Assay Detail
Binding
CHEMBL5151697
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human 20S immunoproteasome beta-1i subunit using (Ac-PAL)2R110 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 | 8.06 | 8.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5171825 | — | — | 1 | 8.57 |
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 8.54 |
| CHEMBL5188533 | — | — | 1 | 7.96 |
| CHEMBL451887 | CARFILZOMIB | 4.0 | 1 | 7.16 |
| CHEMBL5184466 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5171825 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL325041 | BORTEZOMIB | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL5188533 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL451887 | CARFILZOMIB | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL5184466 | — | IC50 | > | 30000.0 | nM | - |