Assay Detail
Binding
CHEMBL4255072
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Inhibition of human 20S immunoproteasome beta-2 using BocLRR-AMC as substrate incubated for 15 mins measured for 45 mins by fluorescence assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-based design of human immuno- and constitutive proteasomes inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 4.91 | 6.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4292640 | — | — | 1 | 6.09 |
| CHEMBL4287879 | — | — | 1 | 5.57 |
| CHEMBL3237875 | — | — | 1 | 5.31 |
| CHEMBL4294116 | — | — | 1 | 5.24 |
| CHEMBL4290574 | — | — | 1 | 5.18 |
| CHEMBL4290714 | — | — | 1 | 5.05 |
| CHEMBL4280336 | — | — | 1 | 4.84 |
| CHEMBL4278967 | — | — | 1 | 4.80 |
| CHEMBL4290295 | — | — | 1 | 4.67 |
| CHEMBL4291704 | — | — | 1 | 4.66 |
| CHEMBL2337850 | — | — | 1 | 4.57 |
| CHEMBL4290977 | — | — | 1 | 4.55 |
| CHEMBL4286888 | — | — | 1 | 4.52 |
| CHEMBL4293405 | — | — | 1 | 4.47 |
| CHEMBL4278272 | — | — | 1 | 4.10 |
| CHEMBL4281070 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4292640 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL4287879 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL3237875 | — | IC50 | = | 4850.0 | nM | 5.31 |
| CHEMBL4294116 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL4290574 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL4290714 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL4280336 | — | IC50 | = | 14300.0 | nM | 4.84 |
| CHEMBL4278967 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL4290295 | — | IC50 | = | 21400.0 | nM | 4.67 |
| CHEMBL4291704 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL2337850 | — | IC50 | = | 27200.0 | nM | 4.57 |
| CHEMBL4290977 | — | IC50 | = | 28300.0 | nM | 4.55 |
| CHEMBL4286888 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL4293405 | — | IC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL4278272 | — | IC50 | = | 79000.0 | nM | 4.10 |
| CHEMBL4281070 | — | IC50 | = | 106000.0 | nM | - |