jnj-63533054

Description: JNJ-63533054, a glycine benzamide analog, is a potent, selective and brain penetrant agonist of hGPR139 (human G-protein-coupled receptors) with an EC50 of 16 nM. It was identified from a focused high throughput screening for GPR139 completed for a select of 100K compounds. Subsequent analysis and structure-activity relationship studies identified (S)-3-chloro-N-(2-oxo-2-((1-phenylethyl)amino)ethyl)benzamide, JNJ-63533054, as a potent and selective agonist of hGPR139 with an EC50 of 16 nM. JNJ-63533054 was found to cross the blood-brain barrier and have good drug-like properties amenable for oral dosing in rat.

References: ACS Med Chem Lett. 2015 Jul 20; 6(9):1015-8.