Assay Detail
Binding
CHEMBL3100304
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of chymotrypsin-like activity of human 20S proteasome beta 5 subunit assessed as hydrolysis of succinyl-LLVY-AMC fluorogenic substrate measured for 1 hr by fluorometric analysis
31
Total Activities
31
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
A novel tamoxifen derivative, ridaifen-F, is a nonpeptidic small-molecule proteasome inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 5.90 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL64925 | MG-132 | — | 1 | 7.96 |
| CHEMBL3099624 | — | — | 1 | 6.24 |
| CHEMBL3099618 | — | — | 1 | 6.19 |
| CHEMBL3099636 | — | — | 1 | 6.17 |
| CHEMBL3099638 | — | — | 1 | 6.12 |
| CHEMBL3099637 | — | — | 1 | 6.10 |
| CHEMBL3099623 | — | — | 1 | 6.05 |
| CHEMBL3099635 | — | — | 1 | 5.98 |
| CHEMBL3099621 | — | — | 1 | 5.93 |
| CHEMBL3099622 | — | — | 1 | 5.86 |
| CHEMBL3099633 | — | — | 1 | 5.84 |
| CHEMBL3099631 | — | — | 1 | 5.80 |
| CHEMBL3099634 | — | — | 1 | 5.78 |
| CHEMBL3099632 | — | — | 1 | 5.78 |
| CHEMBL3099639 | — | — | 1 | 5.78 |
| CHEMBL3099640 | — | — | 1 | 5.71 |
| CHEMBL3099625 | — | — | 1 | 5.66 |
| CHEMBL3099626 | — | — | 1 | 5.57 |
| CHEMBL3099616 | — | — | 1 | 5.47 |
| CHEMBL3099630 | — | — | 1 | 5.47 |
| CHEMBL392916 | — | — | 1 | 5.18 |
| CHEMBL235994 | — | — | 1 | 5.14 |
| CHEMBL159263 | — | — | 1 | - |
| CHEMBL393196 | — | — | 1 | - |
| CHEMBL3099617 | — | — | 1 | - |
| CHEMBL3099619 | — | — | 1 | - |
| CHEMBL3098145 | — | — | 1 | - |
| CHEMBL3099620 | — | — | 1 | - |
| CHEMBL3099627 | — | — | 1 | - |
| CHEMBL3099628 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL64925 | MG-132 | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3099624 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL3099618 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL3099636 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL3099638 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL3099637 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3099623 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3099635 | — | IC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL3099621 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL3099622 | — | IC50 | = | 1370.0 | nM | 5.86 |
| CHEMBL3099633 | — | IC50 | = | 1460.0 | nM | 5.84 |
| CHEMBL3099631 | — | IC50 | = | 1570.0 | nM | 5.80 |
| CHEMBL3099634 | — | IC50 | = | 1650.0 | nM | 5.78 |
| CHEMBL3099632 | — | IC50 | = | 1660.0 | nM | 5.78 |
| CHEMBL3099639 | — | IC50 | = | 1660.0 | nM | 5.78 |
| CHEMBL3099640 | — | IC50 | = | 1940.0 | nM | 5.71 |
| CHEMBL3099625 | — | IC50 | = | 2190.0 | nM | 5.66 |
| CHEMBL3099626 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL3099616 | — | IC50 | = | 3360.0 | nM | 5.47 |
| CHEMBL3099630 | — | IC50 | = | 3380.0 | nM | 5.47 |
| CHEMBL392916 | — | IC50 | = | 6560.0 | nM | 5.18 |
| CHEMBL235994 | — | IC50 | = | 7190.0 | nM | 5.14 |
| CHEMBL159263 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL393196 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3099617 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3099619 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3098145 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3099620 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3099627 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3099628 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3099629 | — | IC50 | > | 10000.0 | nM | - |