Assay Detail
Binding
CHEMBL768300
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Inhibitory activity against 20S Proteasome
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Oryctolagus cuniculus |
| Confidence | 2 — Organism |
| Curated By | Expert |
Publication
Potent and selective inhibitors of the proteasome: dipeptidyl boronic acids.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 7.64 | 10.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL115619 | — | — | 1 | 10.82 |
| CHEMBL114388 | — | — | 1 | 10.52 |
| CHEMBL115762 | — | — | 1 | 9.74 |
| CHEMBL326503 | — | — | 1 | 9.62 |
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 9.21 |
| CHEMBL64925 | MG-132 | — | 1 | 8.40 |
| CHEMBL116231 | — | — | 1 | 7.60 |
| CHEMBL113870 | — | — | 1 | 7.35 |
| CHEMBL325272 | — | — | 1 | 7.01 |
| CHEMBL1790848 | — | — | 1 | 6.89 |
| CHEMBL114840 | — | — | 1 | 6.68 |
| CHEMBL325264 | — | — | 1 | 6.67 |
| CHEMBL331153 | — | — | 1 | 5.85 |
| CHEMBL115100 | — | — | 1 | 5.80 |
| CHEMBL112022 | — | — | 1 | 5.42 |
| CHEMBL320947 | — | — | 1 | 4.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL115619 | — | Ki | = | 0.015 | nM | 10.82 |
| CHEMBL114388 | — | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL115762 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL326503 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL325041 | BORTEZOMIB | Ki | = | 0.62 | nM | 9.21 |
| CHEMBL64925 | MG-132 | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL116231 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL113870 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL325272 | — | Ki | = | 97.0 | nM | 7.01 |
| CHEMBL1790848 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL114840 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL325264 | — | Ki | = | 214.0 | nM | 6.67 |
| CHEMBL331153 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL115100 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL112022 | — | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL320947 | — | Ki | = | 22000.0 | nM | 4.66 |