Discovery of a potent, cell penetrant, and selective p300/CBP-associated factor (PCAF)/general control nonderepressible 5 (GCN5) bromodomain chemical probe

Journal of Medicinal Chemistry

Volumn 60, Issue 2, 2017, Pages 695-709

  Humphreys, Philip G ^a   Bamborough, Paul ^a   Chung, Chun Wa ^a   Craggs, Peter D ^a   Gordon, Laurie ^a   Grandi, Paola ^b   Hayhow, Thomas G ^a   Hussain, Jameed ^a   Jones, Katherine L ^a   Lindon, Matthew ^a   Michon, Anne Marie ^b   Renaux, Jessica F ^a   Suckling, Colin J ^c   Tough, David F ^a   Prinjha, Rab K ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

^b GLAXOSMITHKLINE   (Germany)

^c UNIVERSITY OF STRATHCLYDE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

4 BROMO 2 METHYL 5 ((1 METHYL 5 PHENYLPIPERIDIN 3 YL)AMINO)PYRIDAZIN 3(2H) ONE; ANILINE DERIVATIVE; BET BROMODOMAIN PROTEIN; GENERAL CONTROL NONDEREPRESSIBLE 5; HISTONE ACETYLTRANSFERASE PCAF; PYRIDAZINONE DERIVATIVE; TRANSCRIPTION FACTOR; UNCLASSIFIED DRUG; ARTIFICIAL MEMBRANE; GSK4027; HISTONE ACETYLTRANSFERASE; KAT2A PROTEIN, HUMAN; MOLECULAR PROBE; P300-CBP-ASSOCIATED FACTOR; PIPERIDINE DERIVATIVE; PYRIDAZINE DERIVATIVE;

ARTICLE; CARBOXY TERMINAL SEQUENCE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SELECTIVITY; DRUG SOLUBILITY; PROTEIN FAMILY; STEREOCHEMISTRY; STRUCTURE ACTIVITY RELATION; X RAY CRYSTALLOGRAPHY; ANIMAL; ARTIFICIAL MEMBRANE; CELL MEMBRANE PERMEABILITY; CHEMISTRY; HUMAN; MOLECULAR PROBE; MOUSE; PROTEIN DOMAIN; STEREOISOMERISM; SYNTHESIS;

ANIMALS; CELL MEMBRANE PERMEABILITY; HISTONE ACETYLTRANSFERASES; HUMANS; MEMBRANES, ARTIFICIAL; MICE; MOLECULAR PROBES; P300-CBP TRANSCRIPTION FACTORS; PIPERIDINES; PROTEIN DOMAINS; PYRIDAZINES; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 85010715473     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.6b01566     Document Type: Article

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