dipeptidyl peptidase IV (DPP-IV) 167
DLK1 (MAP3K12) 149
DNA polymerase b 158
DNA polymerase I 157
DNA repair & mitotic enzymes 157
Dopamine 32,104
dopamine release (activator effect) 185
dopamine transporter - antago. radioligand 104
dopamine uptake 104
DP 1 63
DP 1 - agonist radioligand 63
DRAK1 132
drug development 199
drug discovery 4
drug-drug interaction 199,200
drug profile interpretation 7
DYRK1a 126
DYRK2 126
DYRK3 126
DYRK4 126
[E]
ECE-1 171,172
Eg5 158
EGF - agonist radioligand 87
EGFR kinase 109
EGFR kinase (A431 cells) - AlphaScreen 109
EGFR kinase (A431 cells) - impedance 109
EGFR kinase (Hela cells) 109
EGFR kinase (MDA-MB-231 cells) 109
EGF-stimulated A-431 proliferation 192
elastase 168
Endothelin 35
enzyme assays (testing conditions) 204,209
EP 1 64
EP 1 - agonist radioligand 64
EP 2 64
EP 2 - agonist radioligand 64
EP 3 64
EP 3 - agonist radioligand 64
EP 4 65
EP 4 - agonist radioligand 65
EphA1 kinase 110
EphA2 kinase 110
EphA3 kinase 110
EphA4 kinase 110
EphA5 kinase 110
assay list & index ❚
EphA6 kinase 110
EphA7 kinase 111
EphA8 kinase 111
EphB1 kinase 111
EphB2 kinase 111
EphB3 kinase 111
EphB4 kinase 111
Epigenetic & DNA-related enzymes 157
ERa - agonist fluoligand 79
ERb - agonist fluoligand 79
ERK 1 127
ERK 1/2 127
ERK 2 (P42 mapk ) 127
ERK 5 (MAPK7) 127
ER (non-selective)- agonist radioligand 79
ET A 35
ET A - agonist radioligand 35
ET B 36
ET B - agonist radioligand 35
ExpresScreen option 211
Expression of endothelial adhesion proteins:
- ELAM-1 191
- ICAM1/VCAM-1 190
- VCAM-1 191
[F]
FAAH (fatty acid amide hydrolase) 183
FAK 119
Fer kinase 119
Fes kinase 120
FFA1(GPR40) 37
FFA2 (GPR43) 37
FFA3 (GPR41) 37
FGFR kinase 112
FGFR1 kinase 112
FGFR2 kinase 112
FGFR3 kinase 112
FGFR4 kinase 112
Fgr kinase 120
FLT-1 kinase (VEGFR1) 112
FLT-3 kinase 113
FLT-3 D835Y kinase 113
FLT-4 kinase (VEGFR3) 113
fMLP 36
fMLP - agonist radioligand 36
Fms/CSFR kinase 113
form & format (compound) 211
formula weight (FW) 208
n-formyl peptide 36
FP 65
FP - agonist radioligand 65
Free fatty acid 37
Free radical secretion 190
FRK 120
frozen samples (compound) 211
functional nuclear receptor assays 80
Fyn kinase 120
[G]
GABA 38,84,97,104
GABA A 85,98
GABA A1 (a1,b2,g2)- agonist radioligand 85,97
GABA A (automated patch-clamp) 85,97
GABA A (automated patch-clamp,functional
screening) 85,97
GABA A (conventional patch-clamp) 85,98
GABA B 38
GABA B ( 1b )- antagonist radioligand 38
GABA (non-selective)- agonist radioligand 84
GABA transaminase 179
GABA transporter - antagonist radioligand 104
GAL 1 - agonist radioligand 38
GAL 2 39
GAL 2 - agonist radioligand 39
Galanin 38
Cerep
services
Receptors
Ion
channels
Transporters
Kinases
Epigenetic &
DNA-related
enzymes
Other
enzymes
Specialized
cellular
assays
Standard
profiles
Testing
conditions
Ordering
information
Assay list
& index

216 in vitro pharmacology 2011 catalog lipid peroxydation 190
