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Assay Detail

CHEMBL812057

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

Binding
In vitro evaluation for inhibitor of human topoisomerase II from HeLa cells.
23
Total Activities
23
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

Synthesis and antitumor activity of 4-aminomethylthioxanthenone and 5-aminomethylbenzothiopyranoindazole derivatives.
Perni RB, Wentland MP, Huang JI, Powles RG, Aldous S, Klingbeil KM, Peverly AD, Robinson RG, Corbett TH, Jones JL, Mattes KC, Rake JB, Coughlin SA.
J Med Chem (1998) 41 : 3645 -3654
PubMed 9733489 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 23 5.51 6.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27233 1 6.48
CHEMBL121666 1 6.30
CHEMBL30104 1 6.26
CHEMBL121442 1 5.80
CHEMBL283395 1 5.52
CHEMBL122716 1 5.00
CHEMBL121192 1 4.70
CHEMBL333026 1 4.05
CHEMBL330996 1 -
CHEMBL332805 1 -
CHEMBL434812 1 -
CHEMBL27064 1 -
CHEMBL30099 1 -
CHEMBL121547 1 -
CHEMBL333641 1 -
CHEMBL30053 1 -
CHEMBL280609 1 -
CHEMBL25908 1 -
CHEMBL29836 1 -
CHEMBL27542 1 -
CHEMBL281022 1 -
CHEMBL120915 1 -
CHEMBL287205 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27233 EC50 = 330.0 nM 6.48
CHEMBL121666 EC50 = 500.0 nM 6.30
CHEMBL30104 EC50 = 550.0 nM 6.26
CHEMBL121442 EC50 = 1600.0 nM 5.80
CHEMBL283395 EC50 = 3000.0 nM 5.52
CHEMBL122716 EC50 = 10000.0 nM 5.00
CHEMBL121192 EC50 = 20000.0 nM 4.70
CHEMBL333026 EC50 = 90000.0 nM 4.05
CHEMBL330996 EC50 > 270000.0 nM -
CHEMBL332805 EC50 > 500000.0 nM -
CHEMBL434812 EC50 > 480000.0 nM -
CHEMBL27064 EC50 > 260000.0 nM -
CHEMBL30099 EC50 > 220000.0 nM -
CHEMBL121547 EC50 > 210000.0 nM -
CHEMBL333641 EC50 > 220000.0 nM -
CHEMBL30053 EC50 > 210000.0 nM -
CHEMBL280609 EC50 > 240000.0 nM -
CHEMBL25908 EC50 > 230000.0 nM -
CHEMBL29836 EC50 > 220000.0 nM -
CHEMBL27542 EC50 > 240000.0 nM -
CHEMBL281022 EC50 > 250000.0 nM -
CHEMBL120915 EC50 = 510000.0 nM -
CHEMBL287205 EC50 > 260000.0 nM -