Bawn RH

Bisset LC

Blackburn TJ

Cano C

Clegg W

Cottyn B

Golding BT

Griffin RJ

Hammonds T

Hardcastle IR

Harrington RW

Leung H

Molyneux L

Myers SM

Newell DR

Rigoreau L

Vidot S

Wong AC

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

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

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

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