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2i40
From Proteopedia
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(New page: 200px<br /> <applet load="2i40" size="450" color="white" frame="true" align="right" spinBox="true" caption="2i40, resolution 2.80Å" /> '''Cdk2/Cyclin A compl...)
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Revision as of 20:34, 12 November 2007
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Cdk2/Cyclin A complexed with a thiophene carboxamide inhibitor
Overview
The identification and hit-to-lead exploration of a novel, potent and, selective series of substituted benzimidazole-thiophene carbonitrile, inhibitors of IKK-epsilon kinase is described. Compound 12e was identified, with an IKK-epsilon enzyme potency of pIC(50) 7.4, and has a highly, encouraging wider selectivity profile, including selectivity within the, IKK kinase family.
About this Structure
2I40 is a Protein complex structure of sequences from Homo sapiens with BLZ as ligand. Active as Cyclin-dependent kinase, with EC number 2.7.11.22 Full crystallographic information is available from OCA.
Reference
5-(1H-Benzimidazol-1-yl)-3-alkoxy-2-thiophenecarbonitriles as potent, selective, inhibitors of IKK-epsilon kinase., Bamborough P, Christopher JA, Cutler GJ, Dickson MC, Mellor GW, Morey JV, Patel CB, Shewchuk LM, Bioorg Med Chem Lett. 2006 Dec 15;16(24):6236-40. Epub 2006 Sep 25. PMID:16997559
Page seeded by OCA on Mon Nov 12 22:40:31 2007
