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Bioorg Med Chem Lett. 2009 Aug 15;19(16):4882-4. doi: 10.1016/j.bmcl.2009.02.017. Epub 2009 Feb 8.

Benzothiophene inhibitors of MK2. Part 2: improvements in kinase selectivity and cell potency.

Author information

1
Pfizer Global Research and Development, St Louis Laboratories, Chesterfield, MO 63017, USA. david.r.anderson@pfizer.com

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.

PMID:
19616942
DOI:
10.1016/j.bmcl.2009.02.017
[Indexed for MEDLINE]

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