4px6 | pdb_00004px6

SYK catalytic domain in complex with a potent pyridopyrimidinone inhibitor

spinqualitylabelsall models 4px6, resolution 1.60Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 4px6 is a 1 chain structure with sequence from Human. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: 2X6 Activity: Non-specific protein-tyrosine kinase, with EC number 2.7.10.2 Resources: FirstGlance, OCA, RCSB, PDBsum Publication Abstract from PubMed We describe two series of Syk inhibitors which potently abrogate Syk kinase function in enzymatic assays, cellular assays and in primary cells in the presence of blood. Introduction of a 7-aminoindole substituent led to derivatives with good kinase selectivity and little or no hERG channel inhibition (3b, 10c). Syk inhibitors with high potency in presence of blood.,Thoma G, Blanz J, Buhlmayer P, Druckes P, Kittelmann M, Smith AB, van Eis M, Vangrevelinghe E, Zerwes HG, Che JJ, He X, Jin Y, Lee CC, Michellys PY, Uno T, Liu H Bioorg Med Chem Lett. 2014 Apr 3. pii: S0960-894X(14)00302-3. doi:, 10.1016/j.bmcl.2014.03.075. PMID:24726806 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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