DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors

Journal of Medicinal Chemistry

Volumn 59, Issue 5, 2016, Pages 2163-2178

  Harris, Philip A ^a   King, Bryan W ^b   Bandyopadhyay, Deepak ^b   Berger, Scott B ^a   Campobasso, Nino ^b   Capriotti, Carol A ^a   Cox, Julie A ^b   Dare, Lauren ^a   Dong, Xiaoyang ^a   Finger, Joshua N ^a   Grady, LaShadric C ^b   Hoffman, Sandra J ^a   Jeong, Jae U ^a   Kang, James ^a   Kasparcova, Viera ^a   Lakdawala, Ami S ^b   Lehr, Ruth ^b   McNulty, Dean E ^b   Nagilla, Rakesh ^a   Ouellette, Michael T ^b   Pao, Christina S ^b   Rendina, Alan R ^b   Schaeffer, Michelle C ^b   Summerfield, Jennifer D ^b   Swift, Barbara A ^a   Totoritis, Rachel D ^b   Ward, Paris ^b   Zhang, Aming ^b   Zhang, Daohua ^b   Marquis, Robert W ^a   Bertin, John ^a   Gough, Peter J ^a   more..

^a Glaxo SmithKline   (United States)

^b GLAXOSMITHKLINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

(5 METHYL 4 OXO-2,3,4,5 TETRAHYDROBENZO[ B ][1,4]OXAZEPIN 3 YL) 5 (3 (3 (TRIFLUOROMETHYL) 3H DIAZERIN 3 YL) BENZYL) 1H PYRAZOLE 3 CARBOXAMIDE; 5 BENZYL (1 METHYL 2 OXO 7 (3 (TRIFLUOROMETHYL) 3H DIAZIRIN 3 YL) 2,3,4,5 TETRAHYDRO 1H BENZO[B]AZEPIN 3 YL) ISOXAZOLE 3 CARBOXAMIDE; 5 BENZYL N (1 METHYL 2 OXO 2,3,4,5 TETRAHYDRO 1H BENZO[B]AZEPIN 3 YL)ISOXAZOLE 3 CARBOXAMIDE; 5 BENZYL N (1 METHYL 2 OXO 2,3,4,5 TETRAHYDRO 1H BENZO[B][1,4]DIAZEPIN 3 YL)ISOXAZOLE 3 CARBOXAMIDE; 5 BENZYL N (1,1 DIOXIDO 4 OXO 2,3,4,5 TETRAHYDROBENZO [B][1,4]THIAZEPIN 3 YL)ISOXAZOLE 3 CARBOXAMIDE; 5 BENZYL N (2 OXO 2,3,4,5 TETRAHYDRO 1H BENZO[B][1,4] DIAZEPIN 3 YL)ISOXAZOLE 3 CARBOXAMIDE; 5 BENZYL N (4 OXO 2,3,4,5 TETRAHYDROBENZO[ B ][1,4]OXAZEPIN 3 YL)ISOXAZOLE 3 CARBOXAMIDE; 5 BENZYL N (5 METHYL 4 OXO 2,3,4,5 TETRAHYDROBENZO[B] [1,4]OXAZEPIN 3 YL)ISOXAZOLE 3 CARBOXAMIDE; 5 BENZYL N (5 METHYL 4 OXO 2,3,4,5 TETRAHYDROBENZO[B] [1,4]THIAZEPIN 3 YL)ISOXAZOLE 3 CARBOXAMIDE; 5 BENZYL N (5 METHYL 4 OXO 2,3,4,5 TETRAHYDROBENZO[B][1,4]OXAZEPIN 3 YL) 1H PYRAZOLE 3 CARBOXAMIDE; BENZODIAZEPINE DERIVATIVE; N (4 OXO 2,3,4,5 TETRAHYDROBENZO[ B ][1,4]OXAZEPIN 3 YL) 5 PENTYL 1H PYRAZOLE 3 CARBOXAMIDE; N (4 OXO 2,3,4,5 TETRAHYDROBENZO[ B ][1,4]OXAZEPIN-3 YL) 3 PHENOXYBENZAMIDE; PHOSPHOTRANSFERASE; PHOSPHOTRANSFERASE INHIBITOR; RECEPTOR INTERACTING PROTEIN 1; TUMOR NECROSIS FACTOR; UNCLASSIFIED DRUG; DNA; GSK'481; ISOXAZOLE DERIVATIVE; MOLECULAR LIBRARY; OXAZEPINE DERIVATIVE; PROTEIN KINASE INHIBITOR; RECEPTOR INTERACTING PROTEIN SERINE THREONINE KINASE; RIPK1 PROTEIN, HUMAN; RIPK1 PROTEIN, MOUSE;

AREA UNDER THE CURVE; ARTICLE; CHEMICAL STRUCTURE; DOG; DRUG POTENCY; FLUORESCENCE POLARIZATION IMMUNOASSAY; HAPLORHINI; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; IC50; IN VITRO STUDY; INFLAMMATORY DISEASE; MAXIMUM PLASMA CONCENTRATION; MINIPIG; MOLECULAR LIBRARY; MOUSE; NONHUMAN; PROTEIN CONFORMATION; PROTON NUCLEAR MAGNETIC RESONANCE; RABBIT; RAT; SYNTHESIS; U937 CELL LINE; ANIMAL; ANTAGONISTS AND INHIBITORS; CHEMISTRY; DOSE RESPONSE; HT 29 CELL LINE; METABOLISM; PHARMACOLOGY; STRUCTURE ACTIVITY RELATION; TUMOR CELL LINE; X RAY CRYSTALLOGRAPHY;

ANIMALS; CELL LINE, TUMOR; CRYSTALLOGRAPHY, X-RAY; DNA; DOSE-RESPONSE RELATIONSHIP, DRUG; HT29 CELLS; HUMANS; ISOXAZOLES; MICE; MODELS, MOLECULAR; MOLECULAR STRUCTURE; OXAZEPINES; PROTEIN KINASE INHIBITORS; RECEPTOR-INTERACTING PROTEIN SERINE-THREONINE KINASES; SMALL MOLECULE LIBRARIES; STRUCTURE-ACTIVITY RELATIONSHIP; U937 CELLS;

EID: 84961170811     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.5b01898     Document Type: Article

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