Synonyms: EZM-0414
Compound class:
Synthetic organic
Comment: EZM0414 is a first-in-class, oral SETD2 histone methyl transferase inhibitor that was developed by Epizyme for anti-cancer potential. Its chemical structure was disclosed at the AACR spring meeting in 2022 (link to download poster pdf here).
|
|
Bioactivity Comments |
We have been unable to find published quantitative interaction for this ligand at its stated molecular target (June 2022). A SETD2 IC50 value of 18 nM (determined in an enzyme biochemical assay) was originally revealed in a poster presentation at the American Society of Hematology (ASH) 63rd annual meeting in December 2021. Bioactivity data and the chemical structure for EZM0414 were released in the discovery and first disclosure session of the 2022 AACR meeting (link to download poster pdf here). |