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Assay Detail

CHEMBL929247

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

Binding
Displacement of fluorescent 5-(3-(3-(4-((4-((7-(hydroxyamino)-7-oxoheptyl)carbamoyl)phenylamino)methyl)-1H-1,2,3-triazol-1-yl)propyl)thioureido)-2-(3-hydroxy-6-oxo-6H-xanthen-9-yl)benzoic acid from HDAC in human HeLa nuclear cell extract by fluorescence polarization assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Histone deacetylase (CHEMBL2093865)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Development of a fluorescence polarization based assay for histone deacetylase ligand discovery.
Mazitschek R, Patel V, Wirth DF, Clardy J.
Bioorg Med Chem Lett (2008) 18 : 2809 -2812
PubMed 18430569 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.75 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL99 TRICHOSTATIN 1.0 1 8.82
CHEMBL430060 APICIDIN 1 8.10
CHEMBL98 VORINOSTAT 4.0 1 7.62
CHEMBL260653 1 7.24
CHEMBL343448 ROMIDEPSIN 4.0 1 6.97
CHEMBL86537 SPLITOMICIN 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL99 TRICHOSTATIN IC50 = 1.5 nM 8.82
CHEMBL430060 APICIDIN IC50 = 8.0 nM 8.10
CHEMBL98 VORINOSTAT IC50 = 23.9 nM 7.62
CHEMBL260653 IC50 = 58.0 nM 7.24
CHEMBL343448 ROMIDEPSIN IC50 = 107.2 nM 6.97
CHEMBL86537 SPLITOMICIN IC50 > 75000.0 nM -