Evolution of the thienopyridine class of inhibitors of IκB kinase-β: part I: hit-to-lead strategies

…, K Catron, M DeTuri, J Emeigh, C Homon…

Index: Morwick, Tina; Berry, Angela; Brickwood, Janice; Cardozo, Mario; Catron, Katrina; DeTuri, Molly; Emeigh, Jonathan; Homon, Carol; Hrapchak, Matt; Jacober, Stephen; Jakes, Scott; Kaplita, Paul; Kelly, Terence A.; Ksiazek, John; Liuzzi, Michel; Magolda, Ronald; Mao, Can; Marshall, Daniel; McNeil, Daniel; Prokopowicz II, Anthony; Sarko, Christopher; Scouten, Erika; Sledziona, Cynthia; Sun, Sanxing; Watrous, Jane; Wu, Jiang Ping; Cywin, Charles L. Journal of Medicinal Chemistry, 2006 , vol. 49, # 10 p. 2898 - 2908

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Citation Number: 65

Abstract

High-throughput screening is routinely employed as a method for the identification of novel hit structures. Large numbers of active compounds are typically procured in this way and must undergo a rigorous validation process. This process is described in detail for a collection of screening hits identified as inhibitors of IκB kinase-β (IKKβ), a key regulatory enzyme in the nuclear factor-κB (NF-κB) pathway. From these studies, a promising hit ...