Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N- (tetrahydro-2H-pyran-4-yl)benzamide (GW788388): A potent, selective, and orally active transforming growth factor-β type I receptor inhibitor

Journal of Medicinal Chemistry

Volumn 49, Issue 7, 2006, Pages 2210-2221

  Gellibert, Françoise ^a   De Gouville, Anne Charlotte ^a   Woolven, James ^b   Mathews, Neil ^b,d   Nguyen, Van Loc ^a   Bertho Ruault, Cécile ^a   Patikis, Angela ^b   Grygielko, Eugene T ^c   Laping, Nicholas J ^c   Huet, Stéphane ^a  

^a GLAXOSMITHKLINE   (France)

^b GLAXOSMITHKLINE   (United Kingdom)

^c GLAXOSMITHKLINE   (United States)

^d Arrow Therapeutics   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

4 [4 [3 (PYRIDIN 2 YL) 1H PYRAZOL 4 YL]PYRIDIN 2 YL] N (TETRAHYDRO 2H PYRAN 4 YL)BENZAMIDE; COLLAGEN TYPE 1; DIMETHYLNITROSAMINE; GW 788388; MESSENGER RNA; PUROMYCIN AMINONUCLEOSIDE; RECEPTOR BLOCKING AGENT; TRANSFORMING GROWTH FACTOR BETA RECEPTOR 1; TRANSFORMING GROWTH FACTOR BETA RECEPTOR 1 BLOCKING AGENT; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; ARTICLE; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG ELIMINATION; DRUG HALF LIFE; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG STRUCTURE; DRUG SYNTHESIS; EXTRACELLULAR MATRIX; HUMAN; HUMAN CELL; KIDNEY FIBROSIS; LIVER FIBROSIS; LUNG FIBROSIS; MALE; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION;

ACTIVIN RECEPTORS, TYPE I; ACUTE DISEASE; ADMINISTRATION, ORAL; ANIMALS; BENZAMIDES; COLLAGEN TYPE I; DIMETHYLNITROSAMINE; FIBROSIS; KIDNEY; LIVER CIRRHOSIS; MALE; MODELS, MOLECULAR; PUROMYCIN AMINONUCLEOSIDE; PYRAZOLES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, TRANSFORMING GROWTH FACTOR BETA; RNA, MESSENGER; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 33645665682     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm0509905     Document Type: Article

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