Assay Detail
Binding
CHEMBL4255064
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Inhibition of human 20S immunoproteasome beta-5 using Suc-LLVY-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 | 5.69 | 7.99 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4290574 | — | — | 1 | 7.99 |
| CHEMBL3237875 | — | — | 1 | 7.28 |
| CHEMBL4290977 | — | — | 1 | 6.77 |
| CHEMBL4294116 | — | — | 1 | 6.70 |
| CHEMBL4280336 | — | — | 1 | 6.58 |
| CHEMBL4283793 | — | — | 1 | 6.38 |
| CHEMBL4294367 | — | — | 1 | 6.24 |
| CHEMBL4280071 | — | — | 1 | 5.80 |
| CHEMBL4287879 | — | — | 1 | 5.72 |
| CHEMBL4279971 | — | — | 1 | 5.57 |
| CHEMBL4281477 | — | — | 1 | 5.57 |
| CHEMBL4292640 | — | — | 1 | 5.42 |
| CHEMBL4285574 | — | — | 1 | 5.41 |
| CHEMBL4290109 | — | — | 1 | 5.40 |
| CHEMBL4278967 | — | — | 1 | 5.28 |
| CHEMBL4290026 | — | — | 1 | 5.21 |
| CHEMBL4289358 | — | — | 1 | 5.19 |
| CHEMBL4290714 | — | — | 1 | 5.11 |
| CHEMBL4282422 | — | — | 1 | 5.00 |
| CHEMBL4286888 | — | — | 1 | 4.90 |
| CHEMBL4290295 | — | — | 1 | 4.88 |
| CHEMBL4288293 | — | — | 1 | 4.77 |
| CHEMBL4277652 | — | — | 1 | 4.71 |
| CHEMBL4283534 | — | — | 1 | 4.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4290574 | — | IC50 | = | 10.2 | nM | 7.99 |
| CHEMBL3237875 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4290977 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4294116 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4280336 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4283793 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4294367 | — | IC50 | = | 572.0 | nM | 6.24 |
| CHEMBL4280071 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4287879 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4279971 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4281477 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4292640 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL4285574 | — | IC50 | = | 3930.0 | nM | 5.41 |
| CHEMBL4290109 | — | IC50 | = | 3960.0 | nM | 5.40 |
| CHEMBL4278967 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL4290026 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL4289358 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL4290714 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL4282422 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4286888 | — | IC50 | = | 12600.0 | nM | 4.90 |
| CHEMBL4290295 | — | IC50 | = | 13200.0 | nM | 4.88 |
| CHEMBL4288293 | — | IC50 | = | 17100.0 | nM | 4.77 |
| CHEMBL4277652 | — | IC50 | = | 19700.0 | nM | 4.71 |
| CHEMBL4283534 | — | IC50 | = | 25100.0 | nM | 4.60 |