Assay Detail
Binding
CHEMBL2327271
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Inhibition of trypsin-like activity of rabbit 26s proteasome beta 2 subunit assessed as hydrolysis of Ac-RLR-amc fluorogenic substrate preincubated for 30 mins followed by substrate addition measured for 30 mins by fluorescence plate reader analysis
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Oryctolagus cuniculus |
| Confidence | 0 — Uncurated / Unknown |
| 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 | 20 | 6.79 | 8.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2326533 | — | — | 1 | 8.42 |
| CHEMBL2326262 | — | — | 1 | 8.20 |
| CHEMBL2326261 | — | — | 1 | 8.18 |
| CHEMBL2326541 | — | — | 1 | 7.92 |
| CHEMBL2326260 | — | — | 1 | 7.52 |
| CHEMBL2326263 | — | — | 1 | 7.35 |
| CHEMBL2326539 | — | — | 1 | 7.23 |
| CHEMBL2326271 | — | — | 1 | 7.10 |
| CHEMBL2326535 | — | — | 1 | 6.96 |
| CHEMBL2326264 | — | — | 1 | 6.75 |
| CHEMBL2326534 | — | — | 1 | 6.60 |
| CHEMBL2326272 | — | — | 1 | 6.52 |
| CHEMBL2326537 | — | — | 1 | 6.38 |
| CHEMBL2326538 | — | — | 1 | 6.13 |
| CHEMBL2326270 | — | — | 1 | 6.00 |
| CHEMBL2326536 | — | — | 1 | 5.75 |
| CHEMBL2326265 | — | — | 1 | 4.62 |
| CHEMBL2326266 | — | — | 1 | 4.62 |
| CHEMBL2326540 | — | — | 1 | - |
| CHEMBL2326267 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2326533 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL2326262 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL2326261 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL2326541 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2326260 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2326263 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL2326539 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL2326271 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2326535 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL2326264 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL2326534 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL2326272 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2326537 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL2326538 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL2326270 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2326536 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL2326265 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL2326266 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL2326540 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2326267 | — | IC50 | > | 30000.0 | nM | - |