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Assay Detail

CHEMBL4397965

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

Binding
Inhibition of recombinant human HDAC2 assessed as decrease in deacetylation of FLUOR DE LYS Green substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence based assay
6
Total Activities
6
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 2 (CHEMBL1937)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Thioether-based 2-aminobenzamide derivatives: Novel HDAC inhibitors with potent in vitro and in vivo antitumor activity.
Yun F, Cheng C, Ullah S, He J, Zahi MR, Yuan Q.
Eur J Med Chem (2019) 176 : 195 -207
PubMed 31103900 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.50 6.86

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4437865 1 6.86
CHEMBL4450474 1 6.84
CHEMBL4446236 1 6.69
CHEMBL4087968 1 6.51
CHEMBL4437852 1 6.36
CHEMBL235191 TACEDINALINE 3.0 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4437865 IC50 = 139.0 nM 6.86
CHEMBL4450474 IC50 = 144.0 nM 6.84
CHEMBL4446236 IC50 = 205.0 nM 6.69
CHEMBL4087968 IC50 = 310.0 nM 6.51
CHEMBL4437852 IC50 = 441.0 nM 6.36
CHEMBL235191 TACEDINALINE IC50 = 1920.0 nM 5.72