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Synonyms: compound 17 [PMID: 21310613] | example 18 [US8470837] | TAK733
Compound class: Synthetic organic
Comment: TAK-733 is a potent and selective MEK inhibitor with an allosteric binding mode, that was designed as a novel cancer chemotherapeutic .
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. Adjei AA, LoRusso P, Ribas A, Sosman JA, Pavlick A, Dy GK, Zhou X, Gangolli E, Kneissl M, Faucette S et al.. (2017)
A phase I dose-escalation study of TAK-733, an investigational oral MEK inhibitor, in patients with advanced solid tumors.
Invest New Drugs, 35 (1): 47-58. [PMID:27650277]
2. Akinleye A, Furqan M, Mukhi N, Ravella P, Liu D. (2013)
MEK and the inhibitors: from bench to bedside.
J Hematol Oncol, 6: 27. [PMID:23587417]
3. Dong Q, Dougan DR, Gong X, Halkowycz P, Jin B, Kanouni T, O'Connell SM, Scorah N, Shi L, Wallace MB et al.. (2011)
Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer.
Bioorg Med Chem Lett, 21 (5): 1315-9. [PMID:21310613]