Assay Detail
Binding
CHEMBL4370461
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Inhibition of 20S constitutive proteasome beta 2 trypsin-like activity in human RPMI8226 cell lysates after 1 hr by coomassie brilliant blue staining-based fluorescence assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Subcellular | Lysate |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-Based Design of Inhibitors Selective for Human Proteasome β2c or β2i Subunits.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.97 | 6.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2326533 | — | — | 1 | 6.54 |
| CHEMBL4590398 | — | — | 1 | 5.90 |
| CHEMBL4451682 | — | — | 1 | 5.75 |
| CHEMBL4440581 | — | — | 1 | 5.70 |
| CHEMBL4592602 | — | — | 1 | - |
| CHEMBL4546121 | — | — | 1 | - |
| CHEMBL4545073 | — | — | 1 | - |
| CHEMBL4450505 | — | — | 1 | - |
| CHEMBL4442929 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2326533 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4590398 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL4451682 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4440581 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4592602 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4546121 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4545073 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4450505 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4442929 | — | IC50 | > | 10000.0 | nM | - |