1,3-dimethyl benzimidazolones are potent, selective inhibitors of the brpf1 bromodomain

ACS Medicinal Chemistry Letters

Volumn 5, Issue 11, 2014, Pages 1190-1195

  Demont, Emmanuel H ^a   Bamborough, Paul ^b   Chung, Chun Wa ^b   Craggs, Peter D ^b   Fallon, David ^a   Gordon, Laurie J ^b   Grandi, Paola ^c   Hobbs, Clare I ^b   Hussain, Jameed ^b   Jones, Emma J ^b   Le Gall, Armelle ^b   Michon, Anne Marie ^b,c   Mitchell, Darren J ^a   Prinjha, Rab K ^a   Roberts, Andy D ^c   Sheppard, Robert J ^a   Watson, Robert J ^a  

^a Epinova Discovery Performance Unit   (United Kingdom)

^b GLAXOSMITHKLINE   (United Kingdom)

^c GLAXOSMITHKLINE   (Germany)

Author keywords

BRD1; bromodomain; BRPF1; BRPF2; BRPF3; chemical probe; epigenetics; fragment; inhibitor

Indexed keywords

1,3 DIMETHYL BENZIMIDAZOLONE DERIVATIVE; BENZIMIDAZOLE DERIVATIVE; BROMODOMAIN INHIBITOR; BRPF1 BROMODOMAIN INHIBITOR; METHYL GROUP; UNCLASSIFIED DRUG;

ARTICLE; BINDING SITE; CRYSTAL STRUCTURE; DRUG BINDING; DRUG CONFORMATION; DRUG POTENCY; DRUG SELECTIVITY; DRUG SYNTHESIS; HETERONUCLEAR SINGLE QUANTUM COHERENCE; HYDROGEN BOND; MOLECULAR MODEL; NUCLEAR MAGNETIC RESONANCE; PRIORITY JOURNAL; STRUCTURE ACTIVITY RELATION;

EID: 84921309148     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/ml5002932     Document Type: Article

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