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Assay Detail

CHEMBL3875255

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

Binding
Inhibition of human DNA topoisomerase 2alpha-mediated decatenation of kinetoplast DNA after 60 mins by agarose gel electrophoresis
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

DNA topoisomerase 2-alpha (CHEMBL1806)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Quinolino[3,4-b]quinoxalines and pyridazino[4,3-c]quinoline derivatives: Synthesis, inhibition of topoisomerase IIα, G-quadruplex binding and cytotoxic properties.
Palluotto F, Sosic A, Pinato O, Zoidis G, Catto M, Sissi C, Gatto B, Carotti A.
Eur J Med Chem (2016) 123 : 704 -717
PubMed 27521587 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 4.70 5.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53463 DOXORUBICIN 4.0 1 5.52
CHEMBL3883611 1 5.29
CHEMBL3884560 1 4.95
CHEMBL3883967 1 4.86
CHEMBL3885093 1 4.75
CHEMBL3885280 1 4.71
CHEMBL3883774 1 4.71
CHEMBL3884844 1 4.62
CHEMBL3884562 1 4.46
CHEMBL3883657 1 4.45
CHEMBL3884650 1 4.06
CHEMBL3883595 1 4.00
CHEMBL3883370 1 -
CHEMBL3883394 1 -
CHEMBL3883473 1 -
CHEMBL3885393 1 -
CHEMBL3884054 1 -
CHEMBL3883419 1 -
CHEMBL3883499 1 -
CHEMBL3883996 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53463 DOXORUBICIN IC50 = 3000.0 nM 5.52
CHEMBL3883611 IC50 = 5140.0 nM 5.29
CHEMBL3884560 IC50 = 11250.0 nM 4.95
CHEMBL3883967 IC50 = 13900.0 nM 4.86
CHEMBL3885093 IC50 = 17750.0 nM 4.75
CHEMBL3885280 IC50 = 19440.0 nM 4.71
CHEMBL3883774 IC50 = 19500.0 nM 4.71
CHEMBL3884844 IC50 = 23770.0 nM 4.62
CHEMBL3884562 IC50 = 34330.0 nM 4.46
CHEMBL3883657 IC50 = 35650.0 nM 4.45
CHEMBL3884650 IC50 = 87580.0 nM 4.06
CHEMBL3883595 IC50 = 100000.0 nM 4.00
CHEMBL3883370 IC50 > 100000.0 nM -
CHEMBL3883394 IC50 > 100000.0 nM -
CHEMBL3883473 IC50 > 100000.0 nM -
CHEMBL3885393 IC50 > 100000.0 nM -
CHEMBL3884054 IC50 > 100000.0 nM -
CHEMBL3883419 IC50 > 100000.0 nM -
CHEMBL3883499 IC50 > 100000.0 nM -
CHEMBL3883996 IC50 > 100000.0 nM -