Assay Detail
Binding
CHEMBL861973
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Inhibition of chymotrypsin-like proteasome activity of human 20S proteasome
56
Total Activities
56
Compounds Tested
2
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 | 7.14 | 8.96 |
| Ki | 16 | 8.12 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL207598 | — | — | 1 | 9.30 |
| CHEMBL205757 | — | — | 1 | 9.29 |
| CHEMBL206413 | — | — | 1 | 9.19 |
| CHEMBL377532 | — | — | 1 | 9.14 |
| CHEMBL383674 | — | — | 1 | 9.14 |
| CHEMBL204992 | — | — | 1 | 8.96 |
| CHEMBL382203 | — | — | 1 | 8.82 |
| CHEMBL207016 | — | — | 1 | 8.68 |
| CHEMBL114388 | — | — | 1 | 8.64 |
| CHEMBL381735 | — | — | 1 | 8.62 |
| CHEMBL207162 | — | — | 1 | 8.60 |
| CHEMBL206206 | — | — | 1 | 8.54 |
| CHEMBL438612 | — | — | 1 | 8.49 |
| CHEMBL64925 | MG-132 | — | 1 | 8.43 |
| CHEMBL207990 | EPOXOMYCIN | — | 1 | 8.43 |
| CHEMBL206001 | — | — | 1 | 8.37 |
| CHEMBL207160 | — | — | 1 | 8.24 |
| CHEMBL204946 | — | — | 1 | 8.23 |
| CHEMBL208015 | — | — | 1 | 8.21 |
| CHEMBL376815 | — | — | 1 | 8.17 |
| CHEMBL207669 | — | — | 1 | 8.00 |
| CHEMBL207336 | — | — | 1 | 7.77 |
| CHEMBL207196 | — | — | 1 | 7.62 |
| CHEMBL446443 | — | — | 1 | 7.57 |
| CHEMBL207425 | — | — | 1 | 7.50 |
| CHEMBL379669 | — | — | 1 | 7.46 |
| CHEMBL383122 | — | — | 1 | 7.42 |
| CHEMBL208159 | — | — | 1 | 7.36 |
| CHEMBL437311 | — | — | 1 | 7.35 |
| CHEMBL379772 | — | — | 1 | 7.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL207598 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL205757 | — | Ki | = | 0.51 | nM | 9.29 |
| CHEMBL206413 | — | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL377532 | — | Ki | = | 0.72 | nM | 9.14 |
| CHEMBL383674 | — | Ki | = | 0.72 | nM | 9.14 |
| CHEMBL204992 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL382203 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL207016 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL114388 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL381735 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL207162 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL206206 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL438612 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL207990 | EPOXOMYCIN | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL64925 | MG-132 | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL206001 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL207160 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL204946 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL208015 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL376815 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL207669 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL207336 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL207196 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL446443 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL207425 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL379669 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL383122 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL208159 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL437311 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL379772 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL378901 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL437115 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL207403 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL379771 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL207579 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL437882 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL205687 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL381931 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL208019 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL383529 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL381884 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL207284 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL379476 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL383673 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL382180 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL209243 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL377123 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL381089 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL204518 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL383730 | — | IC50 | = | 3300.0 | nM | 5.48 |