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Assay Detail

CHEMBL4005965

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

Binding
Inhibition of human topoisomerase-2alpha-mediated relaxation of supercoiled pBR322 DNA after 1 hr by ethidium bromide staining based agarose gel electrophoresis
13
Total Activities
13
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

Naphthalene diimide-polyamine hybrids as antiproliferative agents: Focus on the architecture of the polyamine chains.
Milelli A, Marchetti C, Greco ML, Moraca F, Costa G, Turrini E, Catanzaro E, Betari N, Calcabrini C, Sissi C, Alcaro S, Fimognari C, Tumiatti V, Minarini A.
Eur J Med Chem (2017) 128 : 107 -122
PubMed 28157593 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.37 5.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4084089 1 5.82
CHEMBL4091846 1 5.66
CHEMBL4084827 1 5.26
CHEMBL583073 1 5.22
CHEMBL4064888 1 5.16
CHEMBL4092588 1 5.09
CHEMBL4102073 1 -
CHEMBL4100323 1 -
CHEMBL4073484 1 -
CHEMBL4074553 1 -
CHEMBL4095021 1 -
CHEMBL4102784 1 -
CHEMBL4103711 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4084089 IC50 = 1500.0 nM 5.82
CHEMBL4091846 IC50 = 2200.0 nM 5.66
CHEMBL4084827 IC50 = 5500.0 nM 5.26
CHEMBL583073 IC50 = 6000.0 nM 5.22
CHEMBL4064888 IC50 = 7000.0 nM 5.16
CHEMBL4092588 IC50 = 8100.0 nM 5.09
CHEMBL4102073 IC50 - -
CHEMBL4100323 IC50 - -
CHEMBL4073484 IC50 - -
CHEMBL4074553 IC50 - -
CHEMBL4095021 IC50 - -
CHEMBL4102784 IC50 - -
CHEMBL4103711 IC50 - -