etoposide [Ligand Id: 6815] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL44657 (Etoposide, Etoposide resolution mixture, Etoposidum, NSC-141540, Sintopozid, Toposar, Vepesid, VP-16-213) |
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| 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 2alpha using supercoiled pNO1 plasmid DNA as substrate incubated for 30 mins by fluorescence based microplate reader analysis | B | 4.15 | pIC50 | 71000 | nM | IC50 | RSC Med Chem (2020) 11: 378-386 [PMID:33479643] |
| ChEMBL | Inhibition of human DNA topoisomerase 2alpha assessed as suppression of decatenation using catenated kinetoplast DNA as substrate measured after 30 mins by SYBR safe DNA staining based staining-based agarose gel electrophoresis method | B | 4.17 | pIC50 | 68300 | nM | IC50 | Eur J Med Chem (2020) 202: 112504-112504 [PMID:32712536] |
| 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 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 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 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 topo2alpha incubated for 30 mins by SYBR safe DNA stain based decatenation assay | B | 4.32 | pIC50 | 47500 | nM | IC50 | J Med Chem (2020) 63: 3508-3521 [PMID:32196342] |
| 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 recombinant human topoisomerase 2alpha using supercoiled pNO1 plasmid as substrate after 30 mins by SYBR-GOLD staining based fluorimetric analysis | B | 4.47 | pIC50 | 33800 | nM | IC50 | J Med Chem (2018) 61: 8947-8980 [PMID:29870668] |
| 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
