- Guide to PHARMACOLOGY
Synonyms: GSK 126 | GSK-126 | GSK2816126
Compound class: Synthetic organic
Comment: GSK126 is a potent and selective small-molecule inhibitor of EZH2 (KMT6) methyltransferase activity . This is likely to be the ligand with the extended reseaerch code GSK2816126, which has anti-lymphoma potential.
Ligand Activity Visualisation Charts
These 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.✖
1. Diaz E, Machutta CA, Chen S, Jiang Y, Nixon C, Hofmann G, Key D, Sweitzer S, Patel M, Wu Z et al.. (2012)
Development and validation of reagents and assays for EZH2 peptide and nucleosome high-throughput screens.
J Biomol Screen, 17 (10): 1279-92. [PMID:22904200]
2. McCabe MT, Ott HM, Ganji G, Korenchuk S, Thompson C, Van Aller GS, Liu Y, Graves AP, Della Pietra 3rd A, Diaz E et al.. (2012)
EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations.
Nature, 492 (7427): 108-12. [PMID:23051747]