Sulfoximine-substituted trifluoromethylpyrimidine analogs as inhibitors of proline-rich tyrosine kinase 2 (PYK2) show reduced hERG activity

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 12, 2009, Pages 3253-3258

  Walker, Daniel P ^a   Zawistoski, Michael P ^a   McGlynn, Molly A ^a   Li, Jian Cheng ^a   Kung, Daniel W ^a   Bonnette, Peter C ^a   Baumann, Amy ^a   Buckbinder, Leonard ^a   Houser, Janet A ^a   Boer, Jason ^a   Mistry, Anil ^a   Han, Seungil ^a   Guzman Perez, Li Xing and Angel ^a  

^a PFIZER INC   (United States)

Author keywords

FAK; hERG; Kinase; Osteoporosis; PYK2; Sulfoximine

Indexed keywords

DOFETILIDE; FLUORINE DERIVATIVE; FOCAL ADHESION KINASE; FOCAL ADHESION KINASE 2; IMINE; METHYL GROUP; N METHYLSULFOXIMINE; PF 431396; POTASSIUM CHANNEL HERG; PYRIMIDINE DERIVATIVE; SULFONE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CRYSTAL STRUCTURE; DISTRIBUTION VOLUME; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG HALF LIFE; DRUG METABOLISM; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SAFETY; DRUG SELECTIVITY; DRUG SYNTHESIS; IN VITRO STUDY; IN VIVO STUDY; NONHUMAN; OSTEOPOROSIS; PATCH CLAMP; RAT; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; ANIMALS; DRUG EVALUATION, PRECLINICAL; ENZYME INHIBITORS; ETHER-A-GO-GO POTASSIUM CHANNELS; FOCAL ADHESION KINASE 2; HUMANS; IMINES; OSTEOPOROSIS; PATCH-CLAMP TECHNIQUES; PHENETHYLAMINES; PYRIMIDINES; RATS; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONAMIDES; SULFONES;

RATTUS;

EID: 65749102118     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.04.093     Document Type: Article

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