| Literature DB >> 17502144 |
John A Christopher1, 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.
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.Entities:
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Year: 2007 PMID： 17502144 DOI： 10.1016/j.bmcl.2007.04.088
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823