❚ assay list & index
galanin (non-selective)- agonist radioligand 38
GCK (MAP4K2) 145
GHRH 41
GLP-1 39
GLP-1 - agonist radioligand 39
GLP-2 39
glucagon 40
Glucagon 39
glucagon - agonist radioligand 40
Glutamate 86,98
Glycine 87,99
glycine (strychnine-insensitive)- antagonist
radioligand 87,99
Glycoprotein hormone 40
GnRH (LH-RH)- agonist radioligand 40
Gonadotrophin-releasing hormone 40
GPCRs 13
GPCRs (tool-box) 6
GPR119 62
G protein-coupled receptors 13
GR - agonist radioligand 80
GRK2 (ADRBK1) 138
GRK3/BARK2 (ADRBK2) 138
GRK5 138
Growth factors 87
Growth hormone-releasing hormone 41
GSK3a 127
GSK3b 127,128
guanylyl cyclase (activator effect) 181
guanylyl cyclase (inhibitor effect) 181
[H]
H 1 41
H 1 - antagonist radioligand 41
H 2 42
H 2 - antagonist radioligand 42
H 2 - inverse agonist effect 42
H 2 O 2 scavenging 190
H 2 O 2 secretion 190
H 3 43
H 3 - agonist radioligand 42,43
H 4 43
H 4 - agonist radioligand 43
HCK 120
HDAC1 158
HDAC2 158
HDAC3 159
HDAC4 159
HDAC5 159
HDAC6 159
HDAC7 159
HDAC8 159
HDAC9 160
HDAC10 160
HDAC11 160
HDACs 158
HER2/ErbB2 kinase 113
HER4/ErbB4 kinase 113
hERG (automated patch-clamp) 94
hERG (conventional patch-clamp) 94
hERG (membrane preparation) - antagonist
radioligand 94
HGK (MAP4K4) 145
high throughput screening 4
HIPK2 128
HIPK3 128
HIPK4 128
Histamine 41
histamine release (activator effect) 185
histamine release (inhibitor effect) 185
HIV-1 protease 171
HMG-CoA reductase 183
HNE (human neutrophil elastase) 168
HNMT (histamine N-methyl transferase) 179
HTRF ® 107
[I]
I 1 - agonist radioligand 88
I 2 - antagonist radioligand 88
IC 50 /EC 50 follow-up studies 204,205,209
IFN-g secretion (inhibitor effect) 188
IGF1Rb kinase 114
IGF1R kinase 114
IKKa 152
IKKb 152
IKKe (IKBKE) 152
IL-1b - agonist radioligand 84
IL-1β secretion (inhibitor effect) 188
IL-2 - agonist radioligand 84
IL-2 secretion (inhibitor effect) 189
IL-4 - agonist radioligand 84
IL-4 secretion (inhibitor effect) 189
IL-5 secretion (inhibitor effect) 189
IL-6 - agonist radioligand 84
IL-6 secretion (inhibitor effect) 189
IL-8 secretion (inhibitor effect) 188
IL-10 secretion (inhibitor effect) 189
Imidazoline 88
inducible NOS 176,177
Inositol phosphate 181
Insulin 88
insulin - agonist radioligand 88
Intracellular ligand-gated channels 102
in vitro ADME profiling 4
in vitro pharmacology assays 11
in vitro safety profiling 4
in vivo PK 4
ion channel patch-clamp assays 95
Ion channels 93
Ion transport systems 186
IP 3 - agonist radioligand 102,181
IP (PGI 2 ) 65
IP (PGI 2 )- agonist radioligand 65
IRAK1 149
IRAK4 150
IRK (InsR) 114
IRK (InsRb) 114
IRR kinase 114
ITK 120
[J]
JAK1 121
JAK2 121
JAK3 121
JNK1 128
JNK1/3 129
JNK2 128
JNK3 129
[K]
K + channels 94
kainate - agonist radioligand 86,99
kallikrein 168
kappa (KOP) 60
kappa (KOP)- agonist radioligand 59
K ATP 95
K ATP - antagonist radioligand 94
KDR kinase (VEGFR2) 115
Kinases 107
K V - antagonist radioligand 95
