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Assay Detail

CHEMBL4315186

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

Binding
Inhibition of human HDAC1 using Arg-His-Lys-Lys (Ac) as substrate incubated for 2 hrs by fluorescence assay
8
Total Activities
8
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 a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor.
Soumyanarayanan U, Ramanujulu PM, Mustafa N, Haider S, Fang Nee AH, Tong JX, Tan KSW, Chng WJ, Dymock BW.
Eur J Med Chem (2019) 184 : 111755 -111755
PubMed 31627059 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.26 8.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL99 TRICHOSTATIN 1.0 1 8.21
CHEMBL4438378 1 6.63
CHEMBL98 VORINOSTAT 4.0 1 6.51
CHEMBL4554522 1 6.05
CHEMBL4444554 1 5.99
CHEMBL4551593 1 5.67
CHEMBL4572459 1 5.51
CHEMBL4461884 1 5.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL99 TRICHOSTATIN IC50 = 6.22 nM 8.21
CHEMBL4438378 IC50 = 233.0 nM 6.63
CHEMBL98 VORINOSTAT IC50 = 306.0 nM 6.51
CHEMBL4554522 IC50 = 896.0 nM 6.05
CHEMBL4444554 IC50 = 1030.0 nM 5.99
CHEMBL4551593 IC50 = 2150.0 nM 5.67
CHEMBL4572459 IC50 = 3080.0 nM 5.51
CHEMBL4461884 IC50 = 3370.0 nM 5.47