10.1021/jm0205705.s001 J. Scott Sawyer J. Scott Sawyer Bryan D. Anderson Bryan D. Anderson Douglas W. Beight Douglas W. Beight Robert M. Campbell Robert M. Campbell Michael L. Jones Michael L. Jones David K. Herron David K. Herron John W. Lampe John W. Lampe Jefferson R. McCowan Jefferson R. McCowan William T. McMillen William T. McMillen Nicholas Mort Nicholas Mort Stephen Parsons Stephen Parsons Edward C. R. Smith Edward C. R. Smith Michal Vieth Michal Vieth Leonard C. Weir Leonard C. Weir Lei Yan Lei Yan Faming Zhang Faming Zhang Jonathan M. Yingling Jonathan M. Yingling Synthesis and Activity of New Aryl- and Heteroaryl-Substituted Pyrazole Inhibitors of the Transforming Growth Factor-β Type I Receptor Kinase Domain American Chemical Society 2003 p 38 MAP kinase T βR receptor kinase domain T βR SAR binding mode New Aryl receptor kinase domain inhibitor 2003-08-12 00:00:00 Journal contribution 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.