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High-throughput screening and hit validation of extracellular-related kinase 5 (ERK5) inhibitors

Lookup NU author(s): Stephanie Myers, Dr Ruth Bawn, Betty Cottyn, Dr Lauren Molyneux, Dr Celine Cano, Emeritus Professor Bill Clegg, Dr Ross Harrington, Dr Laurent Rigoreau, Dr Sandrine Vidot, Professor Bernard Golding, Professor Roger Griffin, Emeritus Professor Herbie Newell, Dr Ian Hardcastle



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.

Publication metadata

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


DOI: 10.1021/acscombsci.5b00155


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