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ChEMBL ligand: CHEMBL837 (7-ethyl-10-hydroxycamptothecin, 7-Ethyl-10-Hydroxy-Camptothecin, Camptothecin, 7-ethyl-10-hydroxy-, Irinotecan related compound b, It-141, IT-141, Nk012, NK 012, NK-012, NK012, SN 38, SN-38) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 | 6.75 | pIC50 | 176 | nM | IC50 | Cancer Res (2004) 64: 2333-2337 [PMID:15059881] |
DNA topoisomerase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1781] [GtoPdb: 2636] [UniProtKB: P11387] | ||||||||
ChEMBL | Inhibition of human topoisomerase 1 | B | 5.26 | pIC50 | 5500 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2018-2021 [PMID:19254843] |
ChEMBL | Inhibition of human topoisomerase 1 | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (2021) 64: 1435-1453 [PMID:33492141] |
ChEMBL | Effective concentration against DNA topoisomerase I | B | 6.49 | pEC50 | 320 | nM | EC50 | Bioorg Med Chem Lett (2004) 14: 5377-5381 [PMID:15454230] |
ChEMBL | Effective concentration against DNA topoisomerase I | B | 7.15 | pEC50 | 70 | nM | EC50 | Bioorg Med Chem Lett (2004) 14: 5377-5381 [PMID:15454230] |
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 | 5.4 | pIC50 | 4000 | nM | IC50 | J Med Chem (2001) 44: 1594-1602 [PMID:11334569] |
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]