Lead Discovery GPCRs


Merck:/Freestyle/BI-Bioscience/Drug-Discovery/Drug-Discovery-Images/LD_GPCRome_Poster.jpg Easily explore the human GPCRome
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GPCRs in Drug Discovery and Safety Pharmacology
G protein coupled receptors (GPCRs) have been and will continue to be prominent drug targets for treating hypertension, pain, asthma, neurological and other disorders. There are ~385 druggable GPCRs, which can share similar binding pockets. Because one drug may interact with more than one receptor, profiling a drug candidate’s GPCR activity can reveal off-target effects, which can be either good or bad for drug safety and efficacy.

Why Profile GPCRs with Functional Assays vs. Binding Assays?
Unlike ligand-binding assays, high-quality, cell-based, functional assays, such as those developed and validated by Merck, can truly elucidate the effect of a compound on GPCR signaling.

  • Functional data can reveal potential safety liability at an off-target hit
  • Functional assays and binding assays are equally sensitive assays for antagonists
  • Functional assays are more sensitive for detecting agonists and off-target interactions
  • Limited radioligands and quality membrane preps means fewer targets can be profiled by binding assays