Structure-based drug design of RN486, a potent and selective Bruton's tyrosine kinase (BTK) inhibitor, for the treatment of rheumatoid arthritis

Journal of Medicinal Chemistry

Volumn 58, Issue 1, 2015, Pages 512-516

  Lou, Yan ^a   Han, Xiaochun ^a   Kuglstatter, Andreas ^a   Kondru, Rama K ^a   Sweeney, Zachary K ^a   Soth, Michael ^a   McIntosh, Joel ^a   Litman, Renee ^a   Suh, Judy ^a   Kocer, Buelent ^a   Davis, Dana ^a   Park, Jaehyeon ^a   Frauchiger, Sandra ^a   Dewdney, Nolan ^a   Zecic, Hasim ^a   Taygerly, Joshua P ^a   Sarma, Keshab ^a   Hong, Junbae ^a   Hill, Ronald J ^a   Gabriel, Tobias ^a   Goldstein, David M ^a   Owens, Timothy D ^a   more..

^a HOFFMANN LA ROCHE INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIRHEUMATIC AGENT; BENZYL ALCOHOL; BRUTON TYROSINE KINASE INHIBITOR; RN 486; UNCLASSIFIED DRUG; AGAMMAGLOBULINAEMIA TYROSINE KINASE; ISOQUINOLINE DERIVATIVE; PROTEIN BINDING; PROTEIN TYROSINE KINASE; RN486;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIINFLAMMATORY ACTIVITY; AREA UNDER THE CURVE; ARTICLE; CHEMICAL ANALYSIS; CHEMICAL REACTION; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG DESIGN; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; LIPOPHILICITY; NONHUMAN; PROCESS OPTIMIZATION; PROTEIN BINDING; RAT; RHEUMATOID ARTHRITIS; STRUCTURE ANALYSIS; SUBSTITUTION REACTION; ANTAGONISTS AND INHIBITORS; ARTHRITIS, RHEUMATOID; CHEMICAL MODEL; CHEMICAL STRUCTURE; CHEMISTRY; METABOLISM; PROTEIN SECONDARY STRUCTURE; PROTEIN TERTIARY STRUCTURE; X RAY CRYSTALLOGRAPHY;

ARTHRITIS, RHEUMATOID; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; HUMANS; ISOQUINOLINES; MODELS, CHEMICAL; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PROTEIN BINDING; PROTEIN STRUCTURE, SECONDARY; PROTEIN STRUCTURE, TERTIARY; PROTEIN-TYROSINE KINASES;

EID: 84920860916     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm500305p     Document Type: Article

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