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Compound class: Synthetic organic
Comment: Bromo-deaza-SAH is a small molecule inhibitor of the chromatin modifying enzymes DOT1-like histone H3K79 methyltransferase (DOT1L) and DNA (cytosine-5-)-methyltransferase 1 (DNMT1).
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. Bernt KM, Zhu N, Sinha AU, Vempati S, Faber J, Krivtsov AV, Feng Z, Punt N, Daigle A, Bullinger L et al.. (2011)
MLL-rearranged leukemia is dependent on aberrant H3K79 methylation by DOT1L.
Cancer Cell, 20 (1): 66-78. [PMID:21741597]
2. Muntean AG, Hess JL. (2012)
The pathogenesis of mixed-lineage leukemia.
Annu Rev Pathol, 7: 283-301. [PMID:22017583]
3. Nguyen AT, Taranova O, He J, Zhang Y. (2011)
DOT1L, the H3K79 methyltransferase, is required for MLL-AF9-mediated leukemogenesis.
Blood, 117 (25): 6912-22. [PMID:21521783]
4. Yu W, Smil D, Li F, Tempel W, Fedorov O, Nguyen KT, Bolshan Y, Al-Awar R, Knapp S, Arrowsmith CH et al.. (2013)
Bromo-deaza-SAH: a potent and selective DOT1L inhibitor.
Bioorg. Med. Chem., 21 (7): 1787-94. [PMID:23433670]