Assay Detail
Binding
CHEMBL3100302
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PGPH-like activity of human 20S proteasome beta 1 subunit assessed as hydrolysis of Z-LLE-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 | 5.96 | 6.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL64925 | MG-132 | — | 1 | 6.92 |
| CHEMBL3099620 | — | — | 1 | 6.46 |
| CHEMBL3099621 | — | — | 1 | 6.43 |
| CHEMBL3099624 | — | — | 1 | 6.43 |
| CHEMBL3099618 | — | — | 1 | 6.37 |
| CHEMBL3099636 | — | — | 1 | 6.20 |
| CHEMBL3099638 | — | — | 1 | 6.11 |
| CHEMBL3099637 | — | — | 1 | 6.10 |
| CHEMBL3099631 | — | — | 1 | 6.08 |
| CHEMBL3099623 | — | — | 1 | 6.06 |
| CHEMBL3099625 | — | — | 1 | 6.05 |
| CHEMBL3099635 | — | — | 1 | 6.04 |
| CHEMBL3099633 | — | — | 1 | 5.99 |
| CHEMBL3099622 | — | — | 1 | 5.98 |
| CHEMBL3099640 | — | — | 1 | 5.97 |
| CHEMBL3099632 | — | — | 1 | 5.92 |
| CHEMBL3099639 | — | — | 1 | 5.87 |
| CHEMBL3099634 | — | — | 1 | 5.81 |
| CHEMBL3099626 | — | — | 1 | 5.78 |
| CHEMBL3099630 | — | — | 1 | 5.60 |
| CHEMBL3099616 | — | — | 1 | 5.52 |
| CHEMBL392916 | — | — | 1 | 5.20 |
| CHEMBL235994 | — | — | 1 | 5.14 |
| CHEMBL393196 | — | — | 1 | 5.12 |
| CHEMBL3098145 | — | — | 1 | - |
| CHEMBL3099617 | — | — | 1 | - |
| CHEMBL3099627 | — | — | 1 | - |
| CHEMBL3099628 | — | — | 1 | - |
| CHEMBL3099629 | — | — | 1 | - |
| CHEMBL159263 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL64925 | MG-132 | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3099620 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL3099621 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL3099624 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL3099618 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL3099636 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL3099638 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL3099637 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL3099631 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL3099623 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL3099625 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL3099635 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL3099633 | — | IC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL3099622 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL3099640 | — | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL3099632 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3099639 | — | IC50 | = | 1350.0 | nM | 5.87 |
| CHEMBL3099634 | — | IC50 | = | 1560.0 | nM | 5.81 |
| CHEMBL3099626 | — | IC50 | = | 1670.0 | nM | 5.78 |
| CHEMBL3099630 | — | IC50 | = | 2510.0 | nM | 5.60 |
| CHEMBL3099616 | — | IC50 | = | 2990.0 | nM | 5.52 |
| CHEMBL392916 | — | IC50 | = | 6370.0 | nM | 5.20 |
| CHEMBL235994 | — | IC50 | = | 7260.0 | nM | 5.14 |
| CHEMBL393196 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL3098145 | — | IC50 | - | — | - | |
| CHEMBL3099617 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3099627 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3099628 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3099629 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL159263 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3099619 | — | IC50 | - | — | - |