Assay Detail
Binding
CHEMBL5735577
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Enzyme Assay: The inhibitory activity of panobinostat dissolved in DMSO and that of the HP-β-CD panobinostat adduct (prepared as described in Example 1) were compared against HDAC types 1-11. Both were tested in singlicate 10-dose IC50 mode with 3-fold serial dilution starting at 10 μM against 11 HDACs.
9
Total Activities
3
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Cyclodextrin-panobinostat adduct
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 5.58 | 5.86 |
| kon | 3 | - | - |
| k_off | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5794018 | — | — | 3 | 5.86 |
| CHEMBL483254 | PANOBINOSTAT | 4.0 | 3 | 5.78 |
| CHEMBL99 | TRICHOSTATIN | 1.0 | 3 | 5.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5794018 | — | IC50 | = | 1380.0 | nM | 5.86 |
| CHEMBL483254 | PANOBINOSTAT | IC50 | = | 1670.0 | nM | 5.78 |
| CHEMBL99 | TRICHOSTATIN | IC50 | = | 7890.0 | nM | 5.10 |
| CHEMBL5794018 | — | kon | = | - | — | - |
| CHEMBL5794018 | — | k_off | = | - | s-1 | - |
| CHEMBL483254 | PANOBINOSTAT | kon | = | - | — | - |
| CHEMBL483254 | PANOBINOSTAT | k_off | = | - | s-1 | - |
| CHEMBL99 | TRICHOSTATIN | kon | = | - | — | - |
| CHEMBL99 | TRICHOSTATIN | k_off | = | - | s-1 | - |