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Assay Detail

CHEMBL1815165

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

Binding
Inhibition of human topoisomerase 2 alpha-mediated relaxation of supercoiled pBR322 DNA after 30 mins by agarose gel electrophoresis
4
Total Activities
4
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

Synthesis and evaluation of mansonone F derivatives as topoisomerase inhibitors.
Wu WB, Ou JB, Huang ZH, Chen SB, Ou TM, Tan JH, Li D, Shen LL, Huang SL, Gu LQ, Huang ZS.
Eur J Med Chem (2011) 46 : 3339 -3347
PubMed 21600681 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.27 5.81

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1812144 1 5.81
CHEMBL1812139 1 5.73
CHEMBL1812137 1 5.31
CHEMBL44657 ETOPOSIDE 4.0 1 4.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1812144 IC50 = 1540.0 nM 5.81
CHEMBL1812139 IC50 = 1880.0 nM 5.73
CHEMBL1812137 IC50 = 4880.0 nM 5.31
CHEMBL44657 ETOPOSIDE IC50 = 60300.0 nM 4.22