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. 2007 Jul 15;17(14):3972-7.
doi: 10.1016/j.bmcl.2007.04.088. Epub 2007 Apr 29.

The discovery of 2-amino-3,5-diarylbenzamide inhibitors of IKK-alpha and IKK-beta kinases

John A Christopher  1 , Barbara G Avitabile, Paul Bamborough, Aurelie C Champigny, Geoffrey J Cutler, Susan L Dyos, Ken G Grace, Jeffrey K Kerns, Jeremy D Kitson, Geoffrey W Mellor, James V Morey, Mary A Morse, Carolyn F O'Malley, Champa B Patel, Nicholas Probst, William Rumsey, Clive A Smith, Michael J Wilson
Affiliations

The discovery of 2-amino-3,5-diarylbenzamide inhibitors of IKK-alpha and IKK-beta kinases

John A Christopher et al. Bioorg Med Chem Lett. .

Abstract

A potent and selective series of 2-amino-3,5-diarylbenzamide inhibitors of IKK-alpha and IKK-beta is described. The most potent compounds are 8h, 8r and 8v, with IKK-beta inhibitory potencies of pIC(50) 7.0, 6.8 and 6.8, respectively. The series has excellent selectivity, both within the IKK family over IKK-epsilon, and across a wide variety of kinase assays. The potency of 8h in the IKK-beta enzyme assay translates to significant cellular activity (pIC(50) 5.7-6.1) in assays of functional and mechanistic relevance.

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