Screening Hit to Clinical Candidate: Discovery of BMS-963272, a Potent, Selective MGAT2 Inhibitor for the Treatment of Metabolic Disorders

MGAT2 inhibition is a potential therapeutic approach for the treatment of metabolic disorders. High-throughput screening of the BMS internal compound collection identified the aryl dihydropyridinone compound 1 (hMGAT2 IC50 = 175 nM) as a hit. Compound 1 had moderate potency against human MGAT2, was...

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Veröffentlicht in:	Journal of medicinal chemistry 2021-10, Vol.64 (19), p.14773-14792
Hauptverfasser:	Turdi, Huji, Chao, Hannguang, Hangeland, Jon J, Ahmad, Saleem, Meng, Wei, Brigance, Robert, Zhao, Guohua, Wang, Wei, Moore, Fang, Ye, Xiang-Yang, Mathur, Arvind, Hou, Xiaoping, Kempson, James, Wu, Dauh-Rurng, Li, Yi-Xin, Azzara, Anthony V, Ma, Zhengping, Chu, Ching-Hsuen, Chen, Luping, Cullen, Mary Jane, Rooney, Suzanne, Harvey, Susan, Kopcho, Lisa, Panemangelor, Reshma, Abell, Lynn, O’Malley, Kevin, Keim, William J, Dierks, Elizabeth, Chang, Shu, Foster, Kimberly, Apedo, Atsu, Harden, David, Dabros, Marta, Gao, Qi, Pelleymounter, Mary Ann, Whaley, Jean M, Robl, Jeffrey A, Cheng, Dong, Lawrence, R. Michael, Devasthale, Pratik
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Crystallography, X-Ray Drug Discovery Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Enzyme Inhibitors - therapeutic use High-Throughput Screening Assays - methods Humans Metabolic Diseases - drug therapy N-Acetylglucosaminyltransferases - antagonists & inhibitors Structure-Activity Relationship
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