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Assay Detail

CHEMBL900121

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

Binding
Inhibition of human recombinant HDAC1
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity.
Moradei OM, Mallais TC, Frechette S, Paquin I, Tessier PE, Leit SM, Fournel M, Bonfils C, Trachy-Bourget MC, Liu J, Yan TP, Lu AH, Rahil J, Wang J, Lefebvre S, Li Z, Vaisburg AF, Besterman JM.
J Med Chem (2007) 50 : 5543 -5546
PubMed 17941625 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.93 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL356066 DACINOSTAT 2.0 1 8.10
CHEMBL235674 1 7.70
CHEMBL235413 1 7.40
CHEMBL235842 1 7.40
CHEMBL235192 1 7.30
CHEMBL399388 1 7.30
CHEMBL237584 1 7.30
CHEMBL235210 1 7.30
CHEMBL392747 1 7.22
CHEMBL393242 1 7.22
CHEMBL235411 1 6.52
CHEMBL211625 1 6.36
CHEMBL27759 ENTINOSTAT 3.0 1 6.27
CHEMBL235191 TACEDINALINE 3.0 1 6.05
CHEMBL236061 1 5.70
CHEMBL236060 1 5.70
CHEMBL399389 1 -
CHEMBL235194 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL356066 DACINOSTAT IC50 = 8.0 nM 8.10
CHEMBL235674 IC50 = 20.0 nM 7.70
CHEMBL235413 IC50 = 40.0 nM 7.40
CHEMBL235842 IC50 = 40.0 nM 7.40
CHEMBL235192 IC50 = 50.0 nM 7.30
CHEMBL399388 IC50 = 50.0 nM 7.30
CHEMBL237584 IC50 = 50.0 nM 7.30
CHEMBL235210 IC50 = 50.0 nM 7.30
CHEMBL392747 IC50 = 60.0 nM 7.22
CHEMBL393242 IC50 = 60.0 nM 7.22
CHEMBL235411 IC50 = 300.0 nM 6.52
CHEMBL211625 IC50 = 440.0 nM 6.36
CHEMBL27759 ENTINOSTAT IC50 = 540.0 nM 6.27
CHEMBL235191 TACEDINALINE IC50 = 900.0 nM 6.05
CHEMBL236061 IC50 = 2000.0 nM 5.70
CHEMBL236060 IC50 = 2000.0 nM 5.70
CHEMBL399389 IC50 > 10000.0 nM -
CHEMBL235194 IC50 > 10000.0 nM -