Assay Detail
Binding
CHEMBL861975
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Inhibition of post glutamyl peptide hydrolase-like proteasome activity of human 20S proteasome
56
Total Activities
56
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Optimization of subsite binding to the beta5 subunit of the human 20S proteasome using vinyl sulfones and 2-keto-1,3,4-oxadiazoles: syntheses and cellular properties of potent, selective proteasome inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 40 | 5.66 | 5.66 |
| Ki | 11 | 5.17 | 6.33 |
| Ki app | 5 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL64925 | MG-132 | — | 1 | 6.33 |
| CHEMBL207990 | EPOXOMYCIN | — | 1 | 5.66 |
| CHEMBL207591 | — | — | 1 | 4.85 |
| CHEMBL114388 | — | — | 1 | 4.32 |
| CHEMBL206525 | — | — | 1 | - |
| CHEMBL207669 | — | — | 1 | - |
| CHEMBL378901 | — | — | 1 | - |
| CHEMBL382203 | — | — | 1 | - |
| CHEMBL438612 | — | — | 1 | - |
| CHEMBL437115 | — | — | 1 | - |
| CHEMBL207196 | — | — | 1 | - |
| CHEMBL207162 | — | — | 1 | - |
| CHEMBL379771 | — | — | 1 | - |
| CHEMBL379772 | — | — | 1 | - |
| CHEMBL446443 | — | — | 1 | - |
| CHEMBL207403 | — | — | 1 | - |
| CHEMBL379669 | — | — | 1 | - |
| CHEMBL207336 | — | — | 1 | - |
| CHEMBL208015 | — | — | 1 | - |
| CHEMBL206206 | — | — | 1 | - |
| CHEMBL204992 | — | — | 1 | - |
| CHEMBL207016 | — | — | 1 | - |
| CHEMBL376815 | — | — | 1 | - |
| CHEMBL206001 | — | — | 1 | - |
| CHEMBL204946 | — | — | 1 | - |
| CHEMBL208372 | — | — | 1 | - |
| CHEMBL206413 | — | — | 1 | - |
| CHEMBL383674 | — | — | 1 | - |
| CHEMBL377532 | — | — | 1 | - |
| CHEMBL381735 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL64925 | MG-132 | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL207990 | EPOXOMYCIN | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL207591 | — | Ki | = | 14000.0 | nM | 4.85 |
| CHEMBL114388 | — | Ki | = | 48000.0 | nM | 4.32 |
| CHEMBL207403 | — | IC50 | > | 150000.0 | nM | - |
| CHEMBL438442 | — | IC50 | - | — | - | |
| CHEMBL379669 | — | IC50 | > | 150000.0 | nM | - |
| CHEMBL207669 | — | IC50 | - | — | - | |
| CHEMBL379476 | — | Ki app | - | — | - | |
| CHEMBL381931 | — | Ki app | - | — | - | |
| CHEMBL437311 | — | Ki app | - | — | - | |
| CHEMBL207160 | — | Ki app | - | — | - | |
| CHEMBL381089 | — | IC50 | - | — | - | |
| CHEMBL383673 | — | IC50 | - | — | - | |
| CHEMBL207394 | — | IC50 | - | — | - | |
| CHEMBL381884 | — | IC50 | - | — | - | |
| CHEMBL208019 | — | IC50 | - | — | - | |
| CHEMBL383529 | — | IC50 | - | — | - | |
| CHEMBL207670 | — | IC50 | - | — | - | |
| CHEMBL437882 | — | IC50 | - | — | - | |
| CHEMBL382180 | — | IC50 | - | — | - | |
| CHEMBL205687 | — | Ki | > | 450000.0 | nM | - |
| CHEMBL204518 | — | IC50 | - | — | - | |
| CHEMBL377123 | — | IC50 | - | — | - | |
| CHEMBL383730 | — | IC50 | - | — | - | |
| CHEMBL208159 | — | IC50 | - | — | - | |
| CHEMBL207284 | — | IC50 | - | — | - | |
| CHEMBL208015 | — | IC50 | > | 150000.0 | nM | - |
| CHEMBL381735 | — | IC50 | > | 150000.0 | nM | - |
| CHEMBL377532 | — | Ki | > | 900000.0 | nM | - |
| CHEMBL383674 | — | Ki | > | 900000.0 | nM | - |
| CHEMBL206413 | — | Ki | > | 450000.0 | nM | - |
| CHEMBL208372 | — | IC50 | > | 450000.0 | nM | - |
| CHEMBL204946 | — | IC50 | > | 450000.0 | nM | - |
| CHEMBL206001 | — | IC50 | > | 450000.0 | nM | - |
| CHEMBL376815 | — | IC50 | > | 450000.0 | nM | - |
| CHEMBL207016 | — | IC50 | > | 450000.0 | nM | - |
| CHEMBL204992 | — | IC50 | > | 450000.0 | nM | - |
| CHEMBL206206 | — | IC50 | > | 450000.0 | nM | - |
| CHEMBL446443 | — | IC50 | > | 150000.0 | nM | - |
| CHEMBL207336 | — | IC50 | > | 450000.0 | nM | - |
| CHEMBL206525 | — | Ki app | - | — | - | |
| CHEMBL378901 | — | IC50 | > | 150000.0 | nM | - |
| CHEMBL382203 | — | IC50 | > | 150000.0 | nM | - |
| CHEMBL438612 | — | IC50 | > | 150000.0 | nM | - |
| CHEMBL437115 | — | IC50 | > | 150000.0 | nM | - |
| CHEMBL207196 | — | IC50 | > | 150000.0 | nM | - |
| CHEMBL207162 | — | IC50 | > | 150000.0 | nM | - |
| CHEMBL379771 | — | IC50 | > | 150000.0 | nM | - |
| CHEMBL379772 | — | IC50 | > | 150000.0 | nM | - |