Assay Detail
Binding
CHEMBL3789477
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of chymotrypsin like activity of human erythrocyte-derived 20S proteasome preincubated for 10 mins using Suc-LLVY-AMC as substrate after 60 mins by fluorescence assay
15
Total Activities
15
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 and docking studies of novel dipeptidyl boronic acid proteasome inhibitors constructed from αα- and αβ-amino acids.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 8.44 | 8.99 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3786398 | — | — | 1 | 8.99 |
| CHEMBL499361 | — | — | 1 | 8.92 |
| CHEMBL499504 | — | — | 1 | 8.80 |
| CHEMBL3785681 | — | — | 1 | 8.33 |
| CHEMBL3786484 | — | — | 1 | 8.32 |
| CHEMBL3785613 | — | — | 1 | 8.20 |
| CHEMBL3787673 | — | — | 1 | 8.16 |
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 8.15 |
| CHEMBL3785317 | — | — | 1 | 8.07 |
| CHEMBL3787060 | — | — | 1 | - |
| CHEMBL3787687 | — | — | 1 | - |
| CHEMBL3786571 | — | — | 1 | - |
| CHEMBL3787573 | — | — | 1 | - |
| CHEMBL3785411 | — | — | 1 | - |
| CHEMBL3787320 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3786398 | — | IC50 | = | 1.02 | nM | 8.99 |
| CHEMBL499361 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL499504 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3785681 | — | IC50 | = | 4.69 | nM | 8.33 |
| CHEMBL3786484 | — | IC50 | = | 4.82 | nM | 8.32 |
| CHEMBL3785613 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL3787673 | — | IC50 | = | 6.94 | nM | 8.16 |
| CHEMBL325041 | BORTEZOMIB | IC50 | = | 7.09 | nM | 8.15 |
| CHEMBL3785317 | — | IC50 | = | 8.47 | nM | 8.07 |
| CHEMBL3787060 | — | IC50 | - | — | - | |
| CHEMBL3787687 | — | IC50 | - | — | - | |
| CHEMBL3786571 | — | IC50 | - | — | - | |
| CHEMBL3787573 | — | IC50 | - | — | - | |
| CHEMBL3785411 | — | IC50 | - | — | - | |
| CHEMBL3787320 | — | IC50 | - | — | - |