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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 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]