etoposide [Ligand Id: 6815] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL44657 (NSC-141540, VP-16-213, Vepesid, Etoposide, Toposar)
  • Arachidonate 15-lipoxygenase in Rabbit [ChEMBL: CHEMBL4358] [UniProtKB: P12530]
  • This target only has 0 pki data point
1 CHEMBL44657_lig_chart_1 Arachidonate 15-lipoxygenase Rabbit
There should be some charts here, you may need to enable JavaScript!
  • Caspase 3/Caspase-3 in Human [ChEMBL: CHEMBL2334] [GtoPdb: 1619] [UniProtKB: P42574]
  • This target only has 0 pki data point
2 CHEMBL44657_lig_chart_2 Caspase-3 Human
There should be some charts here, you may need to enable JavaScript!
  • DNA topoisomerase II alpha in Human [ChEMBL: CHEMBL1806] [GtoPdb: 2637] [UniProtKB: P11388]
  • This target only has 0 pki data point
3 CHEMBL44657_lig_chart_3 DNA topoisomerase II alpha Human
There should be some charts here, you may need to enable JavaScript!
  • DNA topoisomerase II beta in Human [ChEMBL: CHEMBL3396] [UniProtKB: Q02880]
  • This target only has 0 pki data point
4 CHEMBL44657_lig_chart_4 DNA topoisomerase II beta Human
There should be some charts here, you may need to enable JavaScript!
  • Human immunodeficiency virus type 1 integrase in Human immunodeficiency virus 1 [ChEMBL: CHEMBL3471] [UniProtKB: Q7ZJM1]
  • This target only has 0 pki data point
5 CHEMBL44657_lig_chart_5 Human immunodeficiency virus type 1 integrase Human immunodeficiency virus 1
There should be some charts here, you may need to enable JavaScript!
  • ABCB1/P-glycoprotein 1 in Human [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
  • P-glycoprotein 1 in Mouse [ChEMBL: CHEMBL3467] [UniProtKB: P06795]
  • This target only has 0 pki data point
6 CHEMBL44657_lig_chart_6 P-glycoprotein 1 HumanMouse
There should be some charts here, you may need to enable JavaScript!
  • ABCB1/P-glycoprotein 3 in Mouse [ChEMBL: CHEMBL2573] [GtoPdb: 768] [UniProtKB: P21447]
  • This target only has 0 pki data point
7 CHEMBL44657_lig_chart_7 P-glycoprotein 3 Mouse
There should be some charts here, you may need to enable JavaScript!
  • Plasmodium falciparum [ChEMBL: CHEMBL364]
  • This target only has 0 pki data point
8 CHEMBL44657_lig_chart_8 Plasmodium falciparum Plasmodium falciparum
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Arachidonate 15-lipoxygenase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4358] [UniProtKB: P12530]
ChEMBL DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid) B 5.5 pIC50 3187 nM IC50 DrugMatrix in vitro pharmacology data
Caspase 3/Caspase-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2334] [GtoPdb: 1619] [UniProtKB: P42574]
ChEMBL Activation of procaspase-3-mediated human NCI-H226 cell death after 72 hrs by MTS/PMS assay B 4.3 pIC50 >50000 nM IC50 Nat. Chem. Biol. (2006) 2: 543-550 [PMID:16936720]
ChEMBL Activation of procaspase-3-mediated human UACC62 cell death after 72 hrs by MTS/PMS assay B 4.3 pIC50 >50000 nM IC50 Nat. Chem. Biol. (2006) 2: 543-550 [PMID:16936720]
ChEMBL Activation of procaspase-3-mediated human CRL1782 cell death after 72 hrs by MTS/PMS assay B 4.3 pIC50 >50000 nM IC50 Nat. Chem. Biol. (2006) 2: 543-550 [PMID:16936720]
ChEMBL Activation of procaspase-3-mediated human B16-F10 cell death after 72 hrs by MTS/PMS assay B 4.3 pIC50 >50000 nM IC50 Nat. Chem. Biol. (2006) 2: 543-550 [PMID:16936720]
ChEMBL Activation of procaspase-3-mediated human Hs 578T cell death after 72 hrs by MTS/PMS assay B 4.3 pIC50 >50000 nM IC50 Nat. Chem. Biol. (2006) 2: 543-550 [PMID:16936720]
ChEMBL Activation of procaspase-3-mediated human SK-N-SH cell death after 72 hrs by MTS/PMS assay B 6 pIC50 <1000 nM IC50 Nat. Chem. Biol. (2006) 2: 543-550 [PMID:16936720]
ChEMBL Activation of procaspase-3-mediated human HL60 cell death after 72 hrs by MTS/PMS assay B 6 pIC50 <1000 nM IC50 Nat. Chem. Biol. (2006) 2: 543-550 [PMID:16936720]
ChEMBL Activation of procaspase-3-mediated human U937 cell death after 72 hrs by MTS/PMS assay B 6 pIC50 <1000 nM IC50 Nat. Chem. Biol. (2006) 2: 543-550 [PMID:16936720]
ChEMBL Activation of procaspase-3-mediated human PC12 cell death after 72 hrs by MTS/PMS assay B 6 pIC50 <1000 nM IC50 Nat. Chem. Biol. (2006) 2: 543-550 [PMID:16936720]
DNA topoisomerase II alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1806] [GtoPdb: 2637] [UniProtKB: P11388]
ChEMBL Inhibition of human recombinant topoisomerase 2 by decatenation assay B 4.03 pIC50 92900 nM IC50 Bioorg. Med. Chem. (2008) 16: 4545-4550 [PMID:18321715]
ChEMBL Inhibition of human topoisomerase-2alpha using kDNA as substrate assessed as inhibition of ATP-dependent kDNA decatenation after 30 mins by agarose gel electrophoresis B 4.11 pIC50 78400 nM IC50 Bioorg. Med. Chem. (2013) 21: 5782-5793 [PMID:23920485]
