کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10595242 981861 2012 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
The discovery of potent antagonists of NPBWR1 (GPR7)
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
The discovery of potent antagonists of NPBWR1 (GPR7)
چکیده انگلیسی
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 660 pM (9k) in the functional assay and 200 pM in the binding assay (9i).
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 2, 15 January 2012, Pages 1014-1018
نویسندگان
, , , , , , , , , , , , ,