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.
journal_name
ACS Med Chem Lettjournal_title
ACS medicinal chemistry lettersauthors
Dvorak CA,Coate H,Nepomuceno D,Wennerholm M,Kuei C,Lord B,Woody D,Bonaventure P,Liu C,Lovenberg T,Carruthers NIdoi
10.1021/acsmedchemlett.5b00247subject
Has Abstractpub_date
2015-07-20 00:00:00pages
1015-8issue
9issn
1948-5875journal_volume
6pub_type
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