trametinib [Ligand Id: 6495] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2103875 (TMT-212, TMT212, JTP 74057, JTP-74057, Trametinib, Tmt212, GSK1120212, GSK-1120212, Mekinist)
  • mitogen-activated protein kinase kinase 1/Dual specificity mitogen-activated protein kinase kinase 1 in Human [ChEMBL: CHEMBL3587] [GtoPdb: 2062] [UniProtKB: Q02750]
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  • mitogen-activated protein kinase kinase 2/Dual specificity mitogen-activated protein kinase kinase 2 in Human [ChEMBL: CHEMBL2964] [GtoPdb: 2063] [UniProtKB: P36507]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
mitogen-activated protein kinase kinase 1/Dual specificity mitogen-activated protein kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3587] [GtoPdb: 2062] [UniProtKB: Q02750]
ChEMBL Inhibition of B-Raf activated MEK1 (unknown origin) assessed as ERK2-mediated MBP phosphorylation after 30 mins by ELISA B 8.47 pIC50 3.4 nM IC50 MedChemComm (2014) 5: 99-106
GtoPdb Inhibition of unphosphorylated MEK1. - 9.15 pIC50 0.7 nM IC50 Clin Cancer Res (2011) 17: 989-1000 [PMID:21245089];
Int J Oncol (2011) 39: 23-31 [PMID:21523318]
ChEMBL Inhibition of MEK1 (unknown origin) B 9.15 pIC50 0.7 nM IC50 Eur J Med Chem (2019) 168: 315-329 [PMID:30826508]
mitogen-activated protein kinase kinase 2/Dual specificity mitogen-activated protein kinase kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2964] [GtoPdb: 2063] [UniProtKB: P36507]
ChEMBL Inhibition of MEK2 (unknown origin) B 7.83 pIC50 14.9 nM IC50 Eur J Med Chem (2019) 168: 315-329 [PMID:30826508]
GtoPdb - - 8.74 pIC50 1.8 nM IC50 Int J Oncol (2011) 39: 23-31 [PMID:21523318]
ChEMBL Inhibition of B-Raf activated MEK2 (unknown origin) assessed as ERK2-mediated MBP phosphorylation after 30 mins by ELISA B 8.8 pIC50 1.6 nM IC50 MedChemComm (2014) 5: 99-106
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL Inhibition of ABCB1 in human A2780/ADR cells assessed as potentiation of daunorubicin-induced cytotoxicity measured after 72 hrs by MTT assay B 6.61 pEC50 247 nM EC50 Eur J Med Chem (2019) 164: 193-213 [PMID:30594677]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]