1152829-97-4Relevant 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)
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
PYRROLCARBOXAMIDE DERIVATIVES FOR THE INHBITION OF ERK5
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, (2016/04/09)
The invention provides compounds of formula (I) or a tautomer, stereoisomer, N-oxide, pharmaceutically acceptable salt or solvate thereof. The compounds are useful for the prophylaxis or treatment of a disease state or condition mediated by ERK5, in particular cancers.
The discovery and initial optimisation of pyrrole-2-carboxamides as inhibitors of p38α MAP kinase
Down, Kenneth,Bamborough, Paul,Alder, Catherine,Campbell, Amanda,Christopher, John A.,Gerelle, Maria,Ludbrook, Steve,Mallett, Dave,Mellor, Geoff,Miller, David D.,Pearson, Rosannah,Ray, Keith,Solanke, Yemisi,Somers, Don
scheme or table, p. 3936 - 3940 (2010/08/19)
A novel pyrrole-2-carboxamide series of p38α inhibitors, discovered through the application of virtual screening, is presented. Following evaluation of activity, selectivity and developability properties of commercially available analogues, a synthesis program enabled rapid assessment of the series' suitability for further lead optimisation studies.
