Assay Detail
Binding
CHEMBL3240083
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Inhibition of chymotrypsin-like activity of human 20S proteasome using Suc-LLVY-AMC as substrate
17
Total Activities
17
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 | 17 | 8.02 | 8.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3237863 | — | — | 1 | 8.57 |
| CHEMBL3237862 | — | — | 1 | 8.41 |
| CHEMBL3237864 | — | — | 1 | 8.39 |
| CHEMBL3237867 | — | — | 1 | 8.39 |
| CHEMBL3237873 | — | — | 1 | 8.32 |
| CHEMBL3237865 | — | — | 1 | 8.29 |
| CHEMBL3237866 | — | — | 1 | 8.24 |
| CHEMBL3237860 | — | — | 1 | 8.24 |
| CHEMBL3237868 | — | — | 1 | 8.23 |
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 8.15 |
| CHEMBL3237870 | — | — | 1 | 8.15 |
| CHEMBL3237871 | — | — | 1 | 8.12 |
| CHEMBL3237874 | — | — | 1 | 8.11 |
| CHEMBL3237869 | — | — | 1 | 8.11 |
| CHEMBL3237861 | — | — | 1 | 7.54 |
| CHEMBL3237872 | — | — | 1 | 7.27 |
| CHEMBL491636 | BELACTOSIN A | — | 1 | 5.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3237863 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL3237862 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL3237864 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL3237867 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL3237873 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3237865 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL3237866 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL3237860 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL3237868 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL325041 | BORTEZOMIB | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3237870 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL3237871 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL3237874 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL3237869 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL3237861 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3237872 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL491636 | BELACTOSIN A | IC50 | = | 1400.0 | nM | 5.85 |