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.
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 email@example.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
Inverse agonist assays are available on a selected number of targets and can be developed upon request