Assay Detail
Binding
CHEMBL4397984
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Inhibition of HDAC in human HeLa cell nuclear extract 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 |
| Cell Type | HeLa |
| Confidence | 5 — Multiple protein complex / RNA |
| 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 | 5.62 | 6.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4087968 | — | — | 1 | 6.05 |
| CHEMBL235191 | TACEDINALINE | 3.0 | 1 | 5.74 |
| CHEMBL4437852 | — | — | 1 | 5.70 |
| CHEMBL4437865 | — | — | 1 | 4.97 |
| CHEMBL4446236 | — | — | 1 | - |
| CHEMBL4450474 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4087968 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL235191 | TACEDINALINE | IC50 | = | 1810.0 | nM | 5.74 |
| CHEMBL4437852 | — | IC50 | = | 1995.0 | nM | 5.70 |
| CHEMBL4437865 | — | IC50 | = | 10720.0 | nM | 4.97 |
| CHEMBL4446236 | — | IC50 | > | 32000.0 | nM | - |
| CHEMBL4450474 | — | IC50 | > | 32000.0 | nM | - |