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Synonyms: compound 16 [PMID: 35837138] | MS-8815
Compound class:
Synthetic organic
Comment: MS8815 is a bifunctional PROTAC molecule that targets the enhancer of zeste homolog 2 (EZH2) protein for degradation [1]. It contains a VHL-binding ligand VHL-1 (a.k.a. VH032 [3]; PubChem CID 77232228; Kd 188 nM) to recruit the VHL E3 ligase, and the EZH2 engager is the FDA-approved drug tazemetostat (EPZ-6438). EZH2 overexpression is a marker of poor prognosis in triple-negative breast cancer (TNBC). Protein degrading agents are proposed as alternatives to small molecule inhibitors, and are of particular use for 'difficult-to-drug' protein targets.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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