Assay Detail
Binding
CHEMBL3240084
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of caspase-like activity of human 20S proteasome using Ac-nLPnLD-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 | 6.79 | 7.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3237867 | — | — | 1 | 7.34 |
| CHEMBL3237865 | — | — | 1 | 7.12 |
| CHEMBL3237866 | — | — | 1 | 7.12 |
| CHEMBL3237864 | — | — | 1 | 6.92 |
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 6.92 |
| CHEMBL3237869 | — | — | 1 | 6.89 |
| CHEMBL3237862 | — | — | 1 | 6.85 |
| CHEMBL3237863 | — | — | 1 | 6.82 |
| CHEMBL3237873 | — | — | 1 | 6.77 |
| CHEMBL3237870 | — | — | 1 | 6.68 |
| CHEMBL3237868 | — | — | 1 | 6.60 |
| CHEMBL3237872 | — | — | 1 | 6.30 |
| CHEMBL3237871 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3237867 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL3237865 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL3237866 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL3237864 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL325041 | BORTEZOMIB | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3237869 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3237862 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3237863 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3237873 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3237870 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL3237868 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL3237872 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3237871 | — | IC50 | = | 1000.0 | nM | 6.00 |