2. Academic Validation
  3. Discovery of the imidazole-derived GPR40 agonist AM-3189

Discovery of the imidazole-derived GPR40 agonist AM-3189

  • Bioorg Med Chem Lett. 2016 Jan 1;26(1):15-20. doi: 10.1016/j.bmcl.2015.11.050.
Zhihua Ma 1,  Daniel C-H Lin 2,  Rajiv Sharma 1,  Jinqian Liu 1,  Liusheng Zhu 1,  An-Rong Li 1,  Todd Kohn 1,  Yingcai Wang 1,  Jiwen Jim Liu 1,  Michael D Bartberger 1,  Julio C Medina 1,  Run Zhuang 2,  Frank Li 2,  Jane Zhang 2,  Jian Luo 2,  Simon Wong 3,  George R Tonn 3,  Jonathan B Houze 1
Affiliations

Affiliations

  • 1 Department of Therapeutic Discovery, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.
  • 2 Department of Metabolic Disorders, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.
  • 3 Department of Pharmacokinetics & Drug Metabolism, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.
PMID: 26620255 DOI: 10.1016/j.bmcl.2015.11.050
Abstract

As a follow-up to the GPR40 agonist AMG 837, which was evaluated in clinical trials for the treatment of type II diabetes, further optimization led to the discovery of AM-3189 (13k). AM-3189 is representative of a new class of compounds with minimal CNS penetration, superior pharmacokinetic properties and in vivo efficacy comparable to AMG 837.

Keywords

AM-3189; AMG 837; Agonist; FFAR1; GPCR; GPR40; Insulin secretagogue; Type II diabetes.

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