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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.

    Wu JP, Wang J, Abeywardane A, Andersen D, Emmanuel M, Gautschi E, Goldberg DR, Kashem MA, Lukas S, Mao W, Martin L, Morwick T, Moss N, Pargellis C, Patel UR, Patnaude L, Peet GW, Skow D, Snow RJ, Ward Y, Werneburg B, White A.

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

    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 [PubMed - indexed for MEDLINE]

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