Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain.
Article Details
- CitationCopy to clipboard
Sawyer JS, Anderson BD, Beight DW, Campbell RM, Jones ML, Herron DK, Lampe JW, McCowan JR, McMillen WT, Mort N, Parsons S, Smith EC, Vieth M, Weir LC, Yan L, Zhang F, Yingling JM
Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain.
J Med Chem. 2003 Sep 11;46(19):3953-6.
- PubMed ID
- 12954047 [ View in PubMed]
- Abstract
Pyrazole-based inhibitors of the transforming growth factor-beta type I receptor kinase domain (TbetaR-I) are described. Examination of the SAR in both enzyme- and cell-based in vitro assays resulted in the emergence of two subseries featuring differing selectivity versus p38 MAP kinase. A common binding mode at the active site has been established by successful cocrystallization and X-ray analysis of potent inhibitors with the TbetaR-I receptor kinase domain.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) 4-(3-Pyridin-2-Yl-1h-Pyrazol-4-Yl)Quinoline TGF-beta receptor type-1 IC 50 (nM) 47 N/A N/A Details 4-(3-Pyridin-2-Yl-1h-Pyrazol-4-Yl)Quinoline TGF-beta receptor type-1 IC 50 (nM) 51 N/A N/A Details 4-(3-Pyridin-2-Yl-1h-Pyrazol-4-Yl)Quinoline TGF-beta receptor type-1 IC 50 (nM) 89 N/A N/A Details