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Assay Detail

CHEMBL812283

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibitory activity against HeLa cell Topoisomerase II
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HeLa
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

DNA topoisomerase II (CHEMBL2094255)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

3-benzyl-quinolones: Novel, potent inhibitors of mammalian topoisomerase II
Eissenstat MA, Kuo G, Weaver JD, Wentland MP, Robinson RG, Klingbeil KM, Danz DW, Corbett TH, Coughlin SA
Bioorg Med Chem Lett (1995) 5 : 1021 -1026
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 36 5.73 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8 CIPROFLOXACIN 4.0 1 7.52
CHEMBL440642 1 7.02
CHEMBL428339 1 7.01
CHEMBL269139 1 6.80
CHEMBL7877 1 6.80
CHEMBL268458 1 6.48
CHEMBL7690 1 6.44
CHEMBL43 AMSACRINE 4.0 1 6.14
CHEMBL44657 ETOPOSIDE 4.0 1 6.09
CHEMBL7960 1 5.96
CHEMBL8063 1 5.96
CHEMBL7534 1 5.92
CHEMBL267251 1 5.80
CHEMBL7769 1 5.68
CHEMBL7562 1 5.48
CHEMBL8161 1 5.41
CHEMBL267707 1 5.33
CHEMBL7618 1 5.29
CHEMBL7368 1 5.29
CHEMBL8138 1 5.17
CHEMBL7564 1 5.14
CHEMBL8179 WIN-57294 1 5.12
CHEMBL7848 1 5.11
CHEMBL7216 1 5.04
CHEMBL7794 1 4.92
CHEMBL266463 1 4.85
CHEMBL7831 1 4.85
CHEMBL7972 1 4.85
CHEMBL414022 1 4.77
CHEMBL267017 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8 CIPROFLOXACIN EC50 = 30.0 nM 7.52
CHEMBL440642 EC50 = 96.0 nM 7.02
CHEMBL428339 EC50 = 98.0 nM 7.01
CHEMBL269139 EC50 = 160.0 nM 6.80
CHEMBL7877 EC50 = 160.0 nM 6.80
CHEMBL268458 EC50 = 330.0 nM 6.48
CHEMBL7690 EC50 = 360.0 nM 6.44
CHEMBL43 AMSACRINE EC50 = 720.0 nM 6.14
CHEMBL44657 ETOPOSIDE EC50 = 810.0 nM 6.09
CHEMBL7960 EC50 = 1100.0 nM 5.96
CHEMBL8063 EC50 = 1100.0 nM 5.96
CHEMBL7534 EC50 = 1200.0 nM 5.92
CHEMBL267251 EC50 = 1600.0 nM 5.80
CHEMBL7769 EC50 = 2100.0 nM 5.68
CHEMBL7562 EC50 = 3300.0 nM 5.48
CHEMBL8161 EC50 = 3900.0 nM 5.41
CHEMBL267707 EC50 = 4700.0 nM 5.33
CHEMBL7368 EC50 = 5100.0 nM 5.29
CHEMBL7618 EC50 = 5100.0 nM 5.29
CHEMBL8138 EC50 = 6800.0 nM 5.17
CHEMBL7564 EC50 = 7200.0 nM 5.14
CHEMBL8179 WIN-57294 EC50 = 7600.0 nM 5.12
CHEMBL7848 EC50 = 7700.0 nM 5.11
CHEMBL7216 EC50 = 9100.0 nM 5.04
CHEMBL7794 EC50 = 12000.0 nM 4.92
CHEMBL7972 EC50 = 14000.0 nM 4.85
CHEMBL7831 EC50 = 14000.0 nM 4.85
CHEMBL266463 EC50 = 14000.0 nM 4.85
CHEMBL414022 EC50 = 17000.0 nM 4.77
CHEMBL267017 EC50 > 210000.0 nM -
CHEMBL7722 EC50 > 230000.0 nM -
CHEMBL7392 EC50 = 200000.0 nM -
CHEMBL7991 EC50 > 100000.0 nM -
CHEMBL7704 EC50 > 120000.0 nM -
CHEMBL7999 EC50 > 120000.0 nM -
CHEMBL7689 EC50 > 210000.0 nM -