Assay Detail
Binding
CHEMBL4479413
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of catalytic activity of immunoproteasome 20s subunit beta2 in human Raji cells incubated for 1 hr by BODIPY(FL)-LU-112 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 | 7.31 | 7.89 |
| pIC50(app) | 7 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL578478 | — | — | 2 | 7.89 |
| CHEMBL4563298 | — | — | 2 | 7.54 |
| CHEMBL4519899 | — | — | 2 | 7.35 |
| CHEMBL4534488 | — | — | 2 | 7.35 |
| CHEMBL4581491 | — | — | 2 | 7.20 |
| CHEMBL4562527 | — | — | 1 | 6.52 |
| CHEMBL4531811 | — | — | 2 | - |
| CHEMBL4582677 | — | — | 2 | - |
| CHEMBL4545125 | — | — | 1 | - |
| CHEMBL4570216 | — | — | 1 | - |
| CHEMBL4581001 | — | — | 1 | - |
| CHEMBL4522536 | — | — | 1 | - |
| CHEMBL3319483 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL578478 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4563298 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4519899 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4534488 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4581491 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL4562527 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4531811 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4582677 | — | 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) | = | 7.89 | — | - |
| CHEMBL4519899 | — | pIC50(app) | = | 7.34 | — | - |
| CHEMBL4563298 | — | pIC50(app) | = | 7.54 | — | - |
| CHEMBL4534488 | — | pIC50(app) | = | 7.35 | — | - |
| CHEMBL4581491 | — | pIC50(app) | = | 7.2 | — | - |
| CHEMBL4531811 | — | pIC50(app) | < | 4.0 | — | - |
| CHEMBL4582677 | — | pIC50(app) | < | 4.0 | — | - |