Figure 5.

GSK1820795A is a selective antagonist at hGPR132a. Telmisartan analogue GSK1820795A was identified as a GPR132 antagonist through high‐throughput screening. Responses of yeast expressing hGPR132a to agonists NPGly (A), NLGly (B), linoleamide (C), and SB‐583831 (D) were blocked by GSK1820795A in a concentration‐dependent manner. Maximal effects NPGly, NLGly, and linoleamide (A‐C) were depressed by GSK1820795A with little effect on EC₅₀. In contrast, GSK1820795A caused rightward shifts of concentration‐response curves to SB‐583831 without reducing maximal responses. The effect of telmisartan on hGPR132a and Schild analysis are presented in Figure S3. Agonist responses of yeast expressing GPR43/FFA3 to propionate were not significantly affected by GSK1820795A (E). Data points show mean ± SD of four technical replicates (non‐normalized fluorescent counts) from a representative experiment