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Assay Detail

CHEMBL4382900

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

Binding
Poison activity at recombinant human topoisomerase 2beta using pBR322 plasmid as substrate after 30 mins by ethidium bromide staining based agarose gel electrophoresis
5
Total Activities
5
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-beta (CHEMBL3396)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Novel Topoisomerase II Inhibitors by Medicinal Chemistry Approaches.
Hu W, Huang XS, Wu JF, Yang L, Zheng YT, Shen YM, Li ZY, Li X.
J Med Chem (2018) 61 : 8947 -8980
PubMed 29870668 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.01 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL49442 AMETANTRONE 2.0 1 7.52
CHEMBL4553471 1 5.97
CHEMBL4575796 1 5.94
CHEMBL4448353 1 5.36
CHEMBL4467805 1 5.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL49442 AMETANTRONE IC50 = 30.0 nM 7.52
CHEMBL4553471 IC50 = 1060.0 nM 5.97
CHEMBL4575796 IC50 = 1150.0 nM 5.94
CHEMBL4448353 IC50 = 4340.0 nM 5.36
CHEMBL4467805 IC50 = 5250.0 nM 5.28