Synonyms: EED inhibitor-1 | example 2 [WO2016103155A1] | MAK-683
Compound class:
Synthetic organic
Comment: MAK683 is an allosteric inhibitor of the protein-protein interaction (PPI) between embryonic ectoderm development protein (EED) and polycomb repressive complex 2 (PRC2; EZH2) that was developped by Novartis for potential antineoplastic activity. It is one of the chemical structures claimed in Novartis' patent WO2016103155A1, and it targets EED [1]. EED has no intrinsic enzymatic activity but it is essential for PRC2 function. EED binds to histone H3K27 trimethylation marks which localizes the PRC2 complex to the chromatin substrate and allosterically activates PRC2's methyltransferase activity. Disruption of the EED-EZH2 PPI results in a loss of H3K27me3-stimulated PRC2 activity and reduces histone H3K27 trimethylation. In EZH2-mutated and PRC2-dependent cancer cells this PPI disruption modifies gene expression patterns within cancer pathways and ultimately decreases tumour cell proliferation.
![]() 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. ✖ |
|
Classification ![]() |
|
Compound class | Synthetic organic |
IUPAC Name ![]() |
N-[(5-fluoro-2,3-dihydro-1-benzofuran-4-yl)methyl]-8-(2-methylpyridin-3-yl)-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine |
Synonyms ![]() |
EED inhibitor-1 | example 2 [WO2016103155A1] | MAK-683 |
Database Links ![]() |
|
BindingDB Ligand | 291687 |
CAS Registry No. | 1951408-58-4 (source: PubChem) |
GtoPdb PubChem SID | 387065597 |
PubChem CID | 121412508 |
RCSB PDB Ligand | EJR |
Search Google for chemical match using the InChIKey | XLIBABIFOBYHSV-UHFFFAOYSA-N |
Search Google for chemicals with the same backbone | XLIBABIFOBYHSV |
UniChem Compound Search for chemical match using the InChIKey | XLIBABIFOBYHSV-UHFFFAOYSA-N |
UniChem Connectivity Search for chemical match using the InChIKey | XLIBABIFOBYHSV-UHFFFAOYSA-N |
Product supplier links are provided as a service to assist in identifying commercial suppliers of reagents that are mentioned on the IUPHAR/BPS Guide to PHARMACOLOGY database website, and do not imply their endorsement by NC-IUPHAR.
Links are provided in return for sponsorship, used to fund improvements to this database. The sponsorship account is managed and audited by the University of Edinburgh, a charitable body registered in Scotland, SC005336. If you are interested in sponsoring the database, please contact us.
✖
MAK683 (links to external site)
Cat. No. HY-103663 |