Assay Detail
Binding
CHEMBL3226233
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 20S proteasome beta5 subunit in human erythrocytes using Ac-WLA-AMC as substrate by fluorescence assay
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Optimization of a series of dipeptides with a P3 -neopentyl asparagine residue as non-covalent inhibitors of the chymotrypsin-like activity of human 20S proteasome
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 7.96 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3218837 | — | — | 1 | 8.92 |
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 8.70 |
| CHEMBL3218834 | — | — | 1 | 8.68 |
| CHEMBL2141296 | IXAZOMIB | 3.0 | 1 | 8.52 |
| CHEMBL3218831 | — | — | 1 | 8.52 |
| CHEMBL3218833 | — | — | 1 | 8.43 |
| CHEMBL3218836 | — | — | 1 | 8.41 |
| CHEMBL3218830 | — | — | 1 | 8.40 |
| CHEMBL3218835 | — | — | 1 | 8.40 |
| CHEMBL3218828 | — | — | 1 | 8.33 |
| CHEMBL3218827 | — | — | 1 | 8.32 |
| CHEMBL3218824 | — | — | 1 | 8.27 |
| CHEMBL3218826 | — | — | 1 | 8.17 |
| CHEMBL3218843 | — | — | 1 | 8.14 |
| CHEMBL3218823 | — | — | 1 | 8.08 |
| CHEMBL3218832 | — | — | 1 | 7.96 |
| CHEMBL3218844 | — | — | 1 | 7.94 |
| CHEMBL3218822 | — | — | 1 | 7.92 |
| CHEMBL3218829 | — | — | 1 | 7.92 |
| CHEMBL1269181 | — | — | 1 | 7.80 |
| CHEMBL3218840 | — | — | 1 | 7.80 |
| CHEMBL3218825 | — | — | 1 | 7.66 |
| CHEMBL3218839 | — | — | 1 | 7.65 |
| CHEMBL3218841 | — | — | 1 | 7.64 |
| CHEMBL3218821 | — | — | 1 | 7.60 |
| CHEMBL3218838 | — | — | 1 | 7.48 |
| CHEMBL3218820 | — | — | 1 | 7.30 |
| CHEMBL3218845 | — | — | 1 | 7.03 |
| CHEMBL3218842 | — | — | 1 | 6.80 |
| CHEMBL3218819 | — | — | 1 | 6.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3218837 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL325041 | BORTEZOMIB | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3218834 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL2141296 | IXAZOMIB | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3218831 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3218833 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL3218836 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL3218830 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3218835 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3218828 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL3218827 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3218824 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL3218826 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL3218843 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL3218823 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL3218832 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3218844 | — | IC50 | = | 11.6 | nM | 7.94 |
| CHEMBL3218822 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3218829 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1269181 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3218840 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3218825 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3218839 | — | IC50 | = | 22.6 | nM | 7.65 |
| CHEMBL3218841 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3218821 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3218838 | — | IC50 | = | 33.3 | nM | 7.48 |
| CHEMBL3218820 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3218845 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL3218842 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3218819 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL3218817 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3218818 | — | IC50 | > | 1000.0 | nM | - |