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3fyk

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3fyk, resolution 3.50Å ()
Ligands:
Gene: MAPKAP-2, MAPKAPK2 (Homo sapiens)
Activity: Non-specific serine/threonine protein kinase, with EC number 2.7.11.1
Related: 3fyj, 2p3g
Resources: FirstGlance, OCA, PDBsum, RCSB
Coordinates: save as pdb, mmCIF, xml



Contents

Crystal structure of a benzthiophene lead bound to MAPKAP Kinase-2 (MK-2)

Publication Abstract from PubMed

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.

Benzothiophene inhibitors of MK2. Part 2: improvements in kinase selectivity and cell potency., Anderson DR, Meyers MJ, Kurumbail RG, Caspers N, Poda GI, Long SA, Pierce BS, Mahoney MW, Mourey RJ, Parikh MD, Bioorg Med Chem Lett. 2009 Aug 15;19(16):4882-4. Epub 2009 Feb 8. PMID:19616942

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

About this Structure

3fyk is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA.

See Also

Reference

  • Anderson DR, Meyers MJ, Kurumbail RG, Caspers N, Poda GI, Long SA, Pierce BS, Mahoney MW, Mourey RJ, Parikh MD. Benzothiophene inhibitors of MK2. Part 2: improvements in kinase selectivity and cell potency. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4882-4. Epub 2009 Feb 8. PMID:19616942 doi:10.1016/j.bmcl.2009.02.017

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