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Updated: Apr 27, 2026

Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay
Published on: July 28, 2014
Identifying orphan G protein coupled receptors in drug discovery
John Dunlop1, Richard M Eglen2
1Neuroscience Discovery Research, Wyeth Research, CN-8000, Princeton, NJ 08543, USA.
Abstract:
G-protein coupled receptors (GPCRs) represent the most tractable family of drug targets. Those GPCRs identified by sequence only, but lacking an endogenous ligand, are defined as orphan GPCRs (oGPCRs) and might represent the next generation of targets for GPCR drug discovery. Drug discovery at oGPCRs is a resource intensive approach and frequently taken 'at-risk' without a clear understanding of the role in a disease. Identification of oGPCRs is, therefore, a prerequisite for the initiation of a drug discovery program.:
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