2hk5

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Image:2hk5.gif

2hk5, resolution 2.0Å

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Hck Kinase in Complex with Lck targetted Inhibitor PG-1009247

Overview

This communication details the synthesis, biological activity, and binding, mode of a novel class of 2-benzimidazole substituted pyrimidines. The most, potent analogs disclosed showed low nanomolar activity for the inhibition, of Lck kinase and a representative analog was co-crystallized with Hck (a, structurally related member of the Src family kinases).

About this Structure

2HK5 is a Single protein structure of sequence from Homo sapiens with 1BM as ligand. Active as Non-specific protein-tyrosine kinase, with EC number 2.7.10.2 Full crystallographic information is available from OCA.

Reference

The development of 2-benzimidazole substituted pyrimidine based inhibitors of lymphocyte specific kinase (Lck)., Sabat M, VanRens JC, Laufersweiler MJ, Brugel TA, Maier J, Golebiowski A, De B, Easwaran V, Hsieh LC, Walter RL, Mekel MJ, Evdokimov A, Janusz MJ, Bioorg Med Chem Lett. 2006 Dec 1;16(23):5973-7. Epub 2006 Sep 25. PMID:16997556

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