E6201 [Ligand Id: 7836] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1097999 (E6201, E-6201, ER-806201)
  • 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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  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
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  • mitogen-activated protein kinase kinase kinase 1 in Human [GtoPdb: 2069] [UniProtKB: Q13233]
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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 MEK1 (unknown origin) phosphorylation by [gamma-33P]-ATP assay B 7.3 pIC50 50 nM IC50 Eur J Med Chem (2019) 178: 468-483 [PMID:31207462]
ChEMBL Inhibition of MEK1 (unknown origin) using ERK2 as substrate after 40 mins by ELISA B 7.89 pIC50 13 nM IC50 US-20090082313-A1. Multikinase inhibitors for use in the treatment of cancer (2009)
GtoPdb - - 8.28 pIC50 5.2 nM IC50 J Pharmacol Exp Ther (2009) 331: 485-95 [PMID:19684251]
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
ChEMBL Inhibition of FLT3 (unknown origin) phosphorylation by [gamma-33P]-ATP assay B 8.3 pIC50 5 nM IC50 Eur J Med Chem (2019) 178: 468-483 [PMID:31207462]
mitogen-activated protein kinase kinase kinase 1 in Human [GtoPdb: 2069] [UniProtKB: Q13233]
GtoPdb - - 7.51 pIC50 31 nM IC50 J Pharmacol Exp Ther (2009) 331: 485-95 [PMID:19684251]

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]