3bx5
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Revision as of 20:13, 16 April 2008
P38 alpha map kinase complexed with BMS-640994
Overview
A novel structural class of p38alpha MAP kinase inhibitors has been identified via iterative SAR studies of a focused deck screen hit. Optimization of the lead series generated 6e, BMS-640994, a potent and selective p38alpha inhibitor that is orally efficacious in rodent models of acute and chronic inflammation.
About this Structure
3BX5 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitor., Hynes J Jr, Wu H, Pitt S, Shen DR, Zhang R, Schieven GL, Gillooly KM, Shuster DJ, Taylor TL, Yang X, McIntyre KW, McKinnon M, Zhang H, Marathe PH, Doweyko AM, Kish K, Kiefer SE, Sack JS, Newitt JA, Barrish JC, Dodd J, Leftheris K, Bioorg Med Chem Lett. 2008 Mar 15;18(6):1762-7. Epub 2008 Feb 16. PMID:18313298 Page seeded by OCA on Wed Apr 16 23:13:14 2008
