MEK inhibitor II [Ligand Id: 6007] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL404939
  • mitogen-activated protein kinase kinase 1/Dual specificity mitogen-activated protein kinase kinase 1 in Human [ChEMBL: CHEMBL3587] [GtoPdb: 2062] [UniProtKB: Q02750]
  • This target only has 0 pki data point
  • 0
1 CHEMBL404939_lig_chart_1 Dual specificity mitogen-activated protein kinase kinase 1 Human
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  • mitogen-activated protein kinase 3/MAP kinase ERK1 in Human [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361]
  • This target only has 0 pki data point
  • 0
2 CHEMBL404939_lig_chart_2 MAP kinase ERK1 Human
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  • mitogen-activated protein kinase kinase kinase 8/Mitogen-activated protein kinase kinase kinase 8 in Human [ChEMBL: CHEMBL4899] [GtoPdb: 2083] [UniProtKB: P41279]
  • This target only has 0 pki data point
  • 0
3 CHEMBL404939_lig_chart_3 Mitogen-activated protein kinase kinase kinase 8 Human
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  • Raf-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase RAF in Human [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049]
  • This target only has 0 pki data point
  • 0
4 CHEMBL404939_lig_chart_4 Serine/threonine-protein kinase RAF Human
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  • Tubulin alpha chain in Trypanosoma cruzi [ChEMBL: CHEMBL3988589] [UniProtKB: Q27352]
  • This target only has 0 pki data point
  • 0
5 CHEMBL404939_lig_chart_5 Tubulin alpha chain Trypanosoma cruzi
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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]
GtoPdb - - 6.42 pIC50 380 nM IC50 Proc Natl Acad Sci USA (2007) 104: 20523-8 [PMID:18077363]
ChEMBL Inhibition of MEK1 B 6.42 pIC50 380 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
mitogen-activated protein kinase 3/MAP kinase ERK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361]
ChEMBL Inhibition of ERK1 B 4.08 pIC50 82900 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
mitogen-activated protein kinase kinase kinase 8/Mitogen-activated protein kinase kinase kinase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4899] [GtoPdb: 2083] [UniProtKB: P41279]
GtoPdb - - 7.3 pIC50 50 nM IC50 Proc Natl Acad Sci USA (2007) 104: 20523-8 [PMID:18077363]
ChEMBL Inhibition of Tpl2 kinase B 7.3 pIC50 50 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
Raf-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase RAF in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049]
ChEMBL Inhibition of Raf1 B 4.46 pIC50 34500 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
Tubulin alpha chain in Trypanosoma cruzi (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3988589] [UniProtKB: Q27352]
ChEMBL Assembly Assay: Tubulin assembly assays were conducted to assess tubulin polymerization inhibition. The assays were conducted in a 96-well microplate. Assembly reactions were conducted in a buffer containing 0.1 M PIPES (pH 6.9), 1 mM EGTA, 5 mM Mgcl, 1.2 mg/ml purified Trypanosoma cruzi tublin, at concentrations (0.6-40 μM) of the imido-substituted 1,4-naphthoquinone (IMDNQ 1-IMDNQ 11). Components of the reaction mixtures were added to the microplate and assembly was initiated by the addition of 1 mM GTP. The assembly reactions were assayed photometrically by measuring the absorbance at 405 nm using a microplate reader at 30° C. B 5.22 pIC50 6000 nM IC50 US-9422231-B2. Method for inhibiting Trypanosoma cruzi (2016)

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, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]