Assay Detail
Binding
CHEMBL5151698
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human 20S immunoproteasome beta-2i subunit using Ac-RLR-AMC as substrate preincubated for 2 hrs followed by substrate addition and measured after 1 hr by fluorescence intensity assay
5
Total Activities
5
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 | 5 | 6.10 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL451887 | CARFILZOMIB | 4.0 | 1 | 7.89 |
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 5.79 |
| CHEMBL5188533 | — | — | 1 | 5.40 |
| CHEMBL5171825 | — | — | 1 | 5.31 |
| CHEMBL5184466 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL451887 | CARFILZOMIB | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL325041 | BORTEZOMIB | IC50 | = | 1630.0 | nM | 5.79 |
| CHEMBL5188533 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5171825 | — | IC50 | = | 4874.0 | nM | 5.31 |
| CHEMBL5184466 | — | IC50 | > | 30000.0 | nM | - |