Assay Detail
Binding
CHEMBL5151699
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human 20S immunoproteasome beta-5i subunit using Suc-LLVY-AMC as substrate preincubated for 2 hrs followed by substrate addition and measured after 1 hr by fluorescence intensity assay
42
Total Activities
42
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 Optimization and Discovery of M3258, a Specific Inhibitor of the Immunoproteasome Subunit LMP7 (β5i).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 42 | 7.90 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 8.89 |
| CHEMBL5188533 | — | — | 1 | 8.77 |
| CHEMBL5192498 | — | — | 1 | 8.74 |
| CHEMBL5191857 | — | — | 1 | 8.72 |
| CHEMBL5174892 | — | — | 1 | 8.72 |
| CHEMBL5175217 | — | — | 1 | 8.68 |
| CHEMBL5185591 | — | — | 1 | 8.66 |
| CHEMBL5170541 | — | — | 1 | 8.64 |
| CHEMBL5190088 | — | — | 1 | 8.64 |
| CHEMBL5171825 | — | — | 1 | 8.54 |
| CHEMBL5203216 | — | — | 1 | 8.54 |
| CHEMBL5194416 | — | — | 1 | 8.51 |
| CHEMBL5176576 | — | — | 1 | 8.51 |
| CHEMBL5196780 | — | — | 1 | 8.51 |
| CHEMBL451887 | CARFILZOMIB | 4.0 | 1 | 8.49 |
| CHEMBL5184466 | — | — | 1 | 8.44 |
| CHEMBL5173345 | — | — | 1 | 8.43 |
| CHEMBL5191807 | — | — | 1 | 8.39 |
| CHEMBL5172971 | — | — | 1 | 8.36 |
| CHEMBL5196323 | — | — | 1 | 8.35 |
| CHEMBL5185756 | — | — | 1 | 8.28 |
| CHEMBL5200546 | — | — | 1 | 8.23 |
| CHEMBL5175203 | — | — | 1 | 8.22 |
| CHEMBL5195781 | — | — | 1 | 8.19 |
| CHEMBL5201811 | — | — | 1 | 8.00 |
| CHEMBL5194916 | — | — | 1 | 7.96 |
| CHEMBL5177052 | — | — | 1 | 7.82 |
| CHEMBL5179619 | — | — | 1 | 7.75 |
| CHEMBL5202660 | — | — | 1 | 7.55 |
| CHEMBL5197479 | — | — | 1 | 7.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL325041 | BORTEZOMIB | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5188533 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5192498 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5191857 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5174892 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5175217 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL5185591 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL5170541 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL5190088 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL5171825 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL5203216 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL5176576 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL5196780 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL5194416 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL451887 | CARFILZOMIB | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL5184466 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5173345 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL5191807 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL5172971 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL5196323 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL5185756 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL5200546 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL5175203 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5195781 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL5201811 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5194916 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5177052 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5179619 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5202660 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL5197479 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5188026 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5204947 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL5176179 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL5194968 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL5184325 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5188029 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5207266 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5181539 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL5207873 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL5205717 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL5187088 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5179290 | — | IC50 | = | 1200.0 | nM | 5.92 |