Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit

Journal of Medicinal Chemistry

Volumn 59, Issue 10, 2016, Pages 4800-4811

  Gerstenberger, Brian S ^a   Trzupek, John D ^a   Tallant, Cynthia ^b   Fedorov, Oleg ^b   Filippakopoulos, Panagis ^b,c   Brennan, Paul E ^b   Fedele, Vita ^b   Martin, Sarah ^b   Picaud, Sarah ^b   Rogers, Catherine ^b   Parikh, Mihir ^a   Taylor, Alexandria ^a   Samas, Brian ^a   O'Mahony, Alison ^d   Berg, Ellen ^d   Pallares, Gabriel ^e   Torrey, Adam D ^e   Treiber, Daniel K ^e   Samardjiev, Ivan J ^f   Nasipak, Brian T ^g   Padilla Benavides, Teresita ^g   Wu, Qiong ^g   Imbalzano, Anthony N ^g   Nickerson, Jeffrey A ^g   Bunnage, Mark E ^a   Müller, Susanne ^b   Knapp, Stefan ^b,h   Owen, Dafydd R ^a   more..

^a PFIZER INC   (United States)

^b UNIVERSITY OF OXFORD   (United Kingdom)

^c UNIVERSITY OF OXFORD   (United Kingdom)

^d Bioseek Inc   (United States)

^e Division of DiscoveRx   (United States)

^f Eurofins Medinet Inc   (Germany)

^g UNIVERSITY OF MASSACHUSETTS MEDICAL SCHOOL   (United States)

^h GOETHE UNIVERSITY   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

1 (2 HYDROXYPHENYL) 3 [5 (PYRIDIN 2 YL) 2,5DIAZABICYCLO[2.2.1]HEPTAN 2 YL]PROP 2 EN 1 ONE; 3 (4,5 DIHYDRO 1H PYRAZOLO[3,4 C ]PYRIDIN 6(7H) YL] 1 (2 HYDROXYPHENYL)PROP 2 EN 1 ONE; BRG1 PROTEIN; BRM PROTEIN; BROMODOMAIN INHIBITOR; CELL PROTEIN; CYTOTOXIC AGENT; PROTEIN POLYBROMO 1; UNCLASSIFIED DRUG; AZABICYCLO DERIVATIVE; MOLECULAR PROBE; NUCLEAR PROTEIN; PBRM1 PROTEIN, HUMAN; PF-06687252; PYRIDINE DERIVATIVE; TRANSCRIPTION FACTOR;

ADIPOCYTE; ARTICLE; CANCER CELL; CELL DIFFERENTIATION; CELL VIABILITY; DRUG BINDING; DRUG IDENTIFICATION; DRUG SCREENING; KIDNEY CARCINOMA; MOLECULAR PROBE; MYOBLAST; PHENOTYPE; PROCESS OPTIMIZATION; PROTEIN DOMAIN; PROTEIN MOTIF; ANTAGONISTS AND INHIBITORS; CHEMICAL STRUCTURE; CHEMISTRY; DOSE RESPONSE; DRUG EFFECTS; ENZYME SPECIFICITY; HUMAN; METABOLISM; MOLECULAR MODEL; PHARMACOLOGY; PROTEIN PROCESSING; STRUCTURE ACTIVITY RELATION; SYNTHESIS; X RAY CRYSTALLOGRAPHY;

AZABICYCLO COMPOUNDS; CRYSTALLOGRAPHY, X-RAY; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; MODELS, MOLECULAR; MOLECULAR PROBES; MOLECULAR STRUCTURE; NUCLEAR PROTEINS; PROTEIN PROCESSING, POST-TRANSLATIONAL; PYRIDINES; STRUCTURE-ACTIVITY RELATIONSHIP; SUBSTRATE SPECIFICITY; TRANSCRIPTION FACTORS;

EID: 84971647366     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.6b00012     Document Type: Article

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