Identification and SAR of Glycine Benzamides as Potent Agonists for the GPR139 Receptor.

ABSTRACT: A focused high throughput screening for GPR139 was completed for a select 100K compounds, and new agonist leads were identified. Subsequent analysis and structure-activity relationship studies identified (S)-3-chloro-N-(2-oxo-2-((1-phenylethyl)amino)ethyl)benzamide 7c as a potent and selective agonist of hGPR139 with an EC50 = 16 nM. The compound was found to cross the blood-brain barrier and have good drug-like properties amenable for oral dosing in rat.

SUBMITTER: Dvorak CA 

PROVIDER: S-EPMC4569879 | biostudies-literature | 2015 Sep

REPOSITORIES: biostudies-literature