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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]