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Assay Detail

CHEMBL666727

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

Binding
Inhibitory concentration against relaxation activity of DNA topoisomerase II by detecting the conversion of supercoiled pBR322 DNA to its relaxed form
3
Total Activities
3
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

Inhibitory activities against topoisomerase I and II by polyhydroxybenzoyl amide derivatives and their structure-activity relationship.
Abdel-Aziz M, Matsuda K, Otsuka M, Uyeda M, Okawara T, Suzuki K.
Bioorg Med Chem Lett (2004) 14 : 1669 -1672
PubMed 15026047 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.18 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL47027 1 8.05
CHEMBL47885 1 6.82
CHEMBL47526 1 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL47027 IC50 = 9.0 nM 8.05
CHEMBL47885 IC50 = 150.0 nM 6.82
CHEMBL47526 IC50 = 220.0 nM 6.66