Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans

Journal of Medicinal Chemistry

Volumn 60, Issue 5, 2017, Pages 1971-1993

  Thorarensen, Atli ^a   Dowty, Martin E ^a   Banker, Mary Ellen ^a   Juba, Brian ^a   Jussif, Jason ^a   Lin, Tsung ^a   Vincent, Fabien ^a   Czerwinski, Robert M ^a   Casimiro Garcia, Agustin ^a   Unwalla, Ray ^a   Trujillo, John I ^a   Liang, Sidney ^a   Balbo, Paul ^a   Che, Ye ^a   Gilbert, Adam M ^a   Brown, Matthew F ^a   Hayward, Matthew ^a   Montgomery, Justin ^a   Leung, Louis ^a   Yang, Xin ^a   Soucy, Sarah ^a   Hegen, Martin ^a   Coe, Jotham ^a   Langille, Jonathan ^a   Vajdos, Felix ^a   Chrencik, Jill ^a   Telliez, Jean Baptiste ^a   more..

^a PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 [(7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)OCTAHYDRO 6H PYRROLO[2,3 C]PYRIDIN 6 YL]ETHAN 1 ONE; 1 [(7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)OCTAHYDRO 6H PYRROLO[2,3 C]PYRIDIN 6 YL]PROP 2 EN 1 ONE; 1 [3 [(7H PYRROLO[2,3 D]PYRIMIDIN 4 YL) AMINO]PIPERIDIN 1 YL]BUT 2 EN 1 ONE; 1 [3 [(7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)AMINO]PIPERIDIN 1 YL]PROP 2 EN 1 ONE; 1 [3 [METHYL(7H PYRROLO[2,3 D]PYRIMIDIN 4- YL)AMINO]PIPERIDIN 1 YL]PROP 2 EN 1 ONE; 1 [4 METHYL 3 [METHYL (7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)AMINO]PIPERIDIN 1 YL]PROP 2 EN 1 ONE; 2 METHYL 5 [(7H PYRROLO[2,3 D]PYRIMIDIN 4 YLAMINO)PIPERIDIN 1 YL]PROP 2 EN 1 ONE; 3 METHYL 5 [(7H PYRROLO[2,3 D]PYRIMIDIN 4 YLAMINO)PIPERIDIN 1 YL]PROP 2 EN 1 ONE; 3 [(7H PYRROL[2,3 D]PYRIMIDIN 4 YL)AMINO] 2 METHYLPIPERIDIN 1 YL]PROP 2 EN 1 ONE; 3 [[(7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)AMINO] 4 METHYLPIPERIDIN 1 YL]PROP 2 EN 1 ONE; 3 [[(7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)AMINO] 5 METHYLPIPERIDIN 1 YL]PROP 2 EN 1 ONE; 5 [(7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)AMINO] 2 METHYL PIPERIDIN 1 YL]PROP 2 EN 1 ONE; 5 [(7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)AMINO] 2 METHYLPIPERIDIN 1 YL]PROP 2 EN 1 ONE; INTERLEUKIN 15; JANUS KINASE 3; JANUS KINASE 3 INHIBITOR; N [3 (7H PYRROLO[2,3 D]PYRIMIDIN 4 YL)PHENYL]ACRYLAMIDE; PF 06651600; STAT5 PROTEIN; UNCLASSIFIED DRUG; PF-06651600; PROTEIN KINASE INHIBITOR; PYRIMIDINE DERIVATIVE; PYRROLE DERIVATIVE;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CIS ISOMER; CONTROLLED STUDY; COVALENT BOND; CRYSTAL STRUCTURE; DELAYED HYPERSENSITIVITY; DIASTEREOISOMER; DRUG CLEARANCE; DRUG CONFORMATION; DRUG DESIGN; DRUG EFFICACY; DRUG EXPOSURE; DRUG POTENCY; DRUG SAFETY; DRUG SYNTHESIS; ELECTROPHILICITY; ENZYME INACTIVATION; ENZYME SPECIFICITY; HUMAN; HUMAN CELL; HUMAN TISSUE; HYDROGENATION; IC50; IN VIVO STUDY; LIVER MICROSOME; MALE; NONHUMAN; NUCLEOPHILICITY; PERIPHERAL BLOOD MONONUCLEAR CELL; PROTEIN INTERACTION; PROTEIN PHOSPHORYLATION; RACEMIC MIXTURE; RAT; REACTION TIME; SHEEP ERYTHROCYTE; SIGNAL TRANSDUCTION; STEREOCHEMISTRY; SUZUKI REACTION; T LYMPHOCYTE; X RAY CRYSTALLOGRAPHY; ANTAGONISTS AND INHIBITORS; CHEMISTRY; DRUG EFFECTS; METABOLISM; ORAL DRUG ADMINISTRATION;

ADMINISTRATION, ORAL; DRUG DESIGN; HUMANS; JANUS KINASE 3; PROTEIN KINASE INHIBITORS; PYRIMIDINES; PYRROLES; SIGNAL TRANSDUCTION;

EID: 85015195636     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.6b01694     Document Type: Article

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