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 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]
