Assay Detail
Binding
CHEMBL5151705
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 20S immunoproteasome beta-5i subunit in human PBMC using Ac-ANW-luciferin substrate preincubated for 2 hrs followed by substrate addition and measured after 30 mins by luminometric analysis
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | PBMC |
| 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 | 36 | 7.09 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5184466 | — | — | 1 | 8.47 |
| CHEMBL5185591 | — | — | 1 | 8.05 |
| CHEMBL5191857 | — | — | 1 | 7.97 |
| CHEMBL5201811 | — | — | 1 | 7.86 |
| CHEMBL5175217 | — | — | 1 | 7.85 |
| CHEMBL5190088 | — | — | 1 | 7.81 |
| CHEMBL5174892 | — | — | 1 | 7.75 |
| CHEMBL5177052 | — | — | 1 | 7.71 |
| CHEMBL5176576 | — | — | 1 | 7.70 |
| CHEMBL5196780 | — | — | 1 | 7.64 |
| CHEMBL5170541 | — | — | 1 | 7.61 |
| CHEMBL5192498 | — | — | 1 | 7.60 |
| CHEMBL5175203 | — | — | 1 | 7.57 |
| CHEMBL5179619 | — | — | 1 | 7.57 |
| CHEMBL5196323 | — | — | 1 | 7.54 |
| CHEMBL5173345 | — | — | 1 | 7.51 |
| CHEMBL5200546 | — | — | 1 | 7.40 |
| CHEMBL5191807 | — | — | 1 | 7.38 |
| CHEMBL5185756 | — | — | 1 | 7.38 |
| CHEMBL5203216 | — | — | 1 | 7.29 |
| CHEMBL5194416 | — | — | 1 | 7.28 |
| CHEMBL5202660 | — | — | 1 | 7.26 |
| CHEMBL5172971 | — | — | 1 | 7.22 |
| CHEMBL5194916 | — | — | 1 | 7.15 |
| CHEMBL5195781 | — | — | 1 | 6.79 |
| CHEMBL5181539 | — | — | 1 | 6.40 |
| CHEMBL5204947 | — | — | 1 | 6.36 |
| CHEMBL5194968 | — | — | 1 | 6.36 |
| CHEMBL5207266 | — | — | 1 | 6.19 |
| CHEMBL5207873 | — | — | 1 | 6.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5184466 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL5185591 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL5191857 | — | IC50 | = | 10.6 | nM | 7.97 |
| CHEMBL5201811 | — | IC50 | = | 13.7 | nM | 7.86 |
| CHEMBL5175217 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5190088 | — | IC50 | = | 15.5 | nM | 7.81 |
| CHEMBL5174892 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5177052 | — | IC50 | = | 19.6 | nM | 7.71 |
| CHEMBL5176576 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5196780 | — | IC50 | = | 22.8 | nM | 7.64 |
| CHEMBL5170541 | — | IC50 | = | 24.7 | nM | 7.61 |
| CHEMBL5192498 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5175203 | — | IC50 | = | 26.7 | nM | 7.57 |
| CHEMBL5179619 | — | IC50 | = | 27.1 | nM | 7.57 |
| CHEMBL5196323 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5173345 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL5200546 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5185756 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5191807 | — | IC50 | = | 41.5 | nM | 7.38 |
| CHEMBL5203216 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL5194416 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL5202660 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5172971 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL5194916 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL5195781 | — | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL5181539 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL5194968 | — | IC50 | = | 438.0 | nM | 6.36 |
| CHEMBL5204947 | — | IC50 | = | 434.0 | nM | 6.36 |
| CHEMBL5207266 | — | IC50 | = | 643.0 | nM | 6.19 |
| CHEMBL5207873 | — | IC50 | = | 824.0 | nM | 6.08 |
| CHEMBL5197479 | — | IC50 | = | 824.0 | nM | 6.08 |
| CHEMBL5184325 | — | IC50 | = | 896.0 | nM | 6.05 |
| CHEMBL5188026 | — | IC50 | = | 983.0 | nM | 6.01 |
| CHEMBL5179290 | — | IC50 | = | 1407.0 | nM | 5.85 |
| CHEMBL5187088 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL5205717 | — | IC50 | = | 9670.0 | nM | 5.01 |