15372-84-6Relevant articles and documents
Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38α and BRD4
Myers, Stephanie M.,Miller, Duncan C.,Molyneux, Lauren,Arasta, Mercedes,Bawn, Ruth H.,Blackburn, Timothy J.,Cook, Simon J.,Edwards, Noel,Endicott, Jane A.,Golding, Bernard T.,Griffin, Roger J.,Hammonds, Tim,Hardcastle, Ian R.,Harnor, Suzannah J.,Heptinstall, Amy B.,Lochhead, Pamela A.,Martin, Mathew P.,Martin, Nick C.,Newell, David R.,Owen, Paul J.,Pang, Leon C.,Reuillon, Tristan,Rigoreau, Laurent J.M.,Thomas, Huw D.,Tucker, Julie A.,Wang, Lan-Zhen,Wong, Ai-Ching,Noble, Martin E.M.,Wedge, Stephen R.,Cano, Celine
, p. 530 - 543 (2019/06/19)
Extracellular regulated kinase 5 (ERK5) signalling has been implicated in driving a number of cellular phenotypes including endothelial cell angiogenesis and tumour cell motility. Novel ERK5 inhibitors were identified using high throughput screening, with
2-Aminobenzimidazoles as potent ITK antagonists: de novo design of a pyrrole system targeting additional hydrogen bonding interaction
Lo, Ho Yin,Bentzien, J?rg,White, Andre,Man, Chuk C.,Fleck, Roman W.,Pullen, Steven S.,Khine, Hnin Hnin,King, Josephine,Woska Jr., Joseph R.,Wolak, John P.,Kashem, Mohammed A.,Roth, Gregory P.,Takahashi, Hidenori
experimental part, p. 7337 - 7340 (2009/04/14)
Based on information from molecular modeling, a series of 2-aminobenzimidazoles with pyrrole moieties were designed and synthesized as ITK antagonists. Results showed that a significant improvement of intrinsic and cell-based potency was achieved. X-ray c