Assay Detail
Binding
CHEMBL5151702
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human 20S proteasome beta5 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 | 5.84 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL451887 | CARFILZOMIB | 4.0 | 1 | 8.68 |
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 8.49 |
| CHEMBL5171825 | — | — | 1 | 8.30 |
| CHEMBL5188533 | — | — | 1 | 7.39 |
| CHEMBL5185591 | — | — | 1 | 6.85 |
| CHEMBL5190088 | — | — | 1 | 6.64 |
| CHEMBL5191857 | — | — | 1 | 6.40 |
| CHEMBL5174892 | — | — | 1 | 6.39 |
| CHEMBL5196780 | — | — | 1 | 6.28 |
| CHEMBL5170541 | — | — | 1 | 6.27 |
| CHEMBL5173345 | — | — | 1 | 6.11 |
| CHEMBL5175203 | — | — | 1 | 6.09 |
| CHEMBL5191807 | — | — | 1 | 6.07 |
| CHEMBL5175217 | — | — | 1 | 6.05 |
| CHEMBL5200546 | — | — | 1 | 6.03 |
| CHEMBL5196323 | — | — | 1 | 5.92 |
| CHEMBL5179619 | — | — | 1 | 5.85 |
| CHEMBL5195781 | — | — | 1 | 5.77 |
| CHEMBL5185756 | — | — | 1 | 5.77 |
| CHEMBL5194916 | — | — | 1 | 5.64 |
| CHEMBL5176576 | — | — | 1 | 5.62 |
| CHEMBL5184466 | — | — | 1 | 5.60 |
| CHEMBL5192498 | — | — | 1 | 5.54 |
| CHEMBL5201811 | — | — | 1 | 5.37 |
| CHEMBL5197479 | — | — | 1 | 5.30 |
| CHEMBL5202660 | — | — | 1 | 5.30 |
| CHEMBL5188026 | — | — | 1 | 5.25 |
| CHEMBL5194968 | — | — | 1 | 5.20 |
| CHEMBL5177052 | — | — | 1 | 5.19 |
| CHEMBL5194416 | — | — | 1 | 5.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL451887 | CARFILZOMIB | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL325041 | BORTEZOMIB | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL5171825 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5188533 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL5185591 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5190088 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL5191857 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL5174892 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL5196780 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL5170541 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL5173345 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL5175203 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL5191807 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL5175217 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL5200546 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL5196323 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL5179619 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL5195781 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL5185756 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL5194916 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL5176576 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL5184466 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL5192498 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL5201811 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL5197479 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL5202660 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL5188026 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL5194968 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL5177052 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL5194416 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL5203216 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL5172971 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL5204947 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL5176179 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL5187088 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL5207266 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL5207873 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL5181539 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL5184325 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL5205717 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5179290 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5188029 | — | IC50 | > | 30000.0 | nM | - |