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Assay Detail

CHEMBL3778475

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

Binding
Inhibition of human recombinant HDAC1 using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histone deacetylase 1 (CHEMBL325)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
Yang Z, Wang T, Wang F, Niu T, Liu Z, Chen X, Long C, Tang M, Cao D, Wang X, Xiang W, Yi Y, Ma L, You J, Chen L.
J Med Chem (2016) 59 : 1455 -1470
PubMed 26443078 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 6.95 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL483254 PANOBINOSTAT 4.0 1 9.00
CHEMBL98 VORINOSTAT 4.0 1 7.96
CHEMBL2364628 RICOLINOSTAT 2.0 1 7.42
CHEMBL3775539 1 7.14
CHEMBL3775209 1 7.12
CHEMBL3775662 1 7.08
CHEMBL3775072 1 6.92
CHEMBL3774890 1 6.80
CHEMBL3775521 1 6.76
CHEMBL3774993 1 6.75
CHEMBL3775269 1 6.71
CHEMBL3775817 1 6.69
CHEMBL3774858 1 6.69
CHEMBL3774691 1 6.67
CHEMBL3774793 1 6.62
CHEMBL3775654 1 6.60
CHEMBL3775581 1 6.58
CHEMBL3775409 1 6.57
CHEMBL3774994 1 6.51
CHEMBL3774414 1 6.38
CHEMBL3774877 1 -
CHEMBL3775457 1 -
CHEMBL3775009 1 -
CHEMBL3774413 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL483254 PANOBINOSTAT IC50 = 1.0 nM 9.00
CHEMBL98 VORINOSTAT IC50 = 11.0 nM 7.96
CHEMBL2364628 RICOLINOSTAT IC50 = 38.0 nM 7.42
CHEMBL3775539 IC50 = 73.0 nM 7.14
CHEMBL3775209 IC50 = 76.0 nM 7.12
CHEMBL3775662 IC50 = 84.0 nM 7.08
CHEMBL3775072 IC50 = 120.0 nM 6.92
CHEMBL3774890 IC50 = 160.0 nM 6.80
CHEMBL3775521 IC50 = 172.0 nM 6.76
CHEMBL3774993 IC50 = 176.0 nM 6.75
CHEMBL3775269 IC50 = 195.0 nM 6.71
CHEMBL3775817 IC50 = 204.0 nM 6.69
CHEMBL3774858 IC50 = 203.0 nM 6.69
CHEMBL3774691 IC50 = 212.0 nM 6.67
CHEMBL3774793 IC50 = 242.0 nM 6.62
CHEMBL3775654 IC50 = 253.0 nM 6.60
CHEMBL3775581 IC50 = 264.0 nM 6.58
CHEMBL3775409 IC50 = 272.0 nM 6.57
CHEMBL3774994 IC50 = 306.0 nM 6.51
CHEMBL3774414 IC50 = 422.0 nM 6.38
CHEMBL3774877 IC50 > 1000.0 nM -
CHEMBL3775457 IC50 > 1000.0 nM -
CHEMBL3775009 IC50 > 1000.0 nM -
CHEMBL3774413 IC50 > 1000.0 nM -