Assay Detail
Binding
CHEMBL5159800
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of chymotrypsin-like activity of human 20S proteasome using Suc-Leu Leu-Val-Tyr-AMC as substrate preincubated for 15 mins followed by substrate addition measured by fluorescence assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Metabolism guided optimization of peptidomimetics as non-covalent proteasome inhibitors for cancer treatment.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 7.69 | 9.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4102324 | — | — | 1 | 9.04 |
| CHEMBL5197285 | — | — | 1 | 8.46 |
| CHEMBL5171225 | — | — | 1 | 8.39 |
| CHEMBL5186240 | — | — | 1 | 8.29 |
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 8.16 |
| CHEMBL5202627 | — | — | 1 | 8.16 |
| CHEMBL5208573 | — | — | 1 | 8.14 |
| CHEMBL5172645 | — | — | 1 | 8.09 |
| CHEMBL5179570 | — | — | 1 | 8.08 |
| CHEMBL5209077 | — | — | 1 | 8.07 |
| CHEMBL5173459 | — | — | 1 | 8.05 |
| CHEMBL5201055 | — | — | 1 | 8.03 |
| CHEMBL5196378 | — | — | 1 | 8.03 |
| CHEMBL5188065 | — | — | 1 | 8.03 |
| CHEMBL5173758 | — | — | 1 | 7.69 |
| CHEMBL5190485 | — | — | 1 | 7.67 |
| CHEMBL5182408 | — | — | 1 | 7.64 |
| CHEMBL5198183 | — | — | 1 | 7.62 |
| CHEMBL5195393 | — | — | 1 | 7.60 |
| CHEMBL5174390 | — | — | 1 | 7.60 |
| CHEMBL5173174 | — | — | 1 | 7.38 |
| CHEMBL5183805 | — | — | 1 | 7.00 |
| CHEMBL5173789 | — | — | 1 | 5.80 |
| CHEMBL5178551 | — | — | 1 | 5.76 |
| CHEMBL5172317 | — | — | 1 | 5.35 |
| CHEMBL5207222 | — | — | 1 | - |
| CHEMBL5180560 | — | — | 1 | - |
| CHEMBL5181378 | — | — | 1 | - |
| CHEMBL5204673 | — | — | 1 | - |
| CHEMBL5169805 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4102324 | — | IC50 | = | 0.92 | nM | 9.04 |
| CHEMBL5197285 | — | IC50 | = | 3.43 | nM | 8.46 |
| CHEMBL5171225 | — | IC50 | = | 4.03 | nM | 8.39 |
| CHEMBL5186240 | — | IC50 | = | 5.15 | nM | 8.29 |
| CHEMBL325041 | BORTEZOMIB | IC50 | = | 6.91 | nM | 8.16 |
| CHEMBL5202627 | — | IC50 | = | 6.95 | nM | 8.16 |
| CHEMBL5208573 | — | IC50 | = | 7.24 | nM | 8.14 |
| CHEMBL5172645 | — | IC50 | = | 8.09 | nM | 8.09 |
| CHEMBL5179570 | — | IC50 | = | 8.39 | nM | 8.08 |
| CHEMBL5209077 | — | IC50 | = | 8.59 | nM | 8.07 |
| CHEMBL5173459 | — | IC50 | = | 8.92 | nM | 8.05 |
| CHEMBL5201055 | — | IC50 | = | 9.38 | nM | 8.03 |
| CHEMBL5196378 | — | IC50 | = | 9.26 | nM | 8.03 |
| CHEMBL5188065 | — | IC50 | = | 9.31 | nM | 8.03 |
| CHEMBL5173758 | — | IC50 | = | 20.32 | nM | 7.69 |
| CHEMBL5190485 | — | IC50 | = | 21.56 | nM | 7.67 |
| CHEMBL5182408 | — | IC50 | = | 22.63 | nM | 7.64 |
| CHEMBL5198183 | — | IC50 | = | 23.71 | nM | 7.62 |
| CHEMBL5195393 | — | IC50 | = | 24.97 | nM | 7.60 |
| CHEMBL5174390 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5173174 | — | IC50 | = | 41.23 | nM | 7.38 |
| CHEMBL5183805 | — | IC50 | = | 99.76 | nM | 7.00 |
| CHEMBL5173789 | — | IC50 | = | 1588.5 | nM | 5.80 |
| CHEMBL5178551 | — | IC50 | = | 1739.5 | nM | 5.76 |
| CHEMBL5172317 | — | IC50 | = | 4481.0 | nM | 5.35 |
| CHEMBL5207222 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5180560 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5181378 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5204673 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5169805 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5205890 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5206489 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5184789 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5204892 | — | IC50 | > | 10000.0 | nM | - |