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High-Throughput Screening and Hit Validation of Extracellular-Related Kinase 5 (ERK5) Inhibitors

Myers, Stephanie, 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. and Hardcastle, Ian R. (2016) High-Throughput Screening and Hit Validation of Extracellular-Related Kinase 5 (ERK5) Inhibitors. ACS Combinatorial Science, 18 (8). pp. 444-455. ISSN 2156-8952

Item Type: Article


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.

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Depositing User: Stephanie Myers


Item ID: 9285
Identification Number:
ISSN: 2156-8952
Official URL:

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Date Deposited: 09 May 2018 10:07
Last Modified: 18 Dec 2019 16:06


Author: Stephanie Myers
Author: Ruth H. Bawn
Author: Louise C. Bisset
Author: Timothy J. Blackburn
Author: Betty Cottyn
Author: Lauren Molyneux
Author: Ai-Ching Wong
Author: Celine Cano
Author: William Clegg
Author: Ross. W. Harrington
Author: Hing Leung
Author: Laurent Rigoreau
Author: Sandrine Vidot
Author: Bernard T. Golding
Author: Roger J. Griffin
Author: Tim Hammonds
Author: David R. Newell
Author: Ian R. Hardcastle
Author: Stephanie Myers

University Divisions

Faculty of Health Sciences and Wellbeing
Faculty of Health Sciences and Wellbeing > School of Pharmacy and Pharmaceutical Sciences


Sciences > Chemistry
Sciences > Pharmacy and Pharmacology

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