Assay Detail
Binding
CHEMBL4255071
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human 20S constitutive proteasome beta-2 using BocLRR-AMC as substrate incubated for 15 mins measured for 45 mins by fluorescence assay
13
Total Activities
13
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 | 13 | 4.91 | 6.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4292640 | — | — | 1 | 6.28 |
| CHEMBL4287879 | — | — | 1 | 5.54 |
| CHEMBL3237875 | — | — | 1 | 5.33 |
| CHEMBL4290574 | — | — | 1 | 4.88 |
| CHEMBL4294116 | — | — | 1 | 4.87 |
| CHEMBL4280336 | — | — | 1 | 4.79 |
| CHEMBL4290295 | — | — | 1 | 4.73 |
| CHEMBL4278967 | — | — | 1 | 4.71 |
| CHEMBL2337850 | — | — | 1 | 4.61 |
| CHEMBL4290977 | — | — | 1 | 4.58 |
| CHEMBL4290714 | — | — | 1 | 4.52 |
| CHEMBL4286888 | — | — | 1 | 4.51 |
| CHEMBL4291704 | — | — | 1 | 4.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4292640 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL4287879 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL3237875 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL4290574 | — | IC50 | = | 13200.0 | nM | 4.88 |
| CHEMBL4294116 | — | IC50 | = | 13500.0 | nM | 4.87 |
| CHEMBL4280336 | — | IC50 | = | 16200.0 | nM | 4.79 |
| CHEMBL4290295 | — | IC50 | = | 18600.0 | nM | 4.73 |
| CHEMBL4278967 | — | IC50 | = | 19300.0 | nM | 4.71 |
| CHEMBL2337850 | — | IC50 | = | 24800.0 | nM | 4.61 |
| CHEMBL4290977 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL4290714 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL4286888 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL4291704 | — | IC50 | = | 37600.0 | nM | 4.42 |