Ontology highlight
ABSTRACT:
SUBMITTER: Shi F
PROVIDER: S-EPMC4028000 | biostudies-literature | 2011 Apr
REPOSITORIES: biostudies-literature
Shi Feng F Shen Jing Kang JK Chen Danqi D Fog Karina K Thirstrup Kenneth K Hentzer Morten M Karlsson Jens-Jakob JJ Menon Veena V Jones Kenneth A KA Smith Kelli E KE Smith Garrick G
ACS medicinal chemistry letters 20110228 4
GPR139 is an orphan G-protein coupled receptor (GPCR) which is primarily expressed in the central nervous system (CNS). In order to explore the biological function of this receptor, selective tool compounds are required. A screening campaign identified compound 1a as a high potency GPR139 agonist with an EC50 = 39 nM in a calcium mobilization assay in CHO-K1 cells stably expressing the GPR139 receptor. In the absence of a known endogenous ligand, the maximum effect was set as 100% for 1a. Screen ...[more]