BMS-986511

BMS-986511 is a first-in-class small molecule agonist of the G protein-coupled receptor 139 (GPR139), currently under development by Bristol Myers Squibb for the treatment of major depressive disorder (MDD). GPR139 is an orphan GPCR primarily expressed in the central nervous system, with high density in the medial habenula and lateral septum—brain regions implicated in mood regulation and the pathophysiology of depression. By activating GPR139, BMS-986511 is hypothesized to modulate neuronal activity within these circuits, potentially offering a novel antidepressant mechanism distinct from traditional monoaminergic therapies. The compound is being evaluated in Phase 2 clinical trials as a monotherapy to assess its efficacy and safety in adult patients with MDD.