Assay Detail
Binding
CHEMBL933103
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Inhibition of chymotrypsin-like activity of human 20S proteasome in Molt4 cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MOLT-4 |
| 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 |
|---|---|---|---|
| EC50 | 12 | 7.30 | 7.87 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL270515 | DELANZOMIB | 2.0 | 1 | 7.87 |
| CHEMBL272880 | — | — | 1 | 7.80 |
| CHEMBL270727 | — | — | 1 | 7.77 |
| CHEMBL410111 | — | — | 1 | 7.73 |
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 7.68 |
| CHEMBL269875 | — | — | 1 | 7.68 |
| CHEMBL407947 | — | — | 1 | 7.68 |
| CHEMBL259675 | — | — | 1 | 7.57 |
| CHEMBL270762 | — | — | 1 | 7.57 |
| CHEMBL270936 | — | — | 1 | 7.50 |
| CHEMBL272906 | — | — | 1 | 5.87 |
| CHEMBL259677 | — | — | 1 | 4.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL270515 | DELANZOMIB | EC50 | = | 13.5 | nM | 7.87 |
| CHEMBL272880 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL270727 | — | EC50 | = | 16.9 | nM | 7.77 |
| CHEMBL410111 | — | EC50 | = | 18.6 | nM | 7.73 |
| CHEMBL325041 | BORTEZOMIB | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL269875 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL407947 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL259675 | — | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL270762 | — | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL270936 | — | EC50 | = | 32.0 | nM | 7.50 |
| CHEMBL272906 | — | EC50 | = | 1353.0 | nM | 5.87 |
| CHEMBL259677 | — | EC50 | = | 13000.0 | nM | 4.89 |