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Assay Detail

CHEMBL923241

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

Binding
Inhibition of human recombinant topoisomerase 2 by decatenation assay
15
Total Activities
15
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 of 1-/2-substituted-[1,2,3]triazolo[4,5-g]phthalazine-4,9-diones and evaluation of their cytotoxicity and topoisomerase II inhibition.
Kim JS, Rhee HK, Park HJ, Lee SK, Lee CO, Park Choo HY.
Bioorg Med Chem (2008) 16 : 4545 -4550
PubMed 18321715 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 4.34 4.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL261294 1 4.71
CHEMBL259225 1 4.54
CHEMBL261341 1 4.53
CHEMBL260224 1 4.48
CHEMBL259778 1 4.41
CHEMBL260541 1 4.37
CHEMBL261330 1 4.35
CHEMBL258925 1 4.31
CHEMBL259990 1 4.28
CHEMBL261342 1 4.26
CHEMBL406853 1 4.25
CHEMBL259989 1 4.25
CHEMBL261876 1 4.21
CHEMBL260223 1 4.19
CHEMBL44657 ETOPOSIDE 4.0 1 4.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL261294 IC50 = 19400.0 nM 4.71
CHEMBL259225 IC50 = 28600.0 nM 4.54
CHEMBL261341 IC50 = 29800.0 nM 4.53
CHEMBL260224 IC50 = 33300.0 nM 4.48
CHEMBL259778 IC50 = 39000.0 nM 4.41
CHEMBL260541 IC50 = 43200.0 nM 4.37
CHEMBL261330 IC50 = 44400.0 nM 4.35
CHEMBL258925 IC50 = 49000.0 nM 4.31
CHEMBL259990 IC50 = 52800.0 nM 4.28
CHEMBL261342 IC50 = 54500.0 nM 4.26
CHEMBL406853 IC50 = 55600.0 nM 4.25
CHEMBL259989 IC50 = 55600.0 nM 4.25
CHEMBL261876 IC50 = 61500.0 nM 4.21
CHEMBL260223 IC50 = 64800.0 nM 4.19
CHEMBL44657 ETOPOSIDE IC50 = 92900.0 nM 4.03