Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637)

ACS Medicinal Chemistry Letters

Volumn 7, Issue 5, 2016, Pages 531-536

  Taylor, Alexander M ^a   Côté, Alexandre ^a   Hewitt, Michael C ^a   Pastor, Richard ^b   Leblanc, Yves ^a   Nasveschuk, Christopher G ^a   Romero, F Anthony ^b   Crawford, Terry D ^b   Cantone, Nico ^a   Jayaram, Hariharan ^a   Setser, Jeremy ^a   Murray, Jeremy ^b   Beresini, Maureen H ^b   De Leon Boenig, Gladys ^b   Chen, Zhongguo ^c   Conery, Andrew R ^a   Cummings, Richard T ^a   Dakin, Leslie A ^a   Flynn, E Megan ^b   Huang, Oscar W ^b   Kaufman, Susan ^b   Keller, Patricia J ^a   Kiefer, James R ^b   Lai, Tommy ^c   Li, Yingjie ^c   Liao, Jiangpeng ^c   Liu, Wenfeng ^c   Lu, Henry ^c   Pardo, Eneida ^a   Tsui, Vickie ^b   Wang, Jian ^c   Wang, Yongyun ^c   Xu, Zhaowu ^c   Yan, Fen ^c   Yu, Dong ^c   Zawadzke, Laura ^a   Zhu, Xiaoqin ^c   Zhu, Xiaoyu ^c   Sims, Robert J ^a   Cochran, Andrea G ^b   Bellon, Steve ^a   Audia, James E ^a   Magnuson, Steven ^b   Albrecht, Brian K ^a   more..

^a Department of Structural Biology   (United States)

^b GENENTECH INC   (United States)

^c WUXI APPTEC   (China)

Author keywords

benzodiazepinone; Bromodomain; CBP; CREBBP; EP300

Indexed keywords

4 METHYL 1,3,4,5 TETRAHYDRO 2H BENZO[B][1,4]DIAZEPIN 2 ONE; BENZODIAZEPINE DERIVATIVE; BROMODOMAIN INHIBITOR; CBP EP300 BROMODOMAIN INHIBITOR; UNCLASSIFIED DRUG;

ARTICLE; BINDING AFFINITY; DRUG BINDING; DRUG IDENTIFICATION; DRUG POTENCY; DRUG SCREENING; DRUG SELECTIVITY; EC50; HYDROGEN BOND; IC50; IN VITRO STUDY; PHYSICAL CHEMISTRY; PRIORITY JOURNAL; STRUCTURE ACTIVITY RELATION;

EID: 84969523100     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/acsmedchemlett.6b00075     Document Type: Article

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