compound 5z [PMID: 8410981] [Ligand Id: 8893] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL307794
  • DNA topoisomerase I in Human [ChEMBL: CHEMBL1781] [GtoPdb: 2636] [UniProtKB: P11387]
  • DNA topoisomerase I in Bovine [GtoPdb: 2636]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
DNA topoisomerase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1781] [GtoPdb: 2636] [UniProtKB: P11387]
ChEMBL Inhibition of topoisomerase I activity was determined in vitro by using the cleavable complex assay(calf thymus) B 7.11 pIC50 78 nM IC50 J Med Chem (1995) 38: 395-401 [PMID:7853331]
ChEMBL Ability to inhibit calf thymus topoisomerase I when assayed in the cleavable complex formation B 7.52 pIC50 30 nM IC50 Bioorg Med Chem Lett (1995) 5: 2129-2132
ChEMBL Inhibition of Topoisomerase I by cleavage complex formation in human HL-60 cells B 7.57 pIC50 27 nM IC50 J Med Chem (1993) 36: 2689-2700 [PMID:8410981]
ChEMBL Effective concentration against DNA topoisomerase I B 7.3 pEC50 50 nM EC50 Bioorg Med Chem Lett (2004) 14: 5377-5381 [PMID:15454230]
DNA topoisomerase I in Bovine [GtoPdb: 2636]
GtoPdb Inhibition of pBR322 DNA cleavage by calf thymus DNA topoisomerase I. - 7.57 pIC50 27 nM IC50 J Med Chem (1993) 36: 2689-700 [PMID:8410981]

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]