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Assay Detail

CHEMBL828694

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

Binding
In vitro inhibitory concentration against histone deacetylase of DU-145 prostate cell nuclear extract as deacetylation of biotinylated [3H]-acetyl histone H4 peptide
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Histone deacetylase (CHEMBL2093865)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Structure-based optimization of phenylbutyrate-derived histone deacetylase inhibitors.
Lu Q, Wang DS, Chen CS, Hu YD, Chen CS.
J Med Chem (2005) 48 : 5530 -5535
PubMed 16107152 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.99 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL191482 AR-42 2.0 1 7.80
CHEMBL189137 1 7.60
CHEMBL191091 1 7.52
CHEMBL188270 1 7.47
CHEMBL143336 1 7.36
CHEMBL189929 1 7.27
CHEMBL189497 1 7.17
CHEMBL191483 1 7.08
CHEMBL190727 1 7.01
CHEMBL189912 1 6.96
CHEMBL356824 1 6.80
CHEMBL191227 1 6.68
CHEMBL190014 1 6.60
CHEMBL347734 1 6.28
CHEMBL190359 1 6.28
CHEMBL142048 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL191482 AR-42 IC50 = 16.0 nM 7.80
CHEMBL189137 IC50 = 25.0 nM 7.60
CHEMBL191091 IC50 = 30.0 nM 7.52
CHEMBL188270 IC50 = 34.0 nM 7.47
CHEMBL143336 IC50 = 44.0 nM 7.36
CHEMBL189929 IC50 = 54.0 nM 7.27
CHEMBL189497 IC50 = 68.0 nM 7.17
CHEMBL191483 IC50 = 84.0 nM 7.08
CHEMBL190727 IC50 = 98.0 nM 7.01
CHEMBL189912 IC50 = 110.0 nM 6.96
CHEMBL356824 IC50 = 157.0 nM 6.80
CHEMBL191227 IC50 = 210.0 nM 6.68
CHEMBL190014 IC50 = 250.0 nM 6.60
CHEMBL347734 IC50 = 530.0 nM 6.28
CHEMBL190359 IC50 = 520.0 nM 6.28
CHEMBL142048 IC50 = 1200.0 nM 5.92