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Assay Detail

CHEMBL695135

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

Binding
Inhibition of human histone deacetylase (mixture of HDAC1 and HDAC2) prepared from K562 erythroleukemia cells.
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type K562
Confidence 5 — Multiple protein complex / RNA
Curated By Expert

Target

Histone deacetylase (HDAC1 and HDAC2) (CHEMBL2111429)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Trifluoromethyl ketones as inhibitors of histone deacetylase.
Frey RR, Wada CK, Garland RB, Curtin ML, Michaelides MR, Li J, Pease LJ, Glaser KB, Marcotte PA, Bouska JJ, Murphy SS, Davidsen SK.
Bioorg Med Chem Lett (2002) 12 : 3443 -3447
PubMed 12419380 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 5.78 8.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL115812 1 8.04
CHEMBL98 VORINOSTAT 4.0 1 8.00
CHEMBL331158 1 6.52
CHEMBL116702 1 6.51
CHEMBL115011 1 6.42
CHEMBL27759 ENTINOSTAT 3.0 1 5.70
CHEMBL114724 1 5.66
CHEMBL326529 1 5.58
CHEMBL116023 1 5.55
CHEMBL112148 1 5.54
CHEMBL116900 1 5.54
CHEMBL323647 1 5.52
CHEMBL324819 1 5.50
CHEMBL117916 1 5.47
CHEMBL323652 1 5.34
CHEMBL424256 1 5.30
CHEMBL113537 1 5.17
CHEMBL114796 1 5.10
CHEMBL117610 1 5.07
CHEMBL324614 1 4.96
CHEMBL117404 1 4.80
CHEMBL113886 1 -
CHEMBL114725 1 -
CHEMBL116979 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL115812 IC50 = 9.2 nM 8.04
CHEMBL98 VORINOSTAT IC50 = 10.0 nM 8.00
CHEMBL331158 IC50 = 300.0 nM 6.52
CHEMBL116702 IC50 = 310.0 nM 6.51
CHEMBL115011 IC50 = 380.0 nM 6.42
CHEMBL27759 ENTINOSTAT IC50 = 2000.0 nM 5.70
CHEMBL114724 IC50 = 2200.0 nM 5.66
CHEMBL326529 IC50 = 2600.0 nM 5.58
CHEMBL116023 IC50 = 2800.0 nM 5.55
CHEMBL112148 IC50 = 2900.0 nM 5.54
CHEMBL116900 IC50 = 2900.0 nM 5.54
CHEMBL323647 IC50 = 3000.0 nM 5.52
CHEMBL324819 IC50 = 3200.0 nM 5.50
CHEMBL117916 IC50 = 3400.0 nM 5.47
CHEMBL323652 IC50 = 4600.0 nM 5.34
CHEMBL424256 IC50 = 5000.0 nM 5.30
CHEMBL113537 IC50 = 6700.0 nM 5.17
CHEMBL114796 IC50 = 8000.0 nM 5.10
CHEMBL117610 IC50 = 8600.0 nM 5.07
CHEMBL324614 IC50 = 11000.0 nM 4.96
CHEMBL117404 IC50 = 16000.0 nM 4.80
CHEMBL113886 IC50 > 50000.0 nM -
CHEMBL114725 IC50 > 50000.0 nM -
CHEMBL116979 IC50 > 50000.0 nM -