The Discovery of a Potent, Selective, and Peripherally Restricted Pan-Trk Inhibitor (PF-06273340) for the Treatment of Pain

Journal of Medicinal Chemistry

Volumn 59, Issue 22, 2016, Pages 10084-10099

  Skerratt, Sarah E ^a   Andrews, Mark ^b   Bagal, Sharan K ^a   Bilsland, James ^a   Brown, David ^b   Bungay, Peter J ^a   Cole, Susan ^b   Gibson, Karl R ^b   Jones, Russell ^b   Morao, Inaki ^b   Nedderman, Angus ^b   Omoto, Kiyoyuki ^a   Robinson, Colin ^b   Ryckmans, Thomas ^b   Skinner, Kimberly ^b   Stupple, Paul ^b   Waldron, Gareth ^a  

^a PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United States)

^b PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

N [5 [[2 AMINO 7 (2 HYDROXY 1,1 DIMETHYLETHYL) 7H PYRROLO[2,3 D]PYRIMIDIN 5 YL]CARBONYL]PYRIDIN 3 YL] 2 (5 CHLOROPYRIDIN 2 YL)ACETAMIDE; PHOSPHOTRANSFERASE INHIBITOR; UNCLASSIFIED DRUG; PF-06273340; PROTEIN KINASE; PROTEIN KINASE INHIBITOR; PYRIMIDINE DERIVATIVE; PYRROLE DERIVATIVE; TROPOMYOSIN KINASE;

ARTICLE; CHRONIC PAIN; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG CYTOTOXICITY; DRUG EFFICACY; DRUG POTENCY; DRUG SAFETY; DRUG SELECTIVITY; DRUG SOLUBILITY; DRUG SYNTHESIS; DRUG TOLERABILITY; ENZYME INHIBITION; HEPG2 CELL LINE; HUMAN; HUMAN TISSUE; IC50; IN VITRO STUDY; IN VIVO STUDY; LIGAND BINDING; NONHUMAN; PROSPECTIVE STUDY; QUANTITATIVE STRUCTURE ACTIVITY RELATION; CHEMICAL STRUCTURE; CHEMISTRY; DOSE RESPONSE; DRUG DEVELOPMENT; METABOLISM; MOLECULAR MODEL; PAIN; SYNTHESIS;

DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; HUMANS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PAIN; PROTEIN KINASE INHIBITORS; PROTEIN KINASES; PYRIMIDINES; PYRROLES; QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84999723814     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.6b00850     Document Type: Article

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