[L]
LANCEUltra ® 107
Lck kinase 121
lead optimization (or SAR) profiling 4
Leukotrienes 44
LIMK1 150
Locations (Cerep sites)
back cover
LPA 1 - agonist radioligand 45
LPA 2 45
LPA 3 45
LRRK2 150
LTB 4 secretion (inhibitor effect) 187
LTC 4 secretion (inhibitor effect) 187
LTK 115
LXRb - agonist radioligand 81
Lyn A kinase 121
Lyn B kinase 121
Lysophosphatidic acid 45
Lysophospholipid 45
[M]
M 1 50
M 1 - antagonist radioligand 50
M 2 51
M 2 - agonist radioligand 51
M 2 - antagonist radioligand 51
M 2 - inverse agonist effect 51
M 3 52
M 3 - antagonist radioligand 51
M 4 52
M 4 - agonist radioligand 52
M 4 - antagonist radioligand 52
M 4 - inverse agonist effect 52
M 5 53
M 5 - agonist radioligand 53
M 5 - antagonist radioligand 53
MAO-A 179
MAO-A - antagonist radioligand 180
MAO-B 180
MAO-B - antagonist radioligand 180
MAPKAPK2 133
MAPKAPK5 (PRAK) 133
MARK1 133
MARK2 133
MARK3 133
MARK4 133
master service agreement 208
MC 1 47
MC 1 - agonist radioligand 47
MC 2 47
MC 3 48
MC 3 - agonist radioligand 47
MC 4 48
MC 4 - agonist radioligand 48
MC 4 - inverse agonist effect 48
MC 5 48
MCH 1 46
MCH 1 - agonist radioligand 46
MCH 2 47
MCH 2 - agonist radioligand 46
MEK1 145
MEK1 (MAP2K1) 145
MEK5 (MAP2K5) 145
MEKK3 (MAP3K3) 146
MEKK4 (MAP3K4) 146
Melanin concentrating hormone 46
Melanocortin 47
Melatonin 49,89
MELK 134
Membrane ligand-gated channels 97
Mer kinase 115
Metalloproteases 171
MINK 146
Miscellaneous enzymes 182
MKK4/JNK1 146
MKK4/JNK2 146
MKK6 146
MKK6/p38a (mutant active) 147
MLK1 150
MLK2 (MAP3K10) 150
MMP-1 172
MMP-2 172

217
MMP-3 172
MMP-7 172
MMP-8 172
MMP-9 173
MMP-12 173
MMP-13 173
MNK1 134
MNK2 134
M (non-selective)- antagonist radioligand 50
molecular weight (MW) 208,209,210
Monoamine & neurotransmitter synthesis
& metabolism 179
Monomamine & neurotransmitter release 185
MOS kinase 152
Motilin 49
motilin - agonist radioligand 49
motilin 50
MRCKa 138
MSK1 139
MSK2 139
MST1 kinase (STK4) 147
MST2 kinase 147
MST3 kinase 147
MST4 kinase 147
MT 1 (ML 1A ) 49
MT 1 (ML 1A )- agonist radioligand 49
MT1-MMP (MMP-14) 173
MT 2 (ML 1B ) 49
MT 2 (ML 1B )- agonist radioligand 49
MT 3 (ML 2 )- agonist radioligand 89
mTOR kinase (FRAP1) 156
mu (MOP) 60
mu (MOP)- agonist radioligand 60
mu (MOP)- antagonist radioligand 60
Muscarinic 50
MusK 115
myeloperoxidase 183
MYT1 kinase 153
[N]
Na + 96
Na + /Ca 2+ antiport 186
Na + channels 96
Na + /H + antiport 187
Na + /K + - ATPase pump 186
Na + /K + /Cl – cotransport 187
Na + - site 2 - antagonist radioligand 96
Na V 1.5 (automated patch-clamp) 96
Na V 1.5 (conventional patch-clamp) 96
NDR1 kinase 139
NEK1 153
NEK2 153
NEK4 153
NEK6 153
NEK7 153
Neurokinin 53
Neuromedin U 55
Neuropeptide S 56
Neuropeptide W/neuropeptide B 56
Neuropeptide Y 56
Neurotensin 58
neutral endopeptidase 173
N-formyl peptide 36
Nicotinic 89,100
NIK 147
NIM1 kinase (MGC42105) 134
NK 1 53,54
NK 1 - agonist radioligand 53
NK 2 54
