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

Author:

Taylor Alexander M.1,Côté Alexandre1,Hewitt Michael C.1,Pastor Richard2,Leblanc Yves1,Nasveschuk Christopher G.1,Romero F. Anthony2,Crawford Terry D.2,Cantone Nico1,Jayaram Hariharan1,Setser Jeremy1,Murray Jeremy2,Beresini Maureen H.2,de Leon Boenig Gladys2,Chen Zhongguo3,Conery Andrew R.1,Cummings Richard T.1,Dakin Leslie A.1,Flynn E. Megan2,Huang Oscar W.2,Kaufman Susan2,Keller Patricia J.1,Kiefer James R.2,Lai Tommy3,Li Yingjie3,Liao Jiangpeng3,Liu Wenfeng3,Lu Henry3,Pardo Eneida1,Tsui Vickie2,Wang Jian3,Wang Yongyun3,Xu Zhaowu3,Yan Fen3,Yu Dong3,Zawadzke Laura1,Zhu Xiaoqin3,Zhu Xiaoyu3,Sims Robert J.1,Cochran Andrea G.2,Bellon Steve1,Audia James E.1,Magnuson Steven2,Albrecht Brian K.1

Affiliation:

1. Constellation Pharmaceuticals, 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States

2. Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States

3. Wuxi AppTec Co., Ltd., 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, People’s Republic of China

Publisher

American Chemical Society (ACS)

Subject

Organic Chemistry,Drug Discovery,Biochemistry

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