Assay Detail
Binding
CHEMBL933101
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Inhibition of chymotrypsin-like activity of human erythrocyte 20S proteasome
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery of a potent, selective, and orally active proteasome inhibitor for the treatment of cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 8.49 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL270727 | — | — | 1 | 9.10 |
| CHEMBL407947 | — | — | 1 | 9.05 |
| CHEMBL270762 | — | — | 1 | 8.80 |
| CHEMBL269875 | — | — | 1 | 8.74 |
| CHEMBL410111 | — | — | 1 | 8.70 |
| CHEMBL259675 | — | — | 1 | 8.64 |
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 8.42 |
| CHEMBL270515 | DELANZOMIB | 2.0 | 1 | 8.42 |
| CHEMBL272880 | — | — | 1 | 8.34 |
| CHEMBL270936 | — | — | 1 | 8.17 |
| CHEMBL259677 | — | — | 1 | 8.06 |
| CHEMBL272906 | — | — | 1 | 7.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL270727 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL407947 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL270762 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL269875 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL410111 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL259675 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL325041 | BORTEZOMIB | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL270515 | DELANZOMIB | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL272880 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL270936 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL259677 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL272906 | — | IC50 | = | 42.0 | nM | 7.38 |