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Assay Detail

CHEMBL4017637

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

Binding
Inhibition of human topoisomerase 2alpha-mediated kinetoplast DNA decatenation after 60 mins by ethidium bromide staining based agarose gel electrophoresis
9
Total Activities
9
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

Indenocinnoline derivatives as G-quadruplex binders, topoisomerase IIα inhibitors and antiproliferative agents.
Zoidis G, Sosic A, Da Ros S, Gatto B, Sissi C, Palluotto F, Carotti A, Catto M.
Bioorg Med Chem (2017) 25 : 2625 -2634
PubMed 28342691 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 4.99 5.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53463 DOXORUBICIN 4.0 1 5.52
CHEMBL4090898 1 5.31
CHEMBL4066762 1 5.26
CHEMBL4062965 1 5.15
CHEMBL4064044 1 4.87
CHEMBL4093358 1 4.54
CHEMBL4094285 1 4.28
CHEMBL4082118 1 -
CHEMBL127717 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53463 DOXORUBICIN IC50 = 3000.0 nM 5.52
CHEMBL4090898 IC50 = 4880.0 nM 5.31
CHEMBL4066762 IC50 = 5440.0 nM 5.26
CHEMBL4062965 IC50 = 7080.0 nM 5.15
CHEMBL4064044 IC50 = 13400.0 nM 4.87
CHEMBL4093358 IC50 = 29060.0 nM 4.54
CHEMBL4094285 IC50 = 52890.0 nM 4.28
CHEMBL4082118 IC50 > 100000.0 nM -
CHEMBL127717 IC50 > 100000.0 nM -