%0 Journal Article %A Sawyer, J. Scott %A Anderson, Bryan D. %A Beight, Douglas W. %A Campbell, Robert M. %A Jones, Michael L. %A Herron, David K. %A Lampe, John W. %A McCowan, Jefferson R. %A McMillen, William T. %A Mort, Nicholas %A Parsons, Stephen %A Smith, Edward C. R. %A Vieth, Michal %A Weir, Leonard C. %A Yan, Lei %A Zhang, Faming %A Yingling, Jonathan M. %D 2003 %T Synthesis and Activity of New Aryl- and Heteroaryl-Substituted Pyrazole Inhibitors of the Transforming Growth Factor-β Type I Receptor Kinase Domain %U 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 %R 10.1021/jm0205705.s001 %2 https://acs.figshare.com/ndownloader/files/5771103 %K p 38 MAP kinase %K T βR receptor kinase domain %K T βR %K SAR %K binding mode %K New Aryl %K receptor kinase domain %K inhibitor %X 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. %I ACS Publications