Discovery and Preclinical Pharmacology of an Oral Bromodomain and Extra-Terminal (BET) Inhibitor Using Scaffold-Hopping and Structure-Guided Drug Design

Author:

Gavai Ashvinikumar V.1ORCID,Norris Derek1,Delucca George1,Tortolani David1,Tokarski John S.1,Dodd Dharmpal1,O’Malley Daniel1,Zhao Yufen1,Quesnelle Claude1,Gill Patrice1,Vaccaro Wayne1,Huynh Tram1,Ahuja Vijay1,Han Wen-Ching1,Mussari Christopher1,Harikrishnan Lalgudi1,Kamau Muthoni1,Poss Michael1,Sheriff Steven1,Yan Chunhong1,Marsilio Frank1,Menard Krista1,Wen Mei-Li1,Rampulla Richard1,Wu Dauh-Rurng1,Li Jianqing1ORCID,Zhang Huiping1,Li Peng1,Sun Dawn1,Yip Henry1,Traeger Sarah C.1,Zhang Yingru1,Mathur Arvind1,Zhang Haiying1,Huang Christine1,Yang Zheng1,Ranasinghe Asoka1,Everlof Gerry1,Raghavan Nirmala1,Tye Ching Kim1,Wee Susan1,Hunt John T.1,Vite Gregory1,Westhouse Richard1,Lee Francis Y.1

Affiliation:

1. Research and Development, Bristol Myers Squibb Company, P. O. Box 4000, Princeton, New Jersey 08543-4000, United States

Funder

Office of Science

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

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