National Center for
3FYK: Crystal structure of a benzthiophene lead bound to MAPKAP Kinase-2 (MK-2)
Bioorg. Med. Chem. Lett. (2009) 19 p.4882-4884
Optimization of kinase selectivity for a set of benzothiophene MK2 inhibitors provided analogs with potencies of less than 500 nM in a cell based assay. The selectivity of the inhibitors can be rationalized by examination of X-ray crystal structures of inhibitors bound to MK2.