NK 2 - agonist radioligand 54
NK 3 55
NK 3 - agonist radioligand 55
NK 3 - antagonist radioligand 54
NMDA - antagonist radioligand 86,99
NMU1 55
NMU2 - agonist radioligand 56
N muscle-type - antagonist radioligand 90,100
N neuronal (a4b2)- agonist radioligand 89,100
N neuronal (a7) - antagonist radioligand
89,90,100
non-recombinant models (tool-box) 5
Non-steroid nuclear receptors 80
NOP (ORL1) 61
NOP (ORL1)- agonist radioligand 61
Norepinephrine 104
norepinephrine release (activator effect) 185
norepinephrine transporter - antagonist
radioligand 104
norepinephrine uptake 105
NO synthases 176
NPBW1 56
NPS 56
NT (non-selective) 58
NT (non-selective)- agonist radioligand 58
NTS 1 (NT 1 ) 58
NTS 1 (NT 1 )- agonist radioligand 58
NTS 2 58
NuaK1 (ARK5) 134
nuclear receptors 79
[O]
Opioid and opioid-like 59
opioid (non-selective)- antagonist radioligand 59
Ordering information 208
Orexin 61
Orphans (Class A) 62
OT 77
Other enzymes 163
Other kinases 151
Other receptors 83
OX 1 61
OX 1 - agonist radioligand 61
OX 2 62
OX 2 - agonist radioligand 62
[P]
P2X 90,101
P2X - agonist radioligand 90,101
P2Y - agonist radioligand 67
P2Y 1 67
P2Y 2 67
P2Y 4 67
P2Y 6 68
P2 Y - agonist radioligand 67
p38a kinase 129
p38b2 kinase (SAPK2b2) 129
p38g kinase 129
p38d kinase 130
p38 MAPK 129
p70S6K 139
p70S6Kb 139
PAC 1 (PACAP) 76
PAC 1 (PACAP)- agonist radioligand 75
PAF 63
PAF - agonist radioligand 62
PAK1 148
PAK2 148
PAK4 148
PAR1 66
PAR1 - agonist radioligand 66
PAR2 67
PAR2 - agonist radioligand 66
Parathyroid hormone 62
PASK 134
PCP - antagonist radioligand 86,99
PCTAIRE1 kinase 130
PDE1B 174
PDE2A 174
PDE3A 174
PDE3B 174
PDE4A 1A 175
PDE4B 1 175
assay list & index ❚
PDE4D 2 175
PDE5 (non-selective) 175
PDE6 (non-selective) 175
PDE7A 175
PDE8A 176
PDE10A 1 176
PDE11A 4 176
PDGF - agonist radioligand 87
PDGFR kinase 115
PDGFRa kinase 115
PDGFRb kinase 116
PDGF-stimulated A7r5 migration 192
PDGF-stimulated A7r5 proliferation 192
PDGF-stimulated AoSMC migration 192
PDGF-stimulated Balb/c 3T3 proliferation 193
PDK1 139
PEK (EIF2AK3) 154
PGE 2 secretion (inhibitor effect) 187
PGI 2 secretion 188
PHA-stimulated PBMC proliferation 193
PhKg1 135
PhKg2 135
phosphatase 1B (PTP1B) 163
phosphatase 2A (PP2A) 163
phosphatase 2B 164
phosphatase CD45 164
phosphatase CDC25A 164
phosphatase CDC25B 164
phosphatase CDC25C 164
phosphatase DEP1 (PTPRJ) 164
phosphatase LAR (PTPRF) 165
phosphatase MEG1 (PTPN4) 165
phosphatase MEG2 (PTPN9) 165
phosphatase MKP1 165
phosphatase MKP2 165
phosphatase MKP3 165
phosphatase MKP6 166
phosphatase PEST (PTPN12) 166
phosphatase PP1a 163
phosphatase PTPb (PTPRB) 166
phosphatase PTPg (PTPRG) 166
phosphatase PTPµ (PTPRM) 166
Phosphatases 163
phosphatase SHP1 (PTPN6) 166
phosphatase SHP2 (PTPN11) 167
phosphatase TC-PTP (PTPN2) 167
phosphatase VHR (DUSP3) 167
Phosphodiesterases 174
Phospholipase C 182
Pim1 kinase 135
Pim2 kinase 135
(in vivo) PK 4
PK 1 63
PK 2 63
