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Assay Detail

CHEMBL817420

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

Binding
In vitro activity against mammalian topoisomerase II measured as ATP-dependent unknotting of P4 DNA compared to enzyme and DNA control
4
Total Activities
4
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

Antitumor agents. 185. Synthesis and biological evaluation of tridemethylthiocolchicine analogues as novel topoisomerase II inhibitors.
Guan J, Zhu XK, Tachibana Y, Bastow KF, Brossi A, Hamel E, Lee KH.
J Med Chem (1998) 41 : 1956 -1961
PubMed 9599244 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 4.63 5.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL61609 1 5.05
CHEMBL301851 1 4.42
CHEMBL44657 ETOPOSIDE 4.0 1 4.42
CHEMBL61573 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL61609 IC50 = 9000.0 nM 5.05
CHEMBL301851 IC50 = 38000.0 nM 4.42
CHEMBL44657 ETOPOSIDE IC50 = 38000.0 nM 4.42
CHEMBL61573 IC50 > 150000.0 nM -