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Assay Detail

CHEMBL931622

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

Binding
Inhibition of HDAC3 in HEK293 cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Histone deacetylase 3 (CHEMBL1829)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases.
Jones P, Altamura S, De Francesco R, Gallinari P, Lahm A, Neddermann P, Rowley M, Serafini S, Steinkühler C.
Bioorg Med Chem Lett (2008) 18 : 1814 -1819
PubMed 18308563 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.32 8.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL356066 DACINOSTAT 2.0 1 8.44
CHEMBL430060 APICIDIN 1 8.01
CHEMBL112446 1 8.00
CHEMBL408513 BELINOSTAT 4.0 1 7.34
CHEMBL98 VORINOSTAT 4.0 1 7.24
CHEMBL115011 1 6.92
CHEMBL27759 ENTINOSTAT 3.0 1 6.40
CHEMBL272980 MOCETINOSTAT 2.0 1 6.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL356066 DACINOSTAT IC50 = 3.6 nM 8.44
CHEMBL430060 APICIDIN IC50 = 9.7 nM 8.01
CHEMBL112446 IC50 = 10.0 nM 8.00
CHEMBL408513 BELINOSTAT IC50 = 46.0 nM 7.34
CHEMBL98 VORINOSTAT IC50 = 57.0 nM 7.24
CHEMBL115011 IC50 = 120.0 nM 6.92
CHEMBL27759 ENTINOSTAT IC50 = 400.0 nM 6.40
CHEMBL272980 MOCETINOSTAT IC50 = 610.0 nM 6.21