Synonyms: compound 23a [PMID: 29211475] | PF06821497
Compound class:
Synthetic organic
Comment: PF-06821497 is an orally active inhibitor of the histone methyltransferase, enhancer of zeste homolog 2 (EZH2), that was developed by Pfizer for antineoplastic potential [1]. Inhibition of EZH2 activity reduces mono-, di-, and trimethylation of lysine 27 on histone H3 (H3K27me, me2, and me3), and this ultimately leads to an antiproliferative effect on susceptible cancer cells (i.e. where aberrant EZH2-mediated epigenetic alterations are driving tumour initiation and progression).
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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Classification | |
Compound class | Synthetic organic |
IUPAC Name |
5,8-dichloro-2-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-7-[(R)-methoxy(oxetan-3-yl)methyl]-3,4-dihydroisoquinolin-1-one |
Synonyms |
compound 23a [PMID: 29211475] | PF06821497 |
Database Links | |
CAS Registry No. | 1844849-10-0 (source: PubChem) |
ChEMBL Ligand | CHEMBL4080228 |
GtoPdb PubChem SID | 387065598 |
PubChem CID | 118572065 |
RCSB PDB Ligand | CJD |
Search Google for chemical match using the InChIKey | RXCVUHMIWHRLDF-HXUWFJFHSA-N |
Search Google for chemicals with the same backbone | RXCVUHMIWHRLDF |
UniChem Compound Search for chemical match using the InChIKey | RXCVUHMIWHRLDF-HXUWFJFHSA-N |
UniChem Connectivity Search for chemical match using the InChIKey | RXCVUHMIWHRLDF-HXUWFJFHSA-N |