PKA 140
PKCa 140
PKCb1 140
PKCb2 140
PKCg 140
PKCd 140
PKCe 141
PKCz 141
PKCh 141
PKCq 141
PKCi 141
PKD1 (PKCµ) 135
PKD2 135
PKD3 136
PKG1a 141
PKG1b 142
PKG2 142
PKN1 142
PKN2 142
PKR (EIF2AK2) 154
PLA 2 (See sPLA 2)
Platelet activating factor 62
PLC 182
PLK1 154
PLK2 154
Cerep
services
Receptors
Ion
channels
Transporters
Kinases
Epigenetic &
DNA-related
enzymes
Other
enzymes
Specialized
cellular
assays
Standard
profiles
Testing
conditions
Ordering
information
Assay list
& index

218 in vitro pharmacology 2011 catalog Trpv1 (vr1) 97
❚ assaY lisT & index
plK3 154
plK4 154
pnMT (phenylethanolamine n-methyltransferase)
180
ppara 81
ppara - agonist radioligand 81
pparg 81
pparg - agonist radioligand 81
ppard 81
pr 80
pr - agonist radioligand 80
prKx 142
Profile design 7
Profiling/screening services 4
Prokineticin 63
proliferation 192
Prostanoid 63
Proteases 167
Proteinase-activated 66
Protein-serine/threonine kinases 124
Protein-tyrosine kinases 108
protocol(s) 204,205
pTh1 62
Purinergic 67,90,101
pxr - agonist radioligand 82
pYK2 122
[Q]
quotation 208
[R]
radioligand binding assays 204
raf-1 kinase 150
raf-1/MeK1 151
rara - agonist radioligand 82
RECEPTORS 13,79,83
Relaxin 68
requested compound information 208
results reporting 211
ret kinase 116
ripK2 151
rocK1 142
rocK2 143
rolipram - antagonist radioligand 176
ron kinase 116
ros kinase 116
rsK1 143
rsK2 143
rsK3 143
RTK (protein-tyrosine kinases) 108
rxfp1 68
rxfp1 - agonist radioligand 68
rY3 (ryanodine)- antagonist radioligand 102
[S]
safety profiling ( in vitro) 4
s 1 p 1 45
s 1 p 2 46
s 1 p 3 46
sample size(s) 209
screening (high-thtoughput) 4
secretin 40
secretion 187,188,190
Serine proteases 167
Serotonin 68,90,101,105
serum-stimulated a7r5 proliferation 192
service agreement 208
sgK1 143
sgK2 144
sgK3 144
shipment instructions 210
Sigma 91
sigma 1 - agonist radioligand 91
sigma 2 - agonist radioligand 91
sigma (non-selective) 91
sigma (non-selective)- agonist radioligand 91
siK 136
sirtuin 1 (activator effect) 160
sirtuin 1(inhibitor effect) 160
sirtuin 2 160
sirtuin 3 161
Sites (Cerep sites)
back cover
sK ca - antagonist radioligand 95
smMlcK (MYlK) 136
solvent 208
Somatostatin 73
SPECIALIZED CELLULAR ASSAYS 185
Sphingosine 1-phosphate 45,46
spla 2 (bee venom type iii) 178
spla 2 (Type v) 178
src kinase 122
srm kinase 122
sst 1 73
sst 1 - agonist radioligand 73
sst 2 - agonist radioligand 74
sst 4 74
sst 4 - agonist radioligand 74
sst 5 74
sst 5 - agonist radioligand 74
sst (non-selective)- agonist radioligand 73
STANDARD PROFILES 195
standard profiles (sample sizes) 210
standard solubilization process 209
STE (protein-serine/threonine kinases) 144
Steroid nuclear receptors 79
sTK33 136
strychnine-sensitive - antagonist radioligand 87,99
study initiation 208,211
suggested testing:
- binding,enzyme & cellular assays 204
- tissue assays 205
–
superoxide o 2 secretion 190
syk 122
[T]
