Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10595242 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
Abstract
The synthesis and evaluation of small molecule antagonists of the G protein-coupled receptor NPBWR1 (GPR7) are reported for the first time. [4-(5-Chloropyridin-2-yl)piperazin-1-yl][(1S,2S,4R)-4-{[(1R)-1-(4-methoxyphenyl)ethyl]amino}-2-(thiophen-3-yl)cyclohexyl]methanone (1) emerged as a hit from a high-throughput screen. Examination of substituents that focused on replacing the 5-chloropyridine and 4-methoxybenzylamino groups of 1 led to the identification of compounds that exhibited subnanomolar potencies as low as 660Â pM (9k) in the functional assay and 200Â pM in the binding assay (9i).
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Authors
F. Anthony Romero, Nicholas B. Hastings, Remond Moningka, Zhiqiang Guo, Ming Wang, Jerry Di Salvo, Ying Lei, Dorina Trusca, Qiaolin Deng, Vincent Tong, Jenna L. Terebetski, Richard G. Ball, Feroze Ujjainwalla,