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

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ChEMBL ligand: CHEMBL1097999 (E-6201, E6201, 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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]