Assay Detail
Binding
CHEMBL4255068
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Inhibition of human 20S immunoproteasome beta-1 using Ac-PAL-AMC as substrate incubated for 15 mins measured for 45 mins by fluorescence assay
24
Total Activities
24
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 | 24 | 4.98 | 6.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3237875 | — | — | 1 | 6.23 |
| CHEMBL4287879 | — | — | 1 | 5.56 |
| CHEMBL4281477 | — | — | 1 | 5.46 |
| CHEMBL4279971 | — | — | 1 | 5.40 |
| CHEMBL4292640 | — | — | 1 | 5.37 |
| CHEMBL4278967 | — | — | 1 | 5.32 |
| CHEMBL4282422 | — | — | 1 | 5.24 |
| CHEMBL4289358 | — | — | 1 | 5.14 |
| CHEMBL4294116 | — | — | 1 | 5.06 |
| CHEMBL4290026 | — | — | 1 | 5.05 |
| CHEMBL4285574 | — | — | 1 | 4.99 |
| CHEMBL4293405 | — | — | 1 | 4.97 |
| CHEMBL4290295 | — | — | 1 | 4.90 |
| CHEMBL4290714 | — | — | 1 | 4.90 |
| CHEMBL4277652 | — | — | 1 | 4.89 |
| CHEMBL4280336 | — | — | 1 | 4.85 |
| CHEMBL4280071 | — | — | 1 | 4.79 |
| CHEMBL4286888 | — | — | 1 | 4.68 |
| CHEMBL2337850 | — | — | 1 | 4.67 |
| CHEMBL4290574 | — | — | 1 | 4.62 |
| CHEMBL4294367 | — | — | 1 | 4.61 |
| CHEMBL4290109 | — | — | 1 | 4.35 |
| CHEMBL4290977 | — | — | 1 | 4.28 |
| CHEMBL4283534 | — | — | 1 | 4.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3237875 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL4287879 | — | IC50 | = | 2770.0 | nM | 5.56 |
| CHEMBL4281477 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL4279971 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL4292640 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL4278967 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL4282422 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL4289358 | — | IC50 | = | 7310.0 | nM | 5.14 |
| CHEMBL4294116 | — | IC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL4290026 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL4285574 | — | IC50 | = | 10320.0 | nM | 4.99 |
| CHEMBL4293405 | — | IC50 | = | 10600.0 | nM | 4.97 |
| CHEMBL4290295 | — | IC50 | = | 12500.0 | nM | 4.90 |
| CHEMBL4290714 | — | IC50 | = | 12600.0 | nM | 4.90 |
| CHEMBL4277652 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4280336 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL4280071 | — | IC50 | = | 16100.0 | nM | 4.79 |
| CHEMBL4286888 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL2337850 | — | IC50 | = | 21500.0 | nM | 4.67 |
| CHEMBL4290574 | — | IC50 | = | 23800.0 | nM | 4.62 |
| CHEMBL4294367 | — | IC50 | = | 24600.0 | nM | 4.61 |
| CHEMBL4290109 | — | IC50 | = | 45000.0 | nM | 4.35 |
| CHEMBL4290977 | — | IC50 | = | 52000.0 | nM | 4.28 |
| CHEMBL4283534 | — | IC50 | = | 59000.0 | nM | 4.23 |