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. 2006 Dec 15;16(24):6236-40.
doi: 10.1016/j.bmcl.2006.09.018. Epub 2006 Sep 25.

5-(1H-Benzimidazol-1-yl)-3-alkoxy-2-thiophenecarbonitriles as potent, selective, inhibitors of IKK-epsilon kinase

Paul Bamborough  1 , John A Christopher, Geoffrey J Cutler, Marion C Dickson, Geoffrey W Mellor, James V Morey, Champa B Patel, Lisa M Shewchuk
Affiliations

5-(1H-Benzimidazol-1-yl)-3-alkoxy-2-thiophenecarbonitriles as potent, selective, inhibitors of IKK-epsilon kinase

Paul Bamborough et al. Bioorg Med Chem Lett. .

Abstract

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.

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