Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase

Journal of Medicinal Chemistry

Volumn 57, Issue 21, 2014, Pages 8817-8826

  Deng, Yongqi ^a   Shipps, Gerald W ^a   Cooper, Alan ^a   English, Jessie M ^a   Annis, D Allen ^a   Carr, Donna ^a   Nan, Yang ^a   Wang, Tong ^a   Zhu, Hugh Y ^a   Chuang, Cheng Chi ^a   Dayananth, Priya ^a   Hruza, Alan W ^a   Xiao, Li ^a   Jin, Weihong ^a   Kirschmeier, Paul ^a   Windsor, William T ^a   Samatar, Ahmed A ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 [2 [4 (3 CHLOROPHENYL)PIPERAZIN 1 YL] 2 OXOETHYL] N (4 HYDROXYPHENYL)PYRROLIDINE 3 CARBOXAMIDE HYDROCHLORIDE; 1 [2 [4 (4 ACETYLPHENYL)PIPERAZIN 1 YL] 2 OXOETHYL] N (2 CHLORO 4 HYDROXYPHENYL)PYRROLIDINE 3 CARBOXAMIDE HYDROCHLORIDE; 1 [2 [4 (4 ACETYLPHENYL)PIPERAZIN 1 YL] 2 OXOETHYL] N (3 BROMO 4 HYDROXYPHENYL)PYRROLIDINE 3 CARBOXAMIDE HYDROCHLORIDE; 1 [2 [4 (4 ACETYLPHENYL)PIPERAZIN 1 YL] 2 OXOETHYL] N (3 CHLORO 4 HYDROXYPHENYL)PYRROLIDINE 3 CARBOXAMIDE HYDROCHLORIDE; 1 [2 [4 (4 ACETYLPHENYL)PIPERAZIN 1 YL] 2 OXOETHYL] N (3 FLUORO 4 HYDROXYPHENYL)PYRROLIDINE 3 CARBOXAMIDE HYDROCHLORIDE; 1 [2 [4 (4 ACETYLPHENYL)PIPERAZIN 1 YL] 2 OXOETHYL] N (4 HYDROXYPHENYL)PYRROLIDINE 3 CARBOXAMIDE HYDROCHLORIDE; 1 [2 [4 (4 ACETYLPHENYL)PIPERAZIN 1 YL] 2 OXOETHYL]PYRROLIDINE 3 CARBOXYLIC ACID; 1 [2 [4 (4 BROMOPHENYL)PIPERAZIN 1 YL] 2 OXOETHYL] N (3 CHLORO 4 HYDROXYPHENYL)PYRROLIDINE 3 CARBOXAMIDE HYDROCHLORIDE; 1 [2 [4 (4 CHLOROPHENYL)PIPERAZIN 1 YL] 2 OXOETHYL] N (3 CHLORO 4 HYDROXYPHENYL)PYRROLIDINE 3 CARBOXAMIDE HYDROCHLORIDE; 1 [2 [4 (BENZO[D]THIAZOL 2 YL)PIPERAZIN 1 YL] 2 OXOETHYL] N (3 CHLORO 4 HYDROXYPHENYL)PYRROLIDINE 3 CARBOXAMIDE; 1 [2 [4 (BIPHENYL 4)PIPERAZIN 1 YL] 2 OXOETHYL] N (3 CHLORO 4 HYDROXYPHENYL)PYRROLIDINE 3 CARBOXAMIDE; 2 [3 (3 CHLORO 4 HYDROXYPHENYLCARBAMOYL)PYRROLIDIN 1 YL]ACETIC ACID; 2 [3 (4 HYDROXYPHENYLCARBAMOYL)PYRROLIDIN 1 YL]ACETIC ACID; 2 [3 (METHOXYCARBONYL)PYRROLIDIN 1 YL]ACETIC ACID; ETHYL 2 [3 (3 CHLORO 4 HYDROXYPHENYLCARBAMOYL)PYRROLIDIN 1 YL]ACETATE; ETHYL 2 [3 (4 HYDROXYPHENYLCARBAMOYL)PYRROLIDIN 1 YL]ACETATE; METHYL 1 (2 TERT BUTOXY 2 OXOETHYL)PYRROLIDINE 3 CARBOXYLATE; METHYL 1 [2 [4 (4 ACETYLPHENYL)PIPERAZIN 1 YL] 2 OXOETHYL]PYRROLIDINE 3 CARBOXYLATE; METHYL PYRROLIDINE 3 CARBOXYLATE; MITOGEN ACTIVATED PROTEIN KINASE 1; MITOGEN ACTIVATED PROTEIN KINASE 3; N (3 CHLORO 4 HYDROXYPHENYL) 1 [2 OXO 2 [4 [4 (THIOPHEN 3 YL)PHENYL]PIPERAZIN 1 YL]ETHYL]PYRROLIDINE 3 CARBOXAMIDE; N (3 CHLORO 4 HYDROXYPHENYL) 1 [2 [4 (3 CHLOROPHENYL)PIPERAZIN 1 YL] 2 OXOETHYL]PYRROLIDINE 3 CARBOXAMIDE; N (3 CHLORO 4 HYDROXYPHENYL) 1 [2 [4 [4 (FURAN 3 YL)PHENYL]PIPERAZIN 1 YL]2 OXOETHYL]PYRROLIDINE 3 CARBOXAMIDE; N (3 CHLORO 4 HYDROXYPHENYL)PYRROLIDINE 3 CARBOXAMIDE TRIFLUOROACETATE; N (4 HYDROXYPHENYL)PYRROLIDINE 3 CARBOXAMIDE TRIFLUOROACETATE; PROTEIN SERINE THREONINE KINASE INHIBITOR; TERT BUTYL 3 (3 CHLORO 4 HYDROXYPHENYLCARBAMOYL)PYRROLIDINE 1 CARBOXYLATE; TERT BUTYL 3 (4 HYDROXYPHENYLCARBAMOYL)PYRROLIDINE 1 CARBOXYLATE; UNCLASSIFIED DRUG; UNINDEXED DRUG; 1-(2-(4-(4-ACETYLPHENYL)PIPERAZIN-1-YL)-2-OXOETHYL)-N-(3-CHLORO-4-HYDROXYPHENYL)PYRROLIDINE-3-CARBOXAMIDE; AFFINITY LABELING; ANILIDE; PROTEIN KINASE INHIBITOR; PYRROLIDINE DERIVATIVE;

AFFINITY SELECTION MASS SPECTROMETRY; ARTICLE; BINDING AFFINITY; BINDING SITE; CONTROLLED STUDY; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SCREENING; DRUG SELECTIVITY; ENZYME ACTIVITY; ENZYME INACTIVATION; ENZYME INHIBITION; ENZYME PHOSPHORYLATION; ENZYME SUBSTRATE; MASS SPECTROMETRY; X RAY CRYSTALLOGRAPHY; AFFINITY LABELING; ANTAGONISTS AND INHIBITORS; DRUG EFFECTS; IC50; METABOLISM; PHOSPHORYLATION; PROCEDURES; SIGNAL TRANSDUCTION; STRUCTURE ACTIVITY RELATION; SYNTHESIS;

AFFINITY LABELS; ANILIDES; CRYSTALLOGRAPHY, X-RAY; INHIBITORY CONCENTRATION 50; MAP KINASE SIGNALING SYSTEM; MASS SPECTROMETRY; MITOGEN-ACTIVATED PROTEIN KINASE 1; PHOSPHORYLATION; PROTEIN KINASE INHIBITORS; PYRROLIDINES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84923805796     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm500847m     Document Type: Article

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