in vitro PHARMACOLOGY 2011 CATALOG - Cerep

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