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 |
|---|
Abstract
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.
![[img]](http://sure.sunderland.ac.uk/style/images/fileicons/application_pdf.png) |
PDF
HTS and hit validation of ERK5 Inhibitors.pdf - Published Version Restricted to Repository staff only Download (1MB) | Request a copy |
More Information
| Depositing User: Stephanie Myers |
Identifiers
| Item ID: 9285 |
| Identification Number: https://doi.org/10.1021/acscombsci.5b00155 |
| ISSN: 2156-8952 |
| URI: http://sure.sunderland.ac.uk/id/eprint/9285 | Official URL: https://doi.org/10.1021/acscombsci.5b00155 |
Users with ORCIDS
Catalogue record
| 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 WellbeingFaculty of Health Sciences and Wellbeing > School of Pharmacy and Pharmaceutical Sciences
Subjects
Sciences > ChemistrySciences > Pharmacy and Pharmacology
Actions (login required)
 |
View Item (Repository Staff Only) |
