Assay Detail
Binding
CHEMBL2327273
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Inhibition of trypsin-like activity of proteasome beta 2 subunit in HEK-293T cell lysates using BODIPY-BODIPY-TMR-epoxomicin as probe after 1 hr by SDS-PAGE
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK-293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Incorporation of non-natural amino acids improves cell permeability and potency of specific inhibitors of proteasome trypsin-like sites.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.44 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2326261 | — | — | 1 | 7.66 |
| CHEMBL2326260 | — | — | 1 | 7.33 |
| CHEMBL2326541 | — | — | 1 | 7.29 |
| CHEMBL2326533 | — | — | 1 | 7.08 |
| CHEMBL2326262 | — | — | 1 | 7.00 |
| CHEMBL2326264 | — | — | 1 | 6.72 |
| CHEMBL2326263 | — | — | 1 | 6.43 |
| CHEMBL2326535 | — | — | 1 | 5.82 |
| CHEMBL2326537 | — | — | 1 | 5.60 |
| CHEMBL2326267 | — | — | 1 | 5.58 |
| CHEMBL2326265 | — | — | 1 | 5.57 |
| CHEMBL2326266 | — | — | 1 | 5.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2326261 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL2326260 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL2326541 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL2326533 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL2326262 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2326264 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL2326263 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL2326535 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL2326537 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL2326267 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL2326265 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL2326266 | — | IC50 | = | 5600.0 | nM | 5.25 |