Discovery and optimization of indazoles as potent and selective interleukin-2 inducible T cell kinase (ITK) inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 24, Issue 11, 2014, Pages 2448-2452

  Pastor, Richard M ^a   Burch, Jason D ^a   Magnuson, Steven ^a   Ortwine, Daniel F ^a   Chen, Yuan ^a   De La Torre, Kelly ^a   Ding, Xiao ^a   Eigenbrot, Charles ^a   Johnson, Adam ^a   Liimatta, Marya ^a   Liu, Yichin ^a   Shia, Steven ^a   Wang, Xiaolu ^a   Wu, Lawren C ^a   Pei, Zhonghua ^a  

^a GENENTECH INC   (United States)

Author keywords

Indazole; ITK; SBDD; X ray crystallography; stacking

Indexed keywords

INDAZOLE DERIVATIVE; INTERLEUKIN 2 INDUCIBLE T CELL KINASE; PROTEIN TYROSINE KINASE; UNCLASSIFIED DRUG; EMT PROTEIN-TYROSINE KINASE; PROTEIN KINASE INHIBITOR;

ARTICLE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG BINDING; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DESIGN; DRUG INHIBITION; DRUG PENETRATION; DRUG POTENCY; DRUG SELECTIVITY; ENZYME ACTIVITY; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; PROCESS OPTIMIZATION; SCANNING ELECTRON MICROSCOPY; STRUCTURE ACTIVITY RELATION; X RAY CRYSTALLOGRAPHY; ANTAGONISTS AND INHIBITORS; CHEMICAL STRUCTURE; CHEMISTRY; DOSE RESPONSE; DRUG DEVELOPMENT; JURKAT CELL LINE; METABOLISM; SYNTHESIS;

CRYSTALLOGRAPHY, X-RAY; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; HUMANS; INDAZOLES; JURKAT CELLS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PROTEIN KINASE INHIBITORS; PROTEIN-TYROSINE KINASES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84899989274     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2014.04.023     Document Type: Article

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