3bv2 | pdb_00003bv2
Morpholino pyrrolotriazine P38 Alpha map kinase inhibitor compound 30
Overview
A novel series of compounds based on the pyrrolo[2,1-f][1,2,4]triazine ring system have been identified as potent p38alpha MAP kinase inhibitors. The synthesis, structure-activity relationships (SAR), and in vivo activity of selected analogs from this class of inhibitors are reported. Additional studies based on X-ray co-crystallography have revealed that one of the potent inhibitors from this series binds to the DFG-out conformation of the p38alpha enzyme.
About this Structure
3BV2 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
Synthesis and SAR of new pyrrolo[2,1-f][1,2,4]triazines as potent p38alpha MAP kinase inhibitors., Wrobleski ST, Lin S, Hynes J Jr, Wu H, Pitt S, Shen DR, Zhang R, Gillooly KM, Shuster DJ, McIntyre KW, Doweyko AM, Kish KF, Tredup JA, Duke GJ, Sack JS, McKinnon M, Dodd J, Barrish JC, Schieven GL, Leftheris K, Bioorg Med Chem Lett. 2008 Mar 4;. PMID:18364256
