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Assay Detail

CHEMBL693166

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

Binding
Inhibitory activity against histone deacetylase (HDAC1 and HDAC2) isolated from K562 erythroleukemia cells
28
Total Activities
28
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

A novel series of histone deacetylase inhibitors incorporating hetero aromatic ring systems as connection units.
Dai Y, Guo Y, Curtin ML, Li J, Pease LJ, Guo J, Marcotte PA, Glaser KB, Davidsen SK, Michaelides MR.
Bioorg Med Chem Lett (2003) 13 : 3817 -3820
PubMed 14552787 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 7.64 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL123626 1 8.68
CHEMBL124282 1 8.60
CHEMBL339720 1 8.57
CHEMBL340885 1 8.37
CHEMBL435415 1 8.37
CHEMBL123905 1 8.36
CHEMBL125042 1 8.24
CHEMBL124650 1 8.17
CHEMBL340835 1 8.07
CHEMBL127846 1 8.01
CHEMBL340113 1 7.96
CHEMBL126274 1 7.96
CHEMBL339796 1 7.92
CHEMBL127184 1 7.89
CHEMBL124909 1 7.72
CHEMBL339534 1 7.68
CHEMBL338776 1 7.64
CHEMBL127269 1 7.52
CHEMBL126273 1 7.38
CHEMBL127360 1 7.33
CHEMBL125098 1 7.24
CHEMBL123506 1 7.13
CHEMBL124593 1 7.05
CHEMBL98 VORINOSTAT 4.0 1 6.85
CHEMBL124322 1 6.48
CHEMBL112211 1 6.47
CHEMBL123624 1 6.25
CHEMBL57107 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL123626 IC50 = 2.1 nM 8.68
CHEMBL124282 IC50 = 2.5 nM 8.60
CHEMBL339720 IC50 = 2.7 nM 8.57
CHEMBL340885 IC50 = 4.3 nM 8.37
CHEMBL435415 IC50 = 4.3 nM 8.37
CHEMBL123905 IC50 = 4.4 nM 8.36
CHEMBL125042 IC50 = 5.8 nM 8.24
CHEMBL124650 IC50 = 6.8 nM 8.17
CHEMBL340835 IC50 = 8.5 nM 8.07
CHEMBL127846 IC50 = 9.8 nM 8.01
CHEMBL340113 IC50 = 11.0 nM 7.96
CHEMBL126274 IC50 = 11.0 nM 7.96
CHEMBL339796 IC50 = 12.0 nM 7.92
CHEMBL127184 IC50 = 13.0 nM 7.89
CHEMBL124909 IC50 = 19.0 nM 7.72
CHEMBL339534 IC50 = 21.0 nM 7.68
CHEMBL338776 IC50 = 23.0 nM 7.64
CHEMBL127269 IC50 = 30.0 nM 7.52
CHEMBL126273 IC50 = 42.0 nM 7.38
CHEMBL127360 IC50 = 47.0 nM 7.33
CHEMBL125098 IC50 = 58.0 nM 7.24
CHEMBL123506 IC50 = 74.0 nM 7.13
CHEMBL124593 IC50 = 89.0 nM 7.05
CHEMBL98 VORINOSTAT IC50 = 140.0 nM 6.85
CHEMBL124322 IC50 = 330.0 nM 6.48
CHEMBL112211 IC50 = 340.0 nM 6.47
CHEMBL123624 IC50 = 560.0 nM 6.25
CHEMBL57107 IC50 = 1010.0 nM 6.00