Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5053585

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

Binding
Inhibition of human TOP2B assessed as reduction in relaxation of supercoiled DNA using kDNA as substrate incubated for 30 min
3
Total Activities
3
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

Structure-Activity Relationship Study of Dexrazoxane Analogues Reveals ICRF-193 as the Most Potent Bisdioxopiperazine against Anthracycline Toxicity to Cardiomyocytes Due to Its Strong Topoisomerase IIβ Interactions.
Jirkovská A, Karabanovich G, Kubeš J, Skalická V, Melnikova I, Korábečný J, Kučera T, Jirkovský E, Nováková L, Bavlovič Piskáčková H, Škoda J, Štěrba M, Austin CA, Šimůnek T, Roh J.
J Med Chem (2021) 64 : 3997 -4019
PubMed 33750129 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 4.91 5.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5083245 1 5.52
CHEMBL1738 DEXRAZOXANE 4.0 1 4.30
CHEMBL5076925 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5083245 IC50 = 3000.0 nM 5.52
CHEMBL1738 DEXRAZOXANE IC50 = 50000.0 nM 4.30
CHEMBL5076925 IC50 = 505000.0 nM -