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.