Assay Detail
Binding
CHEMBL4479415
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Inhibition of catalytic activity of immunoproteasome 20s subunit beta1 in human Raji cells incubated for 1 hr by Cy5-NC-001 probe based competitive activity based protein profiling assay
20
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Raji |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-Based Design of β5c Selective Inhibitors of Human Constitutive Proteasomes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.67 | 6.92 |
| pIC50(app) | 7 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL578478 | — | — | 2 | 6.92 |
| CHEMBL4563298 | — | — | 2 | 6.89 |
| CHEMBL4519899 | — | — | 2 | 6.80 |
| CHEMBL4581491 | — | — | 2 | 6.05 |
| CHEMBL4534488 | — | — | 2 | - |
| CHEMBL4531811 | — | — | 2 | - |
| CHEMBL4582677 | — | — | 2 | - |
| CHEMBL4562527 | — | — | 1 | - |
| CHEMBL4545125 | — | — | 1 | - |
| CHEMBL4570216 | — | — | 1 | - |
| CHEMBL4581001 | — | — | 1 | - |
| CHEMBL4522536 | — | — | 1 | - |
| CHEMBL3319483 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL578478 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4563298 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4519899 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4581491 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL4534488 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4531811 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4582677 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4562527 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4545125 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4570216 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4581001 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4522536 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3319483 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL578478 | — | pIC50(app) | = | 6.91 | — | - |
| CHEMBL4519899 | — | pIC50(app) | = | 6.79 | — | - |
| CHEMBL4563298 | — | pIC50(app) | = | 6.88 | — | - |
| CHEMBL4534488 | — | pIC50(app) | < | 4.0 | — | - |
| CHEMBL4581491 | — | pIC50(app) | = | 6.05 | — | - |
| CHEMBL4531811 | — | pIC50(app) | < | 4.0 | — | - |
| CHEMBL4582677 | — | pIC50(app) | < | 4.0 | — | - |