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Assay Detail

CHEMBL3829048

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

Binding
Inhibition of HDAC6 in human A2780S cells assessed as tubulin acetylation incubated for 6 hrs by cytoblot assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type A2780
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities.
Chen Y, Wang X, Xiang W, He L, Tang M, Wang F, Wang T, Yang Z, Yi Y, Wang H, Niu T, Zheng L, Lei L, Li X, Song H, Chen L.
J Med Chem (2016) 59 : 5488 -5504
PubMed 27186676 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 6.68 6.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3827894 1 6.84
CHEMBL483254 PANOBINOSTAT 4.0 1 6.82
CHEMBL3827517 1 6.73
CHEMBL3827281 1 6.70
CHEMBL3827814 1 6.68
CHEMBL3622533 FIMEPINOSTAT 2.0 1 6.65
CHEMBL3828518 1 6.61
CHEMBL98 VORINOSTAT 4.0 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3827894 EC50 = 143.7 nM 6.84
CHEMBL483254 PANOBINOSTAT EC50 = 150.71 nM 6.82
CHEMBL3827517 EC50 = 187.9 nM 6.73
CHEMBL3827281 EC50 = 198.6 nM 6.70
CHEMBL3827814 EC50 = 211.05 nM 6.68
CHEMBL3622533 FIMEPINOSTAT EC50 = 221.75 nM 6.65
CHEMBL3828518 EC50 = 248.35 nM 6.61
CHEMBL98 VORINOSTAT EC50 = 399.25 nM 6.40