Tpl2 kinase inhibitor [Ligand Id: 6051] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL200381
  • mitogen-activated protein kinase kinase 1/Dual specificity mitogen-activated protein kinase kinase 1 in Human [ChEMBL: CHEMBL3587] [GtoPdb: 2062] [UniProtKB: Q02750]
Created with Highcharts 10.3.3ValuesChart context menuDual specificity mitogen-activated protein kinase kinase 1pKd HumanpKi HumanpIC50 HumanpEC50 Human012345Highcharts.com
  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
Created with Highcharts 10.3.3ValuesChart context menuEpidermal growth factor receptor erbB1pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525]
Created with Highcharts 10.3.3ValuesChart context menuInterferon-induced, double-stranded RNA-activated protein kinasepKd HumanpKi HumanpIC50 HumanpEC50 Human02468Highcharts.com
  • mitogen-activated protein kinase kinase kinase 8/Mitogen-activated protein kinase kinase kinase 8 in Human [ChEMBL: CHEMBL4899] [GtoPdb: 2083] [UniProtKB: P41279]
Created with Highcharts 10.3.3ValuesChart context menuMitogen-activated protein kinase kinase kinase 8pKd HumanpKi HumanpIC50 HumanpEC50 Human02468Highcharts.com
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 Inhibitory activity against MEK B 4.4 pIC50 >40000 nM IC50 Bioorg Med Chem Lett (2005) 15: 5288-5292 [PMID:16165349]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibition of EGFR kinase autophosphorylation in A431 cells B 5.3 pIC50 <5000 nM IC50 Bioorg Med Chem (2007) 15: 6425-6442 [PMID:17664070]
eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525]
ChEMBL Inhibition of human recombinant PKR autophosphorylation using poly[I:C] after 10 mins by luminescent assay B 6.6 pIC50 250 nM IC50 Bioorg Med Chem Lett (2011) 21: 4108-4114 [PMID:21632247]
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 Bioorg Med Chem Lett (2005) 15: 5288-92 [PMID:16165349]
ChEMBL Inhibitory activity against human Tpl2 kinase via quantification of MEK phosphorylation F 7.3 pIC50 50 nM IC50 Bioorg Med Chem Lett (2005) 15: 5288-5292 [PMID:16165349]

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]