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Lookup NU author(s): Stephanie Myers, Dr Ruth Bawn, Betty Cottyn, Dr Lauren Molyneux, Dr Celine CanoORCiD, Emeritus Professor Bill CleggORCiD, Dr Ross Harrington, Dr Laurent Rigoreau, Dr Sandrine Vidot, Emeritus Professor Bernard Golding, Professor Roger Griffin, Professor Herbie Newell, Dr Ian HardcastleORCiD
This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License (CC BY-NC 4.0).
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 re-assay of the hits demonstrated that one series did not return active compounds, whereas three series returned active hits. The series based on a 4-benzoylpyrrole-2-carboxamide pharmacophore was selected for further investigation. Structure-activity studies established the minimum kinase binding pharmacophore, and key examples demonstrated good selectivity for ERK5 over p38alpha kinase.
Author(s): Myers SM, Bawn RH, Bisset LC, Blackburn TJ, Cottyn B, Molyneux L, Wong AC, Cano C, Clegg W, Harrington RW, Leung H, Rigoreau L, Vidot S, Golding BT, Griffin RJ, Hammonds T, Newell DR, Hardcastle IR
Publication type: Article
Publication status: Published
Journal: ACS Combinatorial Science
Year: 2016
Volume: 18
Issue: 8
Pages: 444-455
Print publication date: 08/08/2016
Online publication date: 11/07/2016
Acceptance date: 06/07/2016
Date deposited: 12/07/2016
ISSN (print): 2156-8952
ISSN (electronic): 2156-8944
Publisher: American Chemical Society
URL: http://dx.doi.org/10.1021/acscombsci.5b00155
DOI: 10.1021/acscombsci.5b00155
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