Discovery of VX-509 (Decernotinib): A Potent and Selective Janus Kinase 3 Inhibitor for the Treatment of Autoimmune Diseases

Journal of Medicinal Chemistry

Volumn 58, Issue 18, 2015, Pages 7195-7216

  Farmer, Luc J ^a   Ledeboer, Mark W ^a   Hoock, Thomas ^a   Arnost, Michael J ^a   Bethiel, Randy S ^a   Bennani, Youssef L ^a   Black, James J ^a   Brummel, Christopher L ^a   Chakilam, Ananthsrinivas ^a   Dorsch, Warren A ^a   Fan, Bin ^a   Cochran, John E ^a   Halas, Summer ^a   Harrington, Edmund M ^a   Hogan, James K ^a   Howe, David ^a   Huang, Hui ^a   Jacobs, Dylan H ^a   Laitinen, Leena M ^a   Liao, Shengkai ^a   Mahajan, Sudipta ^a   Marone, Valerie ^a   Martinez Botella, Gabriel ^a   McCarthy, Pamela ^a   Messersmith, David ^a   Namchuk, Mark ^a   Oh, Luke ^a   Penney, Marina S ^a   Pierce, Albert C ^a   Raybuck, Scott A ^a   Rugg, Arthur ^a   Salituro, Francesco G ^a   Saxena, Kumkum ^a   Shannon, Dean ^a   Shlyakter, Dina ^a   Swenson, Lora ^a   Tian, Shi Kai ^a   Town, Christopher ^a   Wang, Jian ^a   Wang, Tiansheng ^a   Wannamaker, M Woods ^a   Winquist, Raymond J ^a   Zuccola, Harmon J ^a   more..

^a VERTEX PHARMACEUTICALS   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1H PYRROLO[2,3 B]PYRIDINE DERIVATIVE; CYCLOSPORIN A; DECERNOTINIB; INDOLE DERIVATIVE; JANUS KINASE 3; MOLECULAR SCAFFOLD; UNCLASSIFIED DRUG; 2-((2-(1H-PYRROLO(2,3-B)PYRIDIN-3-YL)PYRIMIDIN-4-YL)AMINO)-2-METHYL-N-(2,2,2-TRIFLUOROETHYL)BUTANAMIDE; FUSED HETEROCYCLIC RINGS; JANUS KINASE 2; VALINE;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; AUTOIMMUNE DISEASE; BEAGLE; BINDING AFFINITY; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG EFFICACY; DRUG POTENCY; DRUG SCREENING; DRUG SELECTIVITY; DRUG TARGETING; FEMALE; GRAFT VERSUS HOST REACTION; HUMAN; HUMAN CELL; HUMAN TISSUE; IMMUNOCOMPETENT CELL; IN VIVO STUDY; INTRACELLULAR SIGNALING; MALE; MOUSE; NONHUMAN; RAT; STEREOCHEMISTRY; ANALOGS AND DERIVATIVES; ANIMAL; ANTAGONISTS AND INHIBITORS; AUTOIMMUNE DISEASES; BAGG ALBINO MOUSE; CBA MOUSE; CELL LINE; CHEMICAL DATABASE; CHEMICAL STRUCTURE; CHEMISTRY; DOG; GRAFT VS HOST DISEASE; HAPLORHINI; IMMUNOLOGY; LEWIS RAT; LIVER MICROSOME; METABOLISM; SPRAGUE DAWLEY RAT; STEREOISOMERISM; STRUCTURE ACTIVITY RELATION;

ANIMALS; AUTOIMMUNE DISEASES; CELL LINE; DATABASES, CHEMICAL; DOGS; FEMALE; GRAFT VS HOST DISEASE; HAPLORHINI; HETEROCYCLIC COMPOUNDS, 2-RING; HUMANS; JANUS KINASE 2; JANUS KINASE 3; MALE; MICE; MICE, INBRED BALB C; MICE, INBRED CBA; MICROSOMES, LIVER; MODELS, MOLECULAR; RATS; RATS, INBRED LEW; RATS, SPRAGUE-DAWLEY; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; VALINE;

EID: 84942337457     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.5b00301     Document Type: Article

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