topotecan [Ligand Id: 7101] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL84 (Ff-10850 (liposomal topotecan), Hycamptamine, Hycamptin, Hycamtin, Nogitecan, NSC-609699, NSC-641007, Potactasol, SKF-104864, Topotecan) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| ABCG2/ATP-binding cassette sub-family G member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0] | ||||||||
| ChEMBL | TP_TRANSPORTER: drug resistance(Imatinib mesylate) in BCRP-expressing SaoS2 cells | F | 6.77 | pIC50 | <170 | nM | IC50 | Cancer Res (2004) 64: 2333-2337 [PMID:15059881] |
| CYP3A4/Cytochrome P450 3A4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL340] [GtoPdb: 1337] [UniProtKB: P08684] | ||||||||
| ChEMBL | DRUGMATRIX: CYP450, 3A4 enzyme inhibition (substrate: 7-Benzyloxy-4-(trifluoromethyl)-coumarin) | B | 5.82 | pIC50 | 1521.1 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| DNA topoisomerase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1781] [GtoPdb: 2636] [UniProtKB: P11387] | ||||||||
| ChEMBL | Binding affinity to topoisomerase 1 | B | 7.58 | pKd | 26.5 | nM | Kd | J Nat Prod (2011) 74: 1401-1407 [PMID:21542600] |
| ChEMBL | Inhibition of human topoisomerase I using DNA pBR322 as substrate assessed as DNA relaxation incubated for 45 mins by ethidium bromide staining based agarose gel electrophoresis | B | 4.64 | pIC50 | 22880 | nM | IC50 | Eur J Med Chem (2021) 226: 113817-113817 [PMID:34537445] |
| ChEMBL | Inhibition of DNA topoisomerase 1 in Homo sapiens (human) SW480 cells | B | 5.02 | pIC50 | 9650 | nM | IC50 | Med Chem Res (2010) 19: 817-835 |
| ChEMBL | Inhibition of DNA topoisomerase 1 in Homo sapiens (human) HCT116 cells | B | 5.26 | pIC50 | 5550 | nM | IC50 | Med Chem Res (2010) 19: 817-835 |
| ChEMBL | Inhibition of DNA topoisomerase 1 in Homo sapiens (human) VACO 241 cells | B | 5.28 | pIC50 | 5250 | nM | IC50 | Med Chem Res (2010) 19: 817-835 |
| ChEMBL | Inhibition of Top1 in human MCF7 cells using supercoiled pBS (SK+) DNA as substrate incubated for 30 mins by ethidium bromide staining based agarose gel electrophoresis analysis | B | 5.74 | pIC50 | 1800 | nM | IC50 | Eur J Med Chem (2020) 202: 112551-112551 [PMID:32682183] |
| ChEMBL | Poison activity at TOP1 in human MCF7 cells assessed as decrease in relaxed supercoiled pBS(SK+) DNA mobility measured after 30 mins by ethidium bromide staining based agarose gel electrophoresis | B | 5.74 | pIC50 | 1800 | nM | IC50 | J Med Chem (2019) 62: 3428-3446 [PMID:30897325] |
| ChEMBL | Average concentration of compound to cause 50% inhibition of topoisomerase-1 isolated from calf thymus | B | 5.96 | pIC50 | 1100 | nM | IC50 | J Med Chem (1996) 39: 713-719 [PMID:8576914] |
| ChEMBL | Inhibition of topoisomerase I activity was determined in vitro by using the cleavable complex assay(calf thymus) | B | 5.99 | pIC50 | 1028 | nM | IC50 | J Med Chem (1995) 38: 395-401 [PMID:7853331] |
| ChEMBL | Inhibition of Topoisomerase I by cleavage complex formation in human HL-60 cells | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (1993) 36: 2689-2700 [PMID:8410981] |
| ChEMBL | Inhibition of topoisomerase I-DNA complex in trapping assay | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (2005) 48: 2336-2345 [PMID:15801827] |
| ChEMBL | Inhibition of recombinant human Top1 expressed in baculovirus infected sf9 insect cells using supercoiled pBS (SK+) DNA as substrate incubated for 30 mins by ethidium bromide staining based agarose gel electrophoresis analysis | B | 7.68 | pIC50 | 21 | nM | IC50 | Eur J Med Chem (2020) 202: 112551-112551 [PMID:32682183] |
| ChEMBL | Poison activity at recombinant human TOP1 expressed in baculovirus infected Sf9 insect cells assessed as decrease in relaxed supercoiled pBS(SK+) DNA mobility measured after 30 mins by ethidium bromide staining based agarose gel electrophoresis | B | 7.68 | pIC50 | 21 | nM | IC50 | J Med Chem (2019) 62: 3428-3446 [PMID:30897325] |
| ChEMBL | Inhibition of topoisomerase-1 in human U251 cells assessed as inhibition of HIF-1-mediated hypoxia-induced VEGF expression after 24 hrs by luciferase reporter gene assay | B | 7.15 | pEC50 | 71.3 | nM | EC50 | Eur J Med Chem (2012) 49: 24-40 [PMID:22305612] |
| ChEMBL | Inhibition of topoisomerase-1 in human U251 cells assessed as inhibition of hypoxia-induced HIF-1alpha accumulation in nuclear extract after 6 to 24 hrs by immunoblot analysis | B | 7.27 | pEC50 | 54 | nM | EC50 | Eur J Med Chem (2012) 49: 24-40 [PMID:22305612] |
| DNA topoisomerase I in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2814] [GtoPdb: 2636] [UniProtKB: Q04750] | ||||||||
| ChEMBL | Average concentration to cause 50% inhibition of topo 1 using the cleavable complex assay | B | 4.7 | pIC50 | 20000 | nM | IC50 | J Med Chem (2001) 44: 1594-1602 [PMID:11334569] |
| Hypoxia-inducible factor 1 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4261] [UniProtKB: Q16665] | ||||||||
| ChEMBL | Inhibition of HIF1alpha in human U251 cells under normoxic condition by luciferase reporter gene assay | B | 5.52 | pIC50 | >3000 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 6426-6429 [PMID:20932758] |
| ChEMBL | Inhibition of HIF1alpha in human U251 cells under hypoxic condition by luciferase reporter gene assay | B | 7.22 | pIC50 | 60 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 6426-6429 [PMID:20932758] |
| ChEMBL | Inhibition of human HIF1alpha-mediated transcription expressed in human U251 cells co-transfected with pGL2-TK-HRE incubated for 24 hrs by luciferase reporter gene assay | B | 7.92 | pEC50 | 12 | nM | EC50 | Medchemcomm (2014) 5: 923-926 |
| Multidrug and toxin extrusion/Multidrug and toxin extrusion protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743126] [GtoPdb: 1216] [UniProtKB: Q96FL8] | ||||||||
| ChEMBL | Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | B | 5.89 | pIC50 | 1300 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
| MATE2/Multidrug and toxin extrusion protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743127] [GtoPdb: 1217] [UniProtKB: Q86VL8] | ||||||||
| ChEMBL | Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | B | 5.07 | pIC50 | 8600 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
| Organic cation transporter 2/Solute carrier family 22 member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244] | ||||||||
| ChEMBL | Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay | B | 4.21 | pIC50 | 61000 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
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]
