Assay Detail
Binding
CHEMBL4158925
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Inhibition of chymotrypsin-like activity of 20S proteasome in human SEM cells using Suc-LLVY aminoluciferin as substrate after 2 hrs by proteasome-Glo assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SEM |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 7.38 | 8.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 8.35 |
| CHEMBL4167623 | — | — | 1 | 6.40 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | - |
| CHEMBL2364628 | RICOLINOSTAT | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL325041 | BORTEZOMIB | IC50 | = | 4.43 | nM | 8.35 |
| CHEMBL4167623 | — | IC50 | = | 394.2 | nM | 6.40 |
| CHEMBL98 | VORINOSTAT | IC50 | > | 25000.0 | nM | - |
| CHEMBL2364628 | RICOLINOSTAT | IC50 | > | 25000.0 | nM | - |