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Assay Detail

CHEMBL4156659

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

Binding
Inhibition of human DNA topoisomerase 2beta after 2 hrs by ELISA
7
Total Activities
7
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

Design, synthesis and screening of 1, 2, 4-triazinone derivatives as potential antitumor agents with apoptosis inducing activity on MCF-7 breast cancer cell line.
Zaki I, Abdelhameid MK, El-Deen IM, Abdel Wahab AHA, Ashmawy AM, Mohamed KO.
Eur J Med Chem (2018) 156 : 563 -579
PubMed 30025350 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.46 8.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4161876 1 8.16
CHEMBL4174756 1 7.90
CHEMBL4160802 1 7.50
CHEMBL44657 ETOPOSIDE 4.0 1 7.16
CHEMBL4172196 1 7.09
CHEMBL4169404 1 6.96
CHEMBL61 PODOFILOX 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4161876 IC50 = 6.85 nM 8.16
CHEMBL4174756 IC50 = 12.6 nM 7.90
CHEMBL4160802 IC50 = 31.68 nM 7.50
CHEMBL44657 ETOPOSIDE IC50 = 69.8 nM 7.16
CHEMBL4172196 IC50 = 81.42 nM 7.09
CHEMBL4169404 IC50 = 110.45 nM 6.96
CHEMBL61 PODOFILOX IC50 - -