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Assay Detail

CHEMBL697246

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Binding
Inhibition of histone deacetylase (HDAC) activity in HeLa cell nuclear extract
14
Total Activities
14
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

Stereodefined and polyunsaturated inhibitors of histone deacetylase based on (2E,4E)-5-arylpenta-2,4-dienoic acid hydroxyamides.
Marson CM, Serradji N, Rioja AS, Gastaud SP, Alao JP, Coombes RC, Vigushin DM.
Bioorg Med Chem Lett (2004) 14 : 2477 -2481
PubMed 15109636 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.40 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL99 TRICHOSTATIN 1.0 1 8.30
CHEMBL316183 1 7.31
CHEMBL82931 1 7.13
CHEMBL314643 1 6.76
CHEMBL312098 1 6.60
CHEMBL84395 1 6.55
CHEMBL81522 1 6.52
CHEMBL82989 1 6.10
CHEMBL312400 1 5.93
CHEMBL83750 1 5.77
CHEMBL314389 OXAMFLATIN 1 5.70
CHEMBL84288 1 5.59
CHEMBL82382 1 4.98
CHEMBL312253 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL99 TRICHOSTATIN IC50 = 5.0 nM 8.30
CHEMBL316183 IC50 = 49.0 nM 7.31
CHEMBL82931 IC50 = 74.0 nM 7.13
CHEMBL314643 IC50 = 172.0 nM 6.76
CHEMBL312098 IC50 = 252.0 nM 6.60
CHEMBL84395 IC50 = 279.0 nM 6.55
CHEMBL81522 IC50 = 302.0 nM 6.52
CHEMBL82989 IC50 = 788.0 nM 6.10
CHEMBL312400 IC50 = 1170.0 nM 5.93
CHEMBL83750 IC50 = 1700.0 nM 5.77
CHEMBL314389 OXAMFLATIN IC50 = 2000.0 nM 5.70
CHEMBL84288 IC50 = 2580.0 nM 5.59
CHEMBL82382 IC50 = 10400.0 nM 4.98
CHEMBL312253 IC50 > 100000.0 nM -