In vitro activity: GSK137647A, a diarylsulfonamide analog, is a novel, potent and selective agonists of the free fatty acid receptor 4 (FFA4/GPR120) with pEC50 of 6.3, 6.2, and 6.1 for human, mouse and rat FFA4, respectively. GSK137647A is selective for GPR120 over a panel of 61 other targets, including other FFARs. The free fatty acid receptor 4 (FFA4/GPR120) is a member of the G protein-coupled receptor family and is a potential 7TM (transmembrane) receptor that is involved in long-chain fatty acid-stimulated glucagon-like peptide-1 (GLP-1) secretion. FFA4 is highly expressed in the intestinal endocrine cell line STC-1 and the intestine.

Kinase Assay: GSK137647A is a selective FFA4 agonist, with pEC50 of 6.3, 6.2, and 6.1 for human, Mouse and Rat FFA4, respectively. The pEC50s for Human , Mouse and Rat FFA1/2/3 are ＜ 4.5. GSK137647A is evaluated against a panel of 65 targets in both full curve functional and binding assays and was shown to provide at least 100-fold selectivity against the panel which included 41 G-protein-coupled receptors (GPCRs), including additional members of the free fatty acid receptors (FFA1, FFA2, and FFA3). GSK137647A produces a concentration-dependent increase in glucose stimulated insulin secretion under high glucose conditions (25 mM).