Assay Detail
Binding
CHEMBL4185007
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 20s constitutive proteasome beta5 chymotrypsin-like activity in human erythrocytes using Suc-Leu-Leu-Val-Tyr-AMC as substrate after 10 mins by fluorescence assay
4
Total Activities
4
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
Identification of 2-thioxoimidazolidin-4-one derivatives as novel noncovalent proteasome and immunoproteasome inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 5.66 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL64925 | MG-132 | — | 1 | 8.40 |
| CHEMBL4204445 | — | — | 1 | 4.87 |
| CHEMBL4215753 | — | — | 1 | 4.75 |
| CHEMBL4208777 | — | — | 1 | 4.63 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL64925 | MG-132 | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL4204445 | — | Ki | = | 13600.0 | nM | 4.87 |
| CHEMBL4215753 | — | Ki | = | 17900.0 | nM | 4.75 |
| CHEMBL4208777 | — | Ki | = | 23600.0 | nM | 4.63 |