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Benzothiophene inhibitors of MK2. Part 2: improvements in kinase selectivity and cell potency
David R Anderson1, Marvin J Meyers, Ravi G Kurumbail
1Pfizer Global Research and Development, St Louis Laboratories, Chesterfield, MO 63017, USA. david.r.anderson@pfizer.com
Bioorganic & Medicinal Chemistry Letters
|July 21, 2009
Abstract:
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.

