Assay Detail
Binding
CHEMBL4370447
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Inhibition of 20S constitutive proteasome beta 2 trypsin-like activity in human Raji cell lysates after 1 hr by competitive ABPP assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Raji |
| Subcellular | Lysate |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-Based Design of Inhibitors Selective for Human Proteasome β2c or β2i Subunits.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.70 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4451682 | — | — | 1 | 8.30 |
| CHEMBL4440581 | — | — | 1 | 8.22 |
| CHEMBL4590398 | — | — | 1 | 8.15 |
| CHEMBL2326533 | — | — | 1 | 7.89 |
| CHEMBL4546121 | — | — | 1 | 7.34 |
| CHEMBL4450505 | — | — | 1 | 7.19 |
| CHEMBL4545073 | — | — | 1 | 7.11 |
| CHEMBL4592602 | — | — | 1 | 6.77 |
| CHEMBL4442929 | — | — | 1 | 6.36 |
| CHEMBL4577205 | — | — | 1 | 5.60 |
| CHEMBL4446214 | — | — | 1 | 4.92 |
| CHEMBL4513509 | — | — | 1 | 4.72 |
| CHEMBL4544868 | — | — | 1 | 4.55 |
| CHEMBL4452605 | — | — | 1 | - |
| CHEMBL4518685 | — | — | 1 | - |
| CHEMBL4550552 | — | — | 1 | - |
| CHEMBL4443899 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4451682 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4440581 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4590398 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2326533 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4546121 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4450505 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4545073 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL4592602 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4442929 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL4577205 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4446214 | — | IC50 | = | 12100.0 | nM | 4.92 |
| CHEMBL4513509 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL4544868 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL4452605 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4518685 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4550552 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4443899 | — | IC50 | > | 100000.0 | nM | - |