Document Report Card

ID: ALA1138455

Journal: J Med Chem

Title: Discovery of 6-aryl-7-alkoxyisoquinoline inhibitors of IkappaB kinase-beta (IKK-beta).

Authors: Christopher JA, Bamborough P, Alder C, Campbell A, Cutler GJ, Down K, Hamadi AM, Jolly AM, Kerns JK, Lucas FS, Mellor GW, Miller DD, Morse MA, Pancholi KD, Rumsey W, Solanke YE, Williamson R.

Abstract: The identification and progression of a potent and selective series of isoquinoline inhibitors of IkappaB kinase-beta (IKK-beta) are described. Hit-generation chemistry based on IKK-beta active-site knowledge yielded a weakly potent but tractable chemotype that was rapidly progressed into a series with robust enzyme and cellular activity and significant selectivity over IKK-alpha.

CiteXplore: 19348415

DOI: 10.1021/jm9000117