High-Throughput Screening and Hit Validation of Extracellular-Related Kinase 5 (ERK5) Inhibitors
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https://figshare.com/articles/dataset/High-Throughput_Screening_and_Hit_Validation_of_Extracellular-Related_Kinase_5_ERK5_Inhibitors/3493088
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资源简介：
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.
创建时间：
2016-08-02
