2. Academic Validation
  3. Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120)

Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120)

  • Bioorg Med Chem Lett. 2014 Jul 15;24(14):3100-3. doi: 10.1016/j.bmcl.2014.05.012.
Steven M Sparks 1,  Grace Chen 2,  Jon L Collins 3,  Dana Danger 3,  Steven T Dock 3,  Channa Jayawickreme 2,  Stephen Jenkinson 4,  Christopher Laudeman 4,  M Anthony Leesnitzer 2,  Xi Liang 3,  Patrick Maloney 4,  David C McCoy 4,  David Moncol 2,  Vincent Rash 2,  Thomas Rimele 2,  Padmaja Vulimiri 2,  James M Way 3,  Sean Ross 3
Affiliations

Affiliations

  • 1 Enteroendocrine Discovery Performance Unit, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, United States. Electronic address: steven.m.sparks@gsk.com.
  • 2 Platform Technology & Science, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, United States.
  • 3 Enteroendocrine Discovery Performance Unit, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, United States.
  • 4 Metabolic Center for Excellence in Drug Discovery, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, United States.
PMID: 24881566 DOI: 10.1016/j.bmcl.2014.05.012
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.

Keywords

FFA4; Free fatty acid receptor 4; Free fatty acid receptor 4 agonist; Free fatty acid receptor 4 antagonist; GPR120.

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