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Assay Detail

CHEMBL5543336

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

Binding
Inhibition of human recombinant HDAC1 using Ac-RHKK(Acetyl)-AMC peptide as fluorogenic substrate pre-incubated for 30 mins followed by substrate addition and measured for 60 mins by fluorescence based analysis
6
Total Activities
6
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

Histone deacetylase 1 (CHEMBL325)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Technologies of targeting histone deacetylase in drug discovery: Current progress and emerging prospects.
Ru J, Wang Y, Li Z, Wang J, Ren C, Zhang J.
Eur J Med Chem (2023) 261 : 115800 -115800
PubMed 37708798 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.79 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4788954 1 8.70
CHEMBL4460552 1 8.40
CHEMBL4597954 1 8.30
CHEMBL4635479 1 7.35
CHEMBL5201623 1 7.09
CHEMBL5570728 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4788954 IC50 = 2.0 nM 8.70
CHEMBL4460552 IC50 = 4.0 nM 8.40
CHEMBL4597954 IC50 = 5.0 nM 8.30
CHEMBL4635479 IC50 = 45.0 nM 7.35
CHEMBL5201623 IC50 = 82.0 nM 7.09
CHEMBL5570728 IC50 = 130.0 nM 6.89