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Updated: Feb 8, 2026

Quantifying Agonist Activity at G Protein-coupled Receptors
Published on: December 26, 2011
Discovery of novel selective GPR120 agonists with potent anti-diabetic activity by hybrid design
Ren Sheng1, Liu Yang2, Yanchun Zhang1
1Jiangsu Key Laboratory of Drug Discovery for Metabolic Disease and State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tongjia Xiang, Nanjing 210009, China.
Abstract:
GPR120 is an attractive target for the treatment of type 2 diabetes. In this study, a series of biphenyl derivatives were designed, synthesized by hybrid design. The selected compound 6a exhibited potent GPR120 agonist activity (EC50 = 93 nM) and high selectivity over GPR40. The results of oral glucose tolerance test (OGTT) demonstrated that 6a exhibited significant glucose-lowering effect in glucose-loaded ICR male mice. Analysis of the structure-activity relationship is also presented. Compound 6a deserves further biological evaluation and structural modifications.
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