Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B

Author:

Chen Peiling1,Chaikuad Apirat2,Bamborough Paul3,Bantscheff Marcus4,Bountra Chas5,Chung Chun-wa3,Fedorov Oleg25,Grandi Paola4,Jung David1,Lesniak Robert1,Lindon Matthew,Müller Susanne25,Philpott Martin25,Prinjha Rab,Rogers Catherine25,Selenski Carolyn1,Tallant Cynthia25,Werner Thilo4,Willson Timothy M.1,Knapp Stefan256,Drewry David H.1

Affiliation:

1. Department of Chemical Biology, GlaxoSmithKline, Research Triangle Park, 5 Moore Drive, Research Triangle Park, North Carolina 27709-3398, United States

2. Nuffield Department of Clinical Medicine, Structural Genomics Consortium, University of Oxford, Old Road Campus Research Building, Roosevelt Drive, Headington, Oxford OX3 7DQ, United Kingdom

3. Computational & Structural Chemistry, Molecular Discovery Research, and ⊥Epinova, Discovery Performance Unit, GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom

4. Cellzome GmbH, Molecular Discovery Research, GlaxoSmithKline, Meyerhofstrasse 1, 69117 Heidelberg, Germany

5. Nuffield Department of Clinical Medicine, Target Discovery Institute, University of Oxford, NDM Research Building, Roosevelt Drive, Headington, Oxford OX3 7FZ, United Kingdom

6. Institute for Pharmaceutical Chemistry, Johann Wolfgang Goethe-University, Max-von-Laue-Str. 9, D-60438 Frankfurt am Main, Germany

Funder

Wellcome Trust

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

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