| Literature DB >> 21429745 |
David D Miller1, Paul Bamborough, John A Christopher, Ian R Baldwin, Aurelie C Champigny, Geoffrey J Cutler, Jeffrey K Kerns, Timothy Longstaff, Geoffrey W Mellor, James V Morey, Mary A Morse, Hong Nie, William L Rumsey, John J Taggart.
Abstract
The discovery and hit-to-lead exploration of a novel series of selective IKK-β kinase inhibitors is described. The initial lead fragment 3 was identified by pharmacophore-directed virtual screening. Homology model-driven SAR exploration of the template led to potent inhibitors, such as 12, which demonstrate efficacy in cellular assays and possess encouraging developability profiles.Entities:
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Year: 2011 PMID： 21429745 DOI： 10.1016/j.bmcl.2011.02.107
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823