Discovery of a Potent and Selective First-In-Class Antagonist of GPR15 With In Vivo Anti-Obesity Activity.
GPR15 (G Protein-coupled Receptor 15), an atypical chemokine receptor, is implicated in the pathogenesis of multiple diseases, yet small-molecule GPR15 antagonists remain undeveloped. Herein, we identify and characterize YL410, the first-in-class potent and selective GPR15 antagonist. In the cAMP-GloSensor assay, YL410...