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

Journal of Medicinal Chemistry

Volumn 59, Issue 4, 2016, Pages 1410-1424

  Chen, Peiling ^b   Chaikuad, Apirat ^a   Bamborough, Paul ^c   Bantscheff, Marcus ^d   Bountra, Chas ^a   Chung, Chun Wa ^c   Fedorov, Oleg ^a   Grandi, Paola ^d   Jung, David ^b   Lesniak, Robert ^b   Lindon, Matthew ^c   Müller, Susanne ^a   Philpott, Martin ^a   Prinjha, Rab ^c   Rogers, Catherine ^a   Selenski, Carolyn ^b   Tallant, Cynthia ^a   Werner, Thilo ^d   Willson, Timothy M ^b   Knapp, Stefan ^a,e   Drewry, David H ^b   more..

^a UNIVERSITY OF OXFORD   (United Kingdom)

^b GLAXOSMITHKLINE   (United States)

^c GLAXOSMITHKLINE   (United Kingdom)

^d GLAXOSMITHKLINE   (Germany)

^e GOETHE UNIVERSITY   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

ANIMAL EXPERIMENT; ANIMAL TISSUE; BIOLOGY; BLEACHING; CHEMICAL BINDING; CHROMATIN; CLEARANCE; CONTROLLED STUDY; CRYSTAL; CRYSTAL STRUCTURE; DISSOCIATION CONSTANT; DRUG DOSAGE FORM; EXPOSURE; MONITORING; NONHUMAN; PLASMA; ACETYLATION; ANIMAL; ANTAGONISTS AND INHIBITORS; CELL LINE; CHEMISTRY; HUMAN; MALE; METABOLISM; MOLECULAR MODEL; MOLECULAR PROBE; MOUSE; PHARMACOKINETICS; PHARMACOLOGY; X RAY CRYSTALLOGRAPHY;

1-(1-(3-(METHYLSULFONYL)PHENYL)-7-PROPOXYINDOLIZIN-3-YL)ETHANONE; BAZ2A PROTEIN, HUMAN; BAZ2B PROTEIN, HUMAN; INDOLIZINE DERIVATIVE; LYSINE; MOLECULAR PROBE; NONHISTONE PROTEIN; PROTEIN; PROTEIN BINDING; SULFONE;

ACETYLATION; ANIMALS; CELL LINE; CHROMOSOMAL PROTEINS, NON-HISTONE; CRYSTALLOGRAPHY, X-RAY; HUMANS; INDOLIZINES; LYSINE; MALE; MICE; MODELS, MOLECULAR; MOLECULAR PROBES; PROTEIN BINDING; PROTEINS; SULFONES;

EID: 84959378549     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.5b00209     Document Type: Article

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