3qup | pdb_00003qup

Inhibitor bound structure of the kinase domain of the murine receptor tyrosine kinase TYRO3 (Sky)

spinqualitylabelsall models 3qup, resolution 1.90Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 3qup is a 1 chain structure with sequence from Mus musculus. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: LUN Gene: Tyro3, Dtk, Rse (Mus musculus) Activity: Receptor protein-tyrosine kinase, with EC number 2.7.10.1 Resources: FirstGlance, OCA, RCSB, PDBsum Publication Abstract from PubMed We report the discovery of a novel series of spiroindoline-based inhibitors of Sky kinase that bind in the ATP-binding site and exhibit high levels of kinome selectivity through filling the Ala571-subpocket. These inhibitors exhibit moderate oral bioavailability in the rat due to low absorption across the gut wall. Novel and selective spiroindoline-based inhibitors of sky kinase.,Powell NA, Kohrt JT, Filipski KJ, Kaufman M, Sheehan D, Edmunds JE, Delaney A, Wang Y, Bourbonais F, Lee DY, Schwende F, Sun F, McConnell P, Catana C, Chen H, Ohren J, Perrin LA Bioorg Med Chem Lett. 2011 Nov 16. PMID:22119469 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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