Synthesis and Activity of New Aryl- and Heteroaryl-Substituted Pyrazole Inhibitors of the Transforming Growth Factor-β Type I Receptor Kinase Domain J. Scott Sawyer Bryan D. Anderson Douglas W. Beight Robert M. Campbell Michael L. Jones David K. Herron John W. Lampe Jefferson R. McCowan William T. McMillen Nicholas Mort Stephen Parsons Edward C. R. Smith Michal Vieth Leonard C. Weir Lei Yan Faming Zhang Jonathan M. Yingling 10.1021/jm0205705.s001 https://acs.figshare.com/articles/journal_contribution/Synthesis_and_Activity_of_New_Aryl-_and_Heteroaryl-Substituted_Pyrazole_Inhibitors_of_the_Transforming_Growth_Factor-_Type_I_Receptor_Kinase_Domain/3681318 Pyrazole-based inhibitors of the transforming growth factor-β type I receptor kinase domain (TβR-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 TβR-I receptor kinase domain. 2003-08-12 00:00:00 p 38 MAP kinase T βR receptor kinase domain T βR SAR binding mode New Aryl receptor kinase domain inhibitor