Assay Detail
Binding
CHEMBL4397963
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human HDAC3/NCOR1 assessed as decrease in deacetylation of FLUOR DE LYS SIRT1 substrate preincubated for 10 mins followed by substrate addition and 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 | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Thioether-based 2-aminobenzamide derivatives: Novel HDAC inhibitors with potent in vitro and in vivo antitumor activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 6.63 | 6.87 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4446236 | — | — | 1 | 6.87 |
| CHEMBL4450474 | — | — | 1 | 6.67 |
| CHEMBL4087968 | — | — | 1 | 6.63 |
| CHEMBL4437852 | — | — | 1 | 6.56 |
| CHEMBL4437865 | — | — | 1 | 6.42 |
| CHEMBL235191 | TACEDINALINE | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4446236 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL4450474 | — | IC50 | = | 215.0 | nM | 6.67 |
| CHEMBL4087968 | — | IC50 | = | 234.0 | nM | 6.63 |
| CHEMBL4437852 | — | IC50 | = | 274.0 | nM | 6.56 |
| CHEMBL4437865 | — | IC50 | = | 381.0 | nM | 6.42 |
| CHEMBL235191 | TACEDINALINE | IC50 | > | 32000.0 | nM | - |