1. Academic Validation
  2. 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.
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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