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Assay Detail

CHEMBL4141503

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

Binding
Inhibition of human recombinant full-length HDAC1 (1 to 482 residues) expressed in baculovirus using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay
5
Total Activities
5
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

Discovery of a fluorescent probe with HDAC6 selective inhibition.
Zhang Y, Yan J, Yao TP.
Eur J Med Chem (2017) 141 : 596 -602
PubMed 29102179 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.92 8.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4160632 1 8.28
CHEMBL4176291 1 7.44
CHEMBL98 VORINOSTAT 4.0 1 7.16
CHEMBL2018302 TUBASTATIN A 1 4.79
CHEMBL4165684 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4160632 IC50 = 5.25 nM 8.28
CHEMBL4176291 IC50 = 36.2 nM 7.44
CHEMBL98 VORINOSTAT IC50 = 69.0 nM 7.16
CHEMBL2018302 TUBASTATIN A IC50 = 16400.0 nM 4.79
CHEMBL4165684 IC50 > 20000.0 nM -