Compound class:
Synthetic organic
Comment: A-395 potently binds the embryonic ectoderm development protein (EED) [1], a protein with a scaffolding function and an H3K27me3-binding function. A-395 inhibits this latter function by binding in the H3K27me3-binding pocket of EED. This action prevents allosteric activation of the catalytic activity of the EED-containing polycomb repressive complex 2 (PRC2). A-395 is one of the chemical tools in the Structural Genomics Consortium's Epigenetic Probes Library. and was developed in collaboration with Abbvie.
![]() 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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References |
1. He Y, Selvaraju S, Curtin ML, Jakob CG, Zhu H, Comess KM, Shaw B, The J, Lima-Fernandes E, Szewczyk MM et al.. (2017)
The EED protein-protein interaction inhibitor A-395 inactivates the PRC2 complex. Nat Chem Biol, 13 (4): 389-395. [PMID:28135237] |