Assay Detail
Binding
CHEMBL4233073
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of trypsin-like activity of human 20S proteasome
3
Total Activities
3
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
Design, synthesis, in vitro and in vivo evaluation, and structure-activity relationship (SAR) discussion of novel dipeptidyl boronic acid proteasome inhibitors as orally available anti-cancer agents for the treatment of multiple myeloma and mechanism studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 5.45 | 5.84 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4248209 | — | — | 1 | 5.84 |
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 5.40 |
| CHEMBL1813256 | — | — | 1 | 5.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4248209 | — | IC50 | = | 1442.0 | nM | 5.84 |
| CHEMBL325041 | BORTEZOMIB | IC50 | = | 3998.0 | nM | 5.40 |
| CHEMBL1813256 | — | IC50 | = | 7954.0 | nM | 5.10 |