Tace 173
TaK1-Tab1 (Map3K7) 151
TaoK2 (Tao1) 148
target profile design 8
TbK1 155
Tec kinase 122
TESTING CONDITIONS 203
Tgf-b - agonist radioligand 87
Thyrotropin releasing hormone 75
Tie2 kinase 116
tissue assays 43,205
TKL (protein-serine/threonine kinases) 149
Tnf-a - agonist radioligand 83
Tnf-a secretion (inhibitor effect) 189
Tnk1 122
topoisomerase ii 158
Tp (Tx a2 /pgh 2 ) 66
Tp (Tx a2 /pgh 2 )- antagonist radioligand 66
Transduction signal enzymes 181
Transient receptor potential channels 96
TRANSPORTERS 103
Trh 1 75
Trh 1 - agonist radioligand 75
TrKa 116
TrKb 117
TrKc 117
TrpM8 96
Trpv3 97
Tr (Th)- agonist radioligand 82
tryptase 168
Tsh 40
TssK1 136
TssK2 (sTK22b) 136
TTK 155
tubulin 183
turnaround time 211
Tx a2 synthetase 178
Txb 2 secretion (inhibitor effect) 188
TxK 123
Tyk2 (JTK1) 123
Tyro3/sky kinase 117
tyrosine hydroxylase 180
[U]
UlK1 155
UlK2 155
Urotensin-II 75
UT 75
UT - agonist radioligand 75
[V]
v 1a 77
v 1a - agonist radioligand 77
v 1b - agonist radioligand 78
v 2 78
v 2 - agonist radioligand 78
Vasoactive intestinal peptide 75
Vasopressin 77
vdr - agonist radioligand 82
vegf - agonist radioligand 88
vegfr kinase 117
vegf-stimulated hUv-ec-c proliferation 193
Voltage-gated channels 93
vpac 1 (vip 1 ) 76
vpac 1 (vip 1 )- agonist radioligand 76
vpac 2 (vip 2 ) 76
vpac 2 (vip 2 )- agonist radioligand 76
[W]
Wee1 kinase 155
WnK2 155
WnK3 156
WnK4 156
[X]
xanthine oxidase/superoxide o 2
–
scavenging
183
[Y]
Y 1 57
Y 1 - agonist radioligand 56
Y 2 57
Y 2 - agonist radioligand 57
Y 3 57
Yes kinase 123
Y (non-selective)- agonist radioligand 56
[Z]
Zap70 kinase 123
© cerep - art by françoise rio - conception design & execution: cerep/catherine Moreau
printed in france (december 2010) by imprimerie chirat on fsc/pefc certified paper

contacts
❚ france
[Laboratories]
Le Bois l’Evêque
86600 CELLE L’EVESCAULT
tel. +33 (0)5 49 89 30 00
sales@cerep.com
❚ usa
[Laboratories]
15318 N.E. 95th Street
Redmond, WA 98052
tel. +1 (425) 895 8666
sales@cerep.com
❚ japan
[Sales Office]
Namiki Shoji Co., Ltd.
Kenseishinjuku Bldg. 5-5-3
Shinjuku, Shinjuku-ku
TOKYO, 160-0022
tel. +81 (0)3 3354 4026
ishimoto@namiki-s.co.jp
❚ china
[Laboratories]
上 海 张 江 高 科 技 区 爱 迪 生 路 326 号 302-1 室
(326 Aidisheng Road, B 302-1)
Zhangjiang High-Tech Park
Shanghai 201203
tel. +86 21 5132 0568
sales@cerep-ltd.com
❚ www.cerep.com
•
•
• •

france
Laboratories
Le Bois l’Evêque
86600 CELLE L’EVESCAULT
tel. +33 (0)5 49 89 30 00
sales @ cerep.com
usa
Laboratories
15318 N.E. 95th Street
Redmond, WA 98052
tel. +1 (425) 895 8666
sales @ cerep.com
japan
Sales Office
Namiki Shoji Co., Ltd.
Kenseishinjuku Bldg. 5-5-3
Shinjuku, Shinjuku-ku
TOKYO, 160-0022
tel. +81 (0)3 3354 4026
ishimoto @ namiki-s.co.jp
china
Laboratories
上 海 张 江 高 科 技 区 爱 迪 生 路 326 号 302-1 室
(326 Aidisheng Road, B 302-1)
Zhangjiang High-Tech Park
Shanghai 201203
tel. +86 21 5132 0568
sales @ cerep-ltd.com
www.cerep.com