Assay Detail
Binding
CHEMBL3226234
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 26S proteasome beta5 subunit in human Calu6 cells using Suc-LLVY-aminoluciferin as substrate after 1hr by luminescence assay
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Calu-6 |
| 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 | 7.26 | 8.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 8.41 |
| CHEMBL2141296 | IXAZOMIB | 3.0 | 1 | 8.05 |
| CHEMBL3218837 | — | — | 1 | 8.02 |
| CHEMBL3218827 | — | — | 1 | 8.01 |
| CHEMBL3218833 | — | — | 1 | 7.96 |
| CHEMBL3218826 | — | — | 1 | 7.96 |
| CHEMBL3218832 | — | — | 1 | 7.92 |
| CHEMBL3218834 | — | — | 1 | 7.89 |
| CHEMBL3218824 | — | — | 1 | 7.77 |
| CHEMBL3218831 | — | — | 1 | 7.75 |
| CHEMBL3218836 | — | — | 1 | 7.62 |
| CHEMBL3218828 | — | — | 1 | 7.60 |
| CHEMBL3218822 | — | — | 1 | 7.52 |
| CHEMBL3218844 | — | — | 1 | 7.52 |
| CHEMBL3218835 | — | — | 1 | 7.46 |
| CHEMBL3218825 | — | — | 1 | 7.40 |
| CHEMBL1269181 | — | — | 1 | 7.28 |
| CHEMBL3218823 | — | — | 1 | 7.14 |
| CHEMBL3218830 | — | — | 1 | 7.07 |
| CHEMBL3218829 | — | — | 1 | 6.44 |
| CHEMBL3218821 | — | — | 1 | 6.21 |
| CHEMBL3218839 | — | — | 1 | 6.16 |
| CHEMBL3218838 | — | — | 1 | 6.03 |
| CHEMBL3218820 | — | — | 1 | 6.02 |
| CHEMBL3218841 | — | — | 1 | 5.85 |
| CHEMBL3218845 | — | — | 1 | 5.77 |
| CHEMBL3218819 | — | — | 1 | - |
| CHEMBL3218818 | — | — | 1 | - |
| CHEMBL3218840 | — | — | 1 | - |
| CHEMBL3218842 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL325041 | BORTEZOMIB | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL2141296 | IXAZOMIB | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3218837 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL3218827 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL3218833 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3218826 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3218832 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3218834 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3218824 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3218831 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3218836 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3218828 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3218822 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3218844 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3218835 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3218825 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL1269181 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3218823 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL3218830 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL3218829 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL3218821 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL3218839 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL3218838 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL3218820 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL3218841 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3218845 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3218819 | — | IC50 | - | — | - | |
| CHEMBL3218818 | — | IC50 | - | — | - | |
| CHEMBL3218840 | — | IC50 | - | — | - | |
| CHEMBL3218842 | — | IC50 | - | — | - | |
| CHEMBL3218843 | — | IC50 | - | — | - | |
| CHEMBL3218817 | — | IC50 | - | — | - |