Functional GPCR Assays for Screening and Profiling in Drug Discovery

When assessing potential efficacy and liabilities of a G-protein-coupled receptor (GPCR) therapeutic, it is important to understand its on- and off-target activity. GPCRs can signal through a variety of cascades and a drug will activate, inhibit, or modulate one or more of these. Indeed, compound activity can be complex as certain compounds may elicit different activity on different signaling cascades, also known as ligand-biased signaling.
 
Eurofins Discovery offers functional GPCR services covering several second messenger pathways to better understand compound activity. Combined with GPCR binding assays, these functional GPCR assays can provide an orthogonal approach to confirm the in vitro pharmacology profile of your lead compounds.
 
Eurofins’ functional GPCR functional cell-based assays feature multiple second messenger readouts, including cAMP for Gi and Gs-coupled receptors and IP1 and IP3/calcium flux for Gq-coupled receptors, emphasizing the natural pathway of the receptor. Additionally, assays to look at endogenous receptor signaling as well as traditional GTPγS assays are also available to further develop your compounds of interest.