Assay Detail
Binding
CHEMBL3240085
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of trypsin-like activity of human 20S proteasome using Ac-RLR-AMC as substrate
13
Total Activities
13
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
Structurally novel highly potent proteasome inhibitors created by the structure-based hybridization of nonpeptidic belactosin derivatives and peptide boronates.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 5.63 | 5.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3237862 | — | — | 1 | 5.96 |
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 5.70 |
| CHEMBL3237873 | — | — | 1 | 5.66 |
| CHEMBL3237865 | — | — | 1 | 5.62 |
| CHEMBL3237866 | — | — | 1 | 5.60 |
| CHEMBL3237863 | — | — | 1 | 5.57 |
| CHEMBL3237864 | — | — | 1 | 5.57 |
| CHEMBL3237869 | — | — | 1 | 5.57 |
| CHEMBL3237867 | — | — | 1 | 5.52 |
| CHEMBL3237870 | — | — | 1 | 5.48 |
| CHEMBL3237868 | — | — | 1 | - |
| CHEMBL3237871 | — | — | 1 | - |
| CHEMBL3237872 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3237862 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL325041 | BORTEZOMIB | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3237873 | — | IC50 | = | 2170.0 | nM | 5.66 |
| CHEMBL3237865 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL3237866 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3237863 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL3237864 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL3237869 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL3237867 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL3237870 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL3237868 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3237871 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3237872 | — | IC50 | > | 10000.0 | nM | - |