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Updated: Apr 28, 2026

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120)
Steven M Sparks1, Grace Chen2, Jon L Collins1
1Enteroendocrine Discovery Performance Unit, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, United States.
Abstract:
The exploration of a diarylsulfonamide series of free fatty acid receptor 4 (FFA4/GPR120) agonists is described. This work led to the identification of selective FFA4 agonist 8 (GSK137647A) and selective FFA4 antagonist 39. The in vitro profile of compounds 8 and 39 is presented herein.
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