The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor

Journal of Medicinal Chemistry

Volumn 57, Issue 19, 2014, Pages 8111-8131

  Gosmini, Romain ^a,c   Nguyen, Van Loc ^a   Toum, Jérôme ^a   Simon, Christophe ^a,c   Brusq, Jean Marie G ^a   Krysa, Gael ^a   Mirguet, Olivier ^a,d   Riou Eymard, Alizon M ^a   Boursier, Eric V ^a   Trottet, Lionel ^a   Bamborough, Paul ^b   Clark, Hugh ^b   Chung, Chun Wa ^b   Cutler, Leanne ^b   Demont, Emmanuel H ^b   Kaur, Rejbinder ^b   Lewis, Antonia J ^b   Schilling, Mark B ^b   Soden, Peter E ^b   Taylor, Simon ^b   Walker, Ann L ^b   Walker, Matthew D ^b   Prinjha, Rab K ^b   Nicodème, Edwige ^a   more..

^a GLAXOSMITHKLINE   (France)

^b GLAXOSMITHKLINE   (United Kingdom)

^c DMPK GlaxoSmithKline les Ulis GlaxoSmithKline R and D ^*  (France)

^d INSTITUT DE RECHERCHES INTERNATIONALES SERVIER   (France)

Author keywords

[No Author keywords available]

Indexed keywords

4 [(2,4) 1 ACETYL 4 [(4 CHLOROPHENYL)AMINO] 2 METHYL 1,2,3,4 TETRAHYDROQUINOLIN 6 YL]BENZOIC ACID; APOLIPOPROTEIN A1; BROMODOMAIN INHIBITOR; QUINOLINE DERIVATIVE; UNCLASSIFIED DRUG; 1,2,3,4-TETRAHYDROQUINOLINE; 4-(1-ACETYL-4-((4-CHLOROPHENYL)AMINO)-2-METHYL-1,2,3,4-TETRAHYDROQUINOLIN-6-YL)BENZOIC ACID; AMINOQUINOLINE DERIVATIVE; ANTIINFLAMMATORY AGENT; BENZOIC ACID DERIVATIVE; BRD2 PROTEIN, HUMAN; BRD4 PROTEIN, HUMAN; NUCLEAR PROTEIN; PROTEIN SERINE THREONINE KINASE; TRANSCRIPTION FACTOR;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; DRUG POTENCY; MOUSE; MURINE MODEL; NEUROBLASTOMA; NONHUMAN; SEPTIC SHOCK; SINGLE DRUG DOSE; STRUCTURE ACTIVITY RELATION; UPREGULATION; X RAY CRYSTALLOGRAPHY; ANIMAL; ANTAGONISTS AND INHIBITORS; DRUG DEVELOPMENT; HUMAN; METABOLISM; SYNTHESIS;

AMINOQUINOLINES; ANIMALS; ANTI-INFLAMMATORY AGENTS; APOLIPOPROTEIN A-I; BENZOATES; DRUG DISCOVERY; HUMANS; MICE; NUCLEAR PROTEINS; PROTEIN-SERINE-THREONINE KINASES; QUINOLINES; STRUCTURE-ACTIVITY RELATIONSHIP; TRANSCRIPTION FACTORS;

EID: 84907894098     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm5010539     Document Type: Article

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