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Assay Detail

CHEMBL669720

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

Binding
In vitro 50% inhibition of topoisomerase II mediated k-DNA decatenation
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

9-substituted acridine derivatives with long half-life and potent antitumor activity: synthesis and structure-activity relationships.
Su TL, Chou TC, Kim JY, Huang JT, Ciszewska G, Ren WY, Otter GM, Sirotnak FM, Watanabe KA.
J Med Chem (1995) 38 : 3226 -3235
PubMed 7650675 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 5.71 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL108283 1 7.70
CHEMBL326664 1 7.35
CHEMBL322325 1 7.27
CHEMBL325543 1 7.20
CHEMBL108404 1 6.94
CHEMBL325588 1 6.65
CHEMBL321473 1 6.00
CHEMBL43 AMSACRINE 4.0 1 6.00
CHEMBL111592 1 5.53
CHEMBL111261 1 4.70
CHEMBL326274 1 4.70
CHEMBL322491 1 4.70
CHEMBL320354 1 4.70
CHEMBL109942 1 4.70
CHEMBL111735 1 4.30
CHEMBL320495 1 4.30
CHEMBL109880 1 4.30
CHEMBL444329 1 -
CHEMBL111502 1 -
CHEMBL109534 1 -
CHEMBL109922 1 -
CHEMBL108493 1 -
CHEMBL109928 1 -
CHEMBL109743 1 -
CHEMBL109468 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL108283 IC50 = 20.0 nM 7.70
CHEMBL326664 IC50 = 45.0 nM 7.35
CHEMBL322325 IC50 = 54.0 nM 7.27
CHEMBL325543 IC50 = 63.0 nM 7.20
CHEMBL108404 IC50 = 116.0 nM 6.94
CHEMBL325588 IC50 = 226.0 nM 6.65
CHEMBL321473 IC50 = 1000.0 nM 6.00
CHEMBL43 AMSACRINE IC50 = 1000.0 nM 6.00
CHEMBL111592 IC50 = 2970.0 nM 5.53
CHEMBL111261 IC50 = 20000.0 nM 4.70
CHEMBL326274 IC50 = 20000.0 nM 4.70
CHEMBL322491 IC50 = 20000.0 nM 4.70
CHEMBL320354 IC50 = 20000.0 nM 4.70
CHEMBL109942 IC50 = 20000.0 nM 4.70
CHEMBL111735 IC50 = 50000.0 nM 4.30
CHEMBL320495 IC50 = 50000.0 nM 4.30
CHEMBL109880 IC50 = 50000.0 nM 4.30
CHEMBL444329 IC50 < 1000.0 nM -
CHEMBL111502 IC50 > 100000.0 nM -
CHEMBL109534 IC50 > 100000.0 nM -
CHEMBL109922 IC50 > 100000.0 nM -
CHEMBL108493 IC50 > 100000.0 nM -
CHEMBL109928 IC50 < 1000.0 nM -
CHEMBL109743 IC50 > 100000.0 nM -
CHEMBL109468 IC50 > 100000.0 nM -