Assay Detail
Binding
CHEMBL1832527
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Competitive inhibition of HDAC8 using KI-104 as substrate by fluorescence assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 7.20 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL483254 | PANOBINOSTAT | 4.0 | 1 | 7.66 |
| CHEMBL408513 | BELINOSTAT | 4.0 | 1 | 7.66 |
| CHEMBL3215861 | — | — | 1 | 7.32 |
| CHEMBL1830420 | — | — | 1 | 7.27 |
| CHEMBL1830536 | — | — | 1 | 7.26 |
| CHEMBL1830422 | — | — | 1 | 7.24 |
| CHEMBL1830397 | — | — | 1 | 7.19 |
| CHEMBL1830396 | — | — | 1 | 7.11 |
| CHEMBL1830537 | — | — | 1 | 7.03 |
| CHEMBL491316 | — | — | 1 | 7.02 |
| CHEMBL1830424 | — | — | 1 | 6.87 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 6.76 |
| CHEMBL460963 | — | — | 1 | - |
| CHEMBL489332 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL483254 | PANOBINOSTAT | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL408513 | BELINOSTAT | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL3215861 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL1830420 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL1830536 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL1830422 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL1830397 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL1830396 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL1830537 | — | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL491316 | — | Ki | = | 95.0 | nM | 7.02 |
| CHEMBL1830424 | — | Ki | = | 136.0 | nM | 6.87 |
| CHEMBL98 | VORINOSTAT | Ki | = | 173.0 | nM | 6.76 |
| CHEMBL460963 | — | Ki | - | — | - | |
| CHEMBL489332 | — | Ki | - | — | - |