ChEMBL Inhibition of human topoisomerase-2 alpha assessed as reduction in enzyme-mediated kinetoplast DNA decatenation incubated for 30 mins by ethidium bromide staining based agarose gel electrophoresis method B 4.11 pIC50 78400 nM IC50 Bioorg. Med. Chem. (2015) 23: 5654-5661 [PMID:26216018]
ChEMBL Inhibition of human DNA topoisomerase 2alpha B 4.12 pIC50 75700 nM IC50 J. Nat. Prod. (2002) 65: 1657-1659 [PMID:12444693]
ChEMBL Inhibition of human topoisomerase 2 alpha-mediated relaxation of supercoiled pBR322 DNA after 30 mins by agarose gel electrophoresis B 4.22 pIC50 60300 nM IC50 Eur. J. Med. Chem. (2011) 46: 3339-3347 [PMID:21600681]
ChEMBL Inhibition of human DNA topoisomerase 2alpha-mediated decatenation of kinetoplast plasmid DNA by fluorescent plate reader B 4.25 pIC50 56000 nM IC50 Bioorg. Med. Chem. (2010) 18: 830-838 [PMID:20006518]
ChEMBL Inhibition of recombinant human DNA topoisomerase-2alpha assessed as decrease in relaxation of supercoiled pBR322 DNA after 30 mins by ethidium bromide staining based agarose gel electrophoresis B 4.25 pIC50 56000 nM IC50 Bioorg Med Chem (2017) 25: 4133-4144 [PMID:28619446]
ChEMBL Inhibition of human placenta topoisomerase 2alpha assessed as reduction in pBR322 supercoiled DNA relaxation after 30 mins by ethidium bromide staining based agarose gel electrophoresis B 4.3 pIC50 50200 nM IC50 Bioorg Med Chem (2018) 26: 1920-1928 [PMID:29519604]
ChEMBL Inhibition of human 1 unit topoisomerase 2alpha catalytic activity assessed as relaxation of 198 ng supercoiled pBR322 DNA by agarose gel electrophoresis B 4.3 pIC50 50000 nM IC50 J. Nat. Prod. (2001) 64: 1545-1547 [PMID:11754608]
ChEMBL Inhibition of human DNA topoisomerase 2alpha using plasmid pNO1 substrate incubated at 37 degC for 30 mins by fluorimetry B 4.47 pIC50 33800 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 5762-5768 [PMID:25453816]
ChEMBL Inhibition of human DNA topoisomerase-2alpha assessed as relaxation of supercoiled pBR322 DNA after 30 mins by agarose gel electrophoresis B 4.55 pIC50 28200 nM IC50 Eur. J. Med. Chem. (2013) 69: 139-145 [PMID:24013413]
ChEMBL Inhibition of topoisomerase 2 B 4.66 pIC50 21800 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 3122-3125 [PMID:22483608]
GtoPdb Note: enzyme subunit is not specified in the referenced article - 7.3 pIC50 50.4 nM IC50
DNA topoisomerase II beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3396] [UniProtKB: Q02880]
ChEMBL Inhibition of human topoisomerase-2B after 2 hrs by ELISA B 6.1 pIC50 790 nM IC50 Eur J Med Chem (2018) 150: 403-418 [PMID:29547830]
ChEMBL Inhibition of human DNA topoisomerase 2beta after 2 hrs by ELISA B 7.16 pIC50 69.8 nM IC50 Eur J Med Chem (2018) 156: 563-579 [PMID:30025350]
ChEMBL Inhibition of calf thymus DNA/ethidium bromide complex formation. B 4.15 pEC50 >70000 nM EC50 Bioorg. Med. Chem. Lett. (1995) 5: 405-410
Human immunodeficiency virus type 1 integrase in Human immunodeficiency virus 1 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3471] [UniProtKB: Q7ZJM1]
ChEMBL Compound concentration required to reduce HIV-1 Integrase 3'-processing activity by 50% B 4 pIC50 >100000 nM IC50 J. Med. Chem. (1998) 41: 3948-3960 [PMID:9767632]
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL Inhibition of P-glycoprotein using calcein-AM assay transfected in porcine PBCEC F 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells F 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
P-glycoprotein 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3467] [UniProtKB: P06795]
ChEMBL Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells F 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
ABCB1/P-glycoprotein 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2573] [GtoPdb: 768] [UniProtKB: P21447]
ChEMBL Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells F 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay F 5.2 pIC50 6309.57 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay F 5.3 pIC50 5011.87 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 5.3 pIC50 5011.87 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 5.3 pIC50 5011.87 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5.4 pIC50 3981.07 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 5.4 pIC50 3981.07 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 5.5 pIC50 3162.28 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]

ChEMBL data shown on this page come from version 27:

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]