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6 ADME-Tox & PK 2011 catalog❚ assay design & development❚ tool-box for biochemical assaysIn addition to cellular assays, Cerep offers multiple biochemical assays to accurately study the interaction of compoundswith the target of interest. These assays can be developed on recombinant material or native tissues.Targets Binding assays Functional assaysGPCRs Radioligand binding GTPgSIon channels Radioligand binding –Kinases TR-FRET TR-FRETOther enzymes Radioligand binding Multiple technologiesGrowth factor receptors Radioligand binding –Cytokine receptors Radioligand binding –Nuclear receptors Radioligand binding AlphaScreenTransporters 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 gpcrsDepending on the type of target, study and model, Cerep can recommend the most adapted technology.Studies Targets Gi Gq Gs G12/13AffinityKon/KoffAgonistAntagonistAllosteric (PAM & NAM)Inverse agonistWeak agonistSlow agonistRLB 1RLB 1RLB 1RLB 1SPA 2 SPA 2 SPA 2 SPA 2GTPgSTR-FRET cAMPCDS 3Aequorin 4GTPgSTR-FRET cAMPCDS 3GTPgSTR-FRET cAMPCDS 3TR-FRET IP1FluorescenceCDS 3Aequorin 4TR-FRET IP1CDS 3TR-FRET IP1CDS 3TR-FRET cAMPCDS 3Aequorin 4ELISACDS 3Aequorin 4TR-FRET cAMPCDS 3 CDS 3TR-FRET cAMPCDS 3 CDS 3Deorphanization CDS 3CDS 3CDS 3CDS 3Aequorin 4 Aequorin 4 Aequorin 4 Aequorin 4Coupling mechanism CDS 3 CDS 3 CDS 3 CDS 3Kinase phosphorylation AlphaScreen AlphaScreen AlphaScreen AlphaScreen1RLB: RadioLigand Binding2SPA: Scintillation Proximity Assay3CDS: Cellular Dielectric Spectroscopy4Expression of chimeric or promiscuous G proteins may be required.
7❚ profile designCerep offers a profile design service based on the experience and knowhow of its scientists for both content and executionof profiles. Cerep BioPrint ® database (see below), various publicly available databases, and the scientific literature areused to design different types of profiles according to your needs.❚ tool-box for profile designType Content ApplicationsDisease profileSide effect profilePredictive profileTargets that areassociated to aparticular diseaseTargets that areassociated to aparticular side effectTargets that aresusceptible to behit by a givencompound- 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 optimizationCerepservicesassayselectionguide❚ bioprint ® profile & servicesBioPrint ® is a large, homogenous pharmacology and ADMEdatabase, which provides a unique resource for supportingdecision making in drug discovery. The database is composedof three main data sets: chemical descriptors (structures and chemical information,2D and 3D descriptors), in-house generated in vitro pharmacology and ADMEdata, also considered as compound descriptors, collected and curated in vivo effects of drugs.Chemical and pharmacophoric descriptors together forma data set for QSAR generation supporting organ safetymodeling.BioPrint ® positions a new drug candidate in the context ofmarketed 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 geneticallyparented to a test target (target profile design). Both theseapplications are available as custom services.2,450 compoundschemicalproperties2D structuresand 3D descriptorsin vitro dataconsistentin vitropharmacology& ADME profileson 159 assaysQSARclinicalobservationsorgan safetyside effectsPKtherapeutic effectsin vitroADMEin vitrotoxicityin vivo PK/Bioanalytical❚ BIOPRINT ® PROFILEThe BioPrint ® profile includes the assays used to explore the properties of about 2,450 BioPrint ® compounds (mainlymarketed 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 and5 phosphodiesterases), as well as 20 ADME-Tox assays (Solubility, Absorption, Metabolism and CYP-mediated drug-druginteraction). More than 70% are human targets. The 159 assays of this profile represent a rationalized panel from a largerassay 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 INTERPRETATIONAny compound in drug development, when run as a test compound on the BioPrint ® profile, can be placed in the contextof already marketed drugs, when similar in vitro profiles exist in the database. Hypotheses on clinical behavior of the testcompounds can be drawn by comparison with data on BioPrint ® compounds that have been collected and analyzedstandardprofilesorderinginformationassay list& index
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