Pyrazolopyridine inhibitors of B-RafV600E. Part 4: Rational design and kinase selectivity profile of cell potent type II inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 19, 2012, Pages 6237-6241

  Wenglowsky, Steve ^a   Moreno, David ^a   Laird, Ellen R ^a   Gloor, Susan L ^a   Ren, Li ^a   Risom, Tyler ^a   Rudolph, Joachim ^b   Sturgis, Hillary L ^a   Voegtli, Walter C ^a  

^a ARRAY BIOPHARMA INC   (United States)

^b GENENTECH INC   (United States)

Author keywords

B RafV600E; DFG out; Inactive conformation; Kinase selectivity; Structure based design

Indexed keywords

B RAF KINASE; B RAF KINASE INHIBITOR; MITOGEN ACTIVATED PROTEIN KINASE; PYRAZOLE DERIVATIVE; PYRIDINE DERIVATIVE;

ALPHA HELIX; ARTICLE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG CLEARANCE; DRUG DESIGN; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SELECTIVITY; DRUG SYNTHESIS; ENZYME CONFORMATION; ENZYME INHIBITION; HUMAN; IC 50; LIPOPHILICITY; MOUSE; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION;

ANIMALS; CRYSTALLOGRAPHY, X-RAY; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DESIGN; DRUG STABILITY; HUMANS; MICE; MICROSOMES; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PROTEIN KINASE INHIBITORS; PROTO-ONCOGENE PROTEINS B-RAF; PYRAZOLES; PYRIDINES; RATS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84866350285     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.08.007     Document Type: Article

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