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Bioorg Med Chem Lett. 2007 Aug 15;17(16):4664-9. Epub 2007 Jun 7.

The discovery of carboline analogs as potent MAPKAP-K2 inhibitors.

Author information

1
Research and Development, Boehringer-Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, USA. jwu@rdg.boehringer-ingelheim.com

Abstract

The discovery of a series of potent, carboline-based MK2 inhibitors is described. These compounds inhibit MK2 with IC50s as low as 10 nM, as measured in a DELFIA assay. An X-ray crystal structure reveals that they bind in a region near the p-loop and the hinge region of MK2a.

PMID:
17576063
DOI:
10.1016/j.bmcl.2007.05.101
[Indexed for MEDLINE]

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