15372-84-6Relevant academic research and scientific papers
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
High-Throughput Screening and Hit Validation of Extracellular-Related Kinase 5 (ERK5) Inhibitors
Myers, Stephanie M.,Bawn, Ruth H.,Bisset, Louise C.,Blackburn, Timothy J.,Cottyn, Betty,Molyneux, Lauren,Wong, Ai-Ching,Cano, Celine,Clegg, William,Harrington, Ross. W.,Leung, Hing,Rigoreau, Laurent,Vidot, Sandrine,Golding, Bernard T.,Griffin, Roger J.,Hammonds, Tim,Newell, David R.,Hardcastle, Ian R.
, p. 444 - 455 (2016/08/16)
The extracellular-related kinase 5 (ERK5) is a promising target for cancer therapy. A high-throughput screen was developed for ERK5, based on the IMAP FP progressive binding system, and used to identify hits from a library of 57-617 compounds. Four distinct chemical series were evident within the screening hits. Resynthesis and reassay of the hits demonstrated that one series did not return active compounds, whereas three series returned active hits. Structure-activity studies demonstrated that the 4-benzoylpyrrole-2-carboxamide pharmacophore had excellent potential for further development. The minimum kinase binding pharmacophore was identified, and key examples demonstrated good selectivity for ERK5 over p38α kinase.
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
