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3b2w

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Revision as of 17:02, 21 February 2008 by OCA (Talk | contribs)
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Image:3b2w.jpg

3b2w, resolution 2.30Å

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Crystal structure of pyrimidine amide 11 bound to Lck

Overview

N-3-(Phenylcarbamoyl)arylpyrimidine-5-carboxamides are a novel class of selective Lck inhibitors. This series of compounds derives its selectivity from a hydrogen bond with the gatekeeper Thr316 of the enzyme. X-ray co-crystal structural data, structure-activity relationships, and the synthesis of these inhibitors are reported herein.

About this Structure

3B2W is a Single protein structure of sequence from Homo sapiens with as ligand. Active as Non-specific protein-tyrosine kinase, with EC number 2.7.10.2 Known structural/functional Site: . Full crystallographic information is available from OCA.

Reference

N-(3-(phenylcarbamoyl)arylpyrimidine)-5-carboxamides as potent and selective inhibitors of Lck: structure, synthesis and SAR., Deak HL, Newcomb JR, Nunes JJ, Boucher C, Cheng AC, DiMauro EF, Epstein LF, Gallant P, Hodous BL, Huang X, Lee JH, Patel VF, Schneider S, Turci SM, Zhu X, Bioorg Med Chem Lett. 2008 Feb 1;18(3):1172-6. Epub 2007 Dec 5. PMID:18083554

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