Maximizing diversity from a kinase screen: Identification of novel and selective pan-Trk inhibitors for chronic pain

Journal of Medicinal Chemistry

Volumn 57, Issue 13, 2014, Pages 5800-5816

  Stachel, Shawn J ^a   Sanders, John M ^a   Henze, Darrell A ^a   Rudd, Mike T ^a   Su, Hua Poo ^a   Li, Yiwei ^a   Nanda, Kausik K ^a   Egbertson, Melissa S ^a   Manley, Peter J ^a   Jones, Kristen L G ^a   Brnardic, Edward J ^a   Green, Ahren ^a   Grobler, Jay A ^a   Hanney, Barbara ^a   Leitl, Michael ^a   Lai, Ming Tain ^a   Munshi, Vandna ^a   Murphy, Dennis ^a   Rickert, Keith ^a   Riley, Daniel ^a   Krasowska Zoladek, Alicja ^a   Daley, Christopher ^a   Zuck, Paul ^a   Kane, Stephanie A ^a   Bilodeau, Mark T ^a   more..

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 CYCLOPROPYL 1 [3 (THIAZOL 2 YL)BENZYL] 3 [4 T(RIFLUOROMETHOXY)PHENYL]UREA; 1 ISOPROPYL 1 [3 (THIAZOLO 2 YL)BENZYL] 3 [4(TRIFLUOROMETHOXY)PHENYL]UREA; 1 [2 (4 CHLOROPHENOXY)ETHYL] 4 (3 ETHOXYPHENYL) 1H PYRROLO[3,2 C]PYRIDINE 2 CARBOXYLIC ACID; 2 [4 [6 (1H IMIDAZOL 1 YL)PYRIDIN 3 YL 1H 1,2,3 TRIAZOL 1 YL) N (3 TERT BUTYL) 1 (PYRIDIN 3 YL) 1H PYRAZOL 5 YL)ACETAMIDE; 2 [4 [6 (1H IMIDAZOL 1 YL)PYRIDIN 3 YL 1H 1,2,3 TRIAZOL 1 YL] 2 [4 [6 (1 (3 TERT BUTYL) 1 (PYRIDIN 3 YL) 1H PYRAZOL 5 YL]ACETAMIDE; 4 (NAPHTHYLEN 10 YL) 1 [(5 PHENYL 1,2,4 OXADIAZOL 3 YL)METHYL] 1,2,4 OXADIAZOL 3 YL]METHYL 1H PYRROLO[3,2 ]PYRIDINE 2 CARBOXYLIC ACID; 4 CHLORO 6 [2 (2,5 DIFLUOROPHENYL)PYRROLIDIN 1 YL]PYRIDO[3,2 D]PYRIMIDINE; AZAINDOLE DERIVATIVE; INDOLE DERIVATIVE; N (1H BENZIMIDAZOL 2 YLMETHYL) 6 [2 (2,5 DIFLUOROPHENYL)PYRROLIDIN 1 YL]PYRIDO[3,2 D]PYRIDIMINE 4 AMINE; N (3 CYCLOPROPYL 1 PHENYL 1H PYRAZOL 5 YL) 2 [4 [3 METHOXY 4 (4 METHYL 1H IMIDAZOL 1 YL)PHENYL 1H 1,2,3 TRIAZOL 1YL]ACETAMIDE; N4 (4 MORPHOLINOPHENYL) N6 (PYRIDIN 3 YLMETHYL)PYRIDO[3,2 D]PYRIMIDINE 4,6 DIAMINE; N6 (3 CHLOROBENZYL) N4 [4 (4 METHYLPIPERAZIN 1 YL)PHENYL]PYRIDO[3,2 D]PYRIMIDINE 4,6 DIAMINE; PHENYLTRIAZOLE DERIVATIVE; PROTEIN TYROSINE KINASE A; PROTEIN TYROSINE KINASE INHIBITOR; PYRIDOPYRIMIDINE DERIVATIVE; PYRIMIDINE DERIVATIVE; TRIAZOLE DERIVATIVE; UNCLASSIFIED DRUG; UREA DERIVATIVE;

ARTICLE; BINDING KINETICS; CHRONIC PAIN; CRYSTALLOGRAPHY; DRUG BINDING; DRUG BLOOD LEVEL; DRUG DESIGN; DRUG SCREENING; DRUG SYNTHESIS; HIGH THROUGHPUT SCREENING; INFLAMMATORY PAIN; LIPOPHILICITY; MAXIMUM PLASMA CONCENTRATION; NEUROPATHIC PAIN; PLASMA PROTEIN BINDING; STRUCTURE ACTIVITY RELATION;

ANIMALS; CHRONIC PAIN; DRUG EVALUATION, PRECLINICAL; HUMANS; INDOLES; LIGANDS; MODELS, MOLECULAR; PROTEIN KINASE INHIBITORS; PYRIMIDINES; RATS; RECEPTOR, TRKA; SMALL MOLECULE LIBRARIES; STRUCTURE-ACTIVITY RELATIONSHIP; TRIAZOLES; UREA;

EID: 84904297472     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm5006429     Document Type: Article

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