1148110-23-9Relevant articles and documents
Discovery of 6-aryl-7-alkoxyisoquinoline inhibitors of IκB kinase-β (IKK-β)
Christopher, John A.,Bamborough, Paul,Alder, Catherine,Campbell, Amanda,Cutler, Geoffrey J.,Down, Kenneth,Hamadi, Ahmed M.,Jolly, Adrian M.,Kerns, Jeffrey K.,Lucas, Fiona S.,Mellor, Geoffrey W.,Miller, David D.,Morse, Mary A.,Pancholi, Kiritkant D.,Rumsey, William,Solanke, Yemisi E.,Williamson, Rick
experimental part, p. 3098 - 3102 (2010/03/03)
The identification and progression of a potent and selective series of isoquinoline inhibitors of IκB kinase-β (IKK-β) are described. Hit-generation chemistry based on IKK-β 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-α.
