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Assay Detail

CHEMBL2025280

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

Binding
Inhibition of HDAC6 in human HeLa cell nuclear extract using Fluor de Lys as substrate after 15 mins by fluorometric analysis
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HeLa
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histone deacetylase 6 (CHEMBL1865)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Dual targeting of histone deacetylase and topoisomerase II with novel bifunctional inhibitors.
Guerrant W, Patil V, Canzoneri JC, Oyelere AK.
J Med Chem (2012) 55 : 1465 -1477
PubMed 22260166 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.41 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2023530 1 7.72
CHEMBL2023529 1 7.70
CHEMBL2023526 1 7.70
CHEMBL98 VORINOSTAT 4.0 1 7.57
CHEMBL2023528 1 7.52
CHEMBL2023527 1 6.26
CHEMBL178 DAUNORUBICIN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2023530 IC50 = 19.0 nM 7.72
CHEMBL2023529 IC50 = 20.0 nM 7.70
CHEMBL2023526 IC50 = 20.0 nM 7.70
CHEMBL98 VORINOSTAT IC50 = 27.0 nM 7.57
CHEMBL2023528 IC50 = 30.0 nM 7.52
CHEMBL2023527 IC50 = 555.0 nM 6.26
CHEMBL178 DAUNORUBICIN IC50 - -