Fragment-based discovery of bromodomain inhibitors part 1: Inhibitor binding modes and implications for lead discovery

Journal of Medicinal Chemistry

Volumn 55, Issue 2, 2012, Pages 576-586

  Chung, Chun Wa ^a   Dean, Anthony W ^a   Woolven, James M ^a   Bamborough, Paul ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

1 (1 (PYRIDIN 2 YL)INDOLIZIN 3 YL)ETHANONE; 3 METHYL 3,4 DIHYDROQUINAZOLIN 2(1H)ONE; BRD2 PROTEIN; METHYL GROUP; N ACETYL 2 METHYLTETRAHYDROQUINOLINE; N METHYLPYRROLIDIN 2 ONE; PARACETAMOL; PEPTIDE FRAGMENT; PROTEIN; PROTEIN INHIBITOR; UNCLASSIFIED DRUG;

ARTICLE; DRUG BINDING; DRUG BINDING SITE; DRUG SCREENING; DRUG STRUCTURE; ENZYME ACTIVE SITE; EPIGENETICS; GENETIC TRANSCRIPTION; HIGH THROUGHPUT SCREENING; HYDROGEN BOND; MOLECULAR WEIGHT; PROTEIN BINDING; PROTEIN DOMAIN; X RAY CRYSTALLOGRAPHY;

ACETAMINOPHEN; AMINO ACID SEQUENCE; CRYSTALLOGRAPHY, X-RAY; FLUORESCENCE POLARIZATION; HUMANS; INDOLIZINES; MODELS, MOLECULAR; MOLECULAR SEQUENCE DATA; MOLECULAR STRUCTURE; NUCLEAR PROTEINS; PEPTIDOMIMETICS; PROTEIN BINDING; PROTEIN STRUCTURE, TERTIARY; PROTEIN-SERINE-THREONINE KINASES; PYRIDINES; PYRROLIDINONES; QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIP; QUINAZOLINONES; RNA-BINDING PROTEINS; TRANSCRIPTION FACTORS;

EID: 84856397832     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm201320w     Document Type: Article

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