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Synonyms: ARRY 162 | ARRY-162 | ARRY-438162 | MEK-162 | MEK162 | Mektovi®
binimetinib is an approved drug (FDA and EMA (2018))
Compound class: Synthetic organic
Comment: Binimetinib is a potent non-ATP competitive inhibitor of MEK1/2 kinase activity  (link directly to abstract 794 online here).
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. Ascierto PA, Schadendorf D, Berking C, Agarwala SS, van Herpen CM, Queirolo P, Blank CU, Hauschild A, Beck JT, St-Pierre A et al.. (2013)
MEK162 for patients with advanced melanoma harbouring NRAS or Val600 BRAF mutations: a non-randomised, open-label phase 2 study.
Lancet Oncol, 14 (3): 249-56. [PMID:23414587]
2. Dummer R, Ascierto PA, Gogas HJ, Arance A, Mandala M, Liszkay G, Garbe C, Schadendorf D, Krajsova I, Gutzmer R et al.. (2018)
Encorafenib plus binimetinib versus vemurafenib or encorafenib in patients with BRAF-mutant melanoma (COLUMBUS): a multicentre, open-label, randomised phase 3 trial.
Lancet Oncol, 19 (5): 603-615. [PMID:29573941]
3. Pheneger J, Wallace, E, Marlow, A Hurley B, Lyssikatos J, Bendele AM, Lee PA. (2006)
Characterization of ARRY-438162, a Potent MEK Inhibitor in Combination with Methotrexate or Ibuprofen in In Vivo Models of Arthritis.[abstract].
American College of Rheumatology 2006 Annual Scientific Meeting,: Abstract 794.