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Assay Detail

CHEMBL3829047

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

Binding
Inhibition of HDAC in human HeLa cell nuclear extract using Ac-Leu-Gly-Lys (Ac)-AMC as substrate after 30 mins by fluorescence assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HeLa
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Histone deacetylase (CHEMBL2093865)
Type PROTEIN FAMILY
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
IC50 8 8.38 9.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL483254 PANOBINOSTAT 4.0 1 9.08
CHEMBL3827814 1 8.49
CHEMBL3827894 1 8.48
CHEMBL3828518 1 8.47
CHEMBL3827281 1 8.21
CHEMBL3827517 1 8.20
CHEMBL3622533 FIMEPINOSTAT 2.0 1 8.17
CHEMBL98 VORINOSTAT 4.0 1 7.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL483254 PANOBINOSTAT IC50 = 0.83 nM 9.08
CHEMBL3827814 IC50 = 3.2 nM 8.49
CHEMBL3827894 IC50 = 3.3 nM 8.48
CHEMBL3828518 IC50 = 3.4 nM 8.47
CHEMBL3827281 IC50 = 6.1 nM 8.21
CHEMBL3827517 IC50 = 6.3 nM 8.20
CHEMBL3622533 FIMEPINOSTAT IC50 = 6.8 nM 8.17
CHEMBL98 VORINOSTAT IC50 = 11.5 nM 7.94