If you have a panel of lead candidates and need to concentrate on optimizing just some of them, Cerep can help you make the right decision.
Profiled against a diverse panel of assays, Cerep’s functional profiling platform can be used to identify pathways underlying drug efficacy, safety, and toxicity; and to affect attrition of novel compounds with undesirable or toxic properties.
The profiling platform can also be used to identify new uses of therapeutic agents, to screen libraries of chemical compounds, to perform lead optimization, and to perform studies of structure-activity relationships in the context of intact cells.
The profiling platform can be applied to any test compound, drug lead, known drug or toxicant, and therapeutic indication.

Platform features
 We study the natural pathway of the receptor to increase the physiological relevance:
       no promiscuous or chimeric G proteins
       a novel patented¹ host cell line to measure cAMP production for Gi-coupled receptors
       cAMP measurement for Gi and Gs, calcium flux for Gq-coupled receptors.
 The assays are developed using the same cell lines as those used in our binding platform to allow a better comparison.
 The assays are developed using cells and membranes produced and quality controlled in-house, resulting in high reproducibility of our results.
 Two technologies were selected for use in the functional GPCR platform: HTRF® to determine cAMP concentration and real time fluorescence to monitor calcium concentration. Our platform is adapted to monitor Gs, Gi and Gq-coupled receptors using homogenous conditions resulting in high throughput profiling.
 The functional GPCR platform uses Cerep’s growing list of GPCR targets and robust cell-based assays (agonist and antagonist measures).

Relation between binding & functional assays
We can provide advice on concentrations to be used in our functional GPCR platform when binding affinity is known; this is especially important as experimental functional inhibitions can be shifted to the right when compared to binding inhibitions in most targets.
Please contact us at sales@cerep.com for details.

Advantages of Cerep’s functional GPCR platform
 Identification of off-target activities early in the drug discovery
 No promiscuous G protein
 Novel patented host cell line¹ for Gi protein coupled receptors
 Allows binding and functional comparison because the same biological material is used
 Agonist and antagonist assays are available for all targets
 No down time: independent from providers for biological material
 Testing conditions can be advised when binding affinity is known
 High throughput
 Inverse agonist assays are available on a selected number of targets and can be developed upon request