Assay Detail
Binding
CHEMBL1034145
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Inhibition of trypsin-like activity of rabbit 20S proteasome
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Oryctolagus cuniculus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Leaving groups prolong the duration of 20S proteasome inhibition and enhance the potency of salinosporamides.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.10 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL463977 | — | — | 1 | 8.00 |
| CHEMBL457226 | — | — | 1 | 7.92 |
| CHEMBL195340 | IODOSALINOSPORAMIDE | — | 1 | 7.89 |
| CHEMBL433778 | BROMOSALINOSPORAMIDE | — | 1 | 7.85 |
| CHEMBL371405 | MARIZOMIB | 3.0 | 1 | 7.58 |
| CHEMBL464596 | — | — | 1 | 7.19 |
| CHEMBL373150 | — | — | 1 | 6.43 |
| CHEMBL371634 | SALINOSPORAMIDE B | — | 1 | 6.21 |
| CHEMBL191911 | — | — | 1 | 5.96 |
| CHEMBL2374248 | hydroxysalinosporamide A | — | 1 | 5.92 |
| CHEMBL514721 | FLUOROSALINOSPORAMIDE | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL463977 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL457226 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL195340 | IODOSALINOSPORAMIDE | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL433778 | BROMOSALINOSPORAMIDE | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL371405 | MARIZOMIB | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL464596 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL373150 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL371634 | SALINOSPORAMIDE B | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL191911 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL2374248 | hydroxysalinosporamide A | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL514721 | FLUOROSALINOSPORAMIDE | IC50 | - | — | - |