Assay Detail
Functional
CHEMBL828517
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Inhibition of trypsin-like (T-L) activity of rabbit 20S proteasome
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Oryctolagus cuniculus |
| Confidence | 1 — Organism |
| Curated By | Expert |
Publication
Structure-activity relationship studies of salinosporamide A (NPI-0052), a novel marine derived proteasome inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.46 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL195340 | IODOSALINOSPORAMIDE | — | 1 | 7.89 |
| CHEMBL433778 | BROMOSALINOSPORAMIDE | — | 1 | 7.85 |
| CHEMBL371405 | MARIZOMIB | 3.0 | 1 | 7.68 |
| CHEMBL365537 | — | — | 1 | 7.04 |
| CHEMBL191717 | — | — | 1 | 6.68 |
| CHEMBL192046 | — | — | 1 | 6.60 |
| CHEMBL373150 | — | — | 1 | 6.47 |
| CHEMBL381627 | OMURALIDE | — | 1 | 6.27 |
| CHEMBL371634 | SALINOSPORAMIDE B | — | 1 | 6.19 |
| CHEMBL427534 | — | — | 1 | 6.11 |
| CHEMBL2374248 | hydroxysalinosporamide A | — | 1 | 6.10 |
| CHEMBL191911 | — | — | 1 | 5.96 |
| CHEMBL2096820 | — | — | 1 | 5.60 |
| CHEMBL191700 | — | — | 1 | 5.48 |
| CHEMBL363365 | — | — | 1 | 5.00 |
| CHEMBL195714 | — | — | 1 | - |
| CHEMBL370705 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL195340 | IODOSALINOSPORAMIDE | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL433778 | BROMOSALINOSPORAMIDE | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL371405 | MARIZOMIB | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL365537 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL191717 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL192046 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL373150 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL381627 | OMURALIDE | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL371634 | SALINOSPORAMIDE B | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL427534 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL2374248 | hydroxysalinosporamide A | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL191911 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL2096820 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL191700 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL363365 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL195714 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL370705 | — | IC50 | > | 20000.0 | nM | - |