Assay Detail
Binding
CHEMBL1817341
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Inhibition of intracellular chymotrypsin-like activity of 20S proteasome in human HEK293 cells after 24 hrs by fluorescence plate reader
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Chemical and biological evaluation of dipeptidyl boronic acid proteasome inhibitors for use in prodrugs and pro-soft drugs targeting solid tumors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 6.07 | 7.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 7.57 |
| CHEMBL490055 | — | — | 1 | 6.82 |
| CHEMBL1813238 | — | — | 1 | 6.35 |
| CHEMBL1813226 | — | — | 1 | 6.28 |
| CHEMBL272906 | — | — | 1 | 6.10 |
| CHEMBL1813239 | — | — | 1 | 6.10 |
| CHEMBL1813249 | — | — | 1 | 6.00 |
| CHEMBL1813245 | — | — | 1 | 5.89 |
| CHEMBL1813240 | — | — | 1 | 5.85 |
| CHEMBL1813227 | — | — | 1 | 5.75 |
| CHEMBL1813244 | — | — | 1 | 5.68 |
| CHEMBL1813225 | — | — | 1 | 5.60 |
| CHEMBL1813243 | — | — | 1 | 5.51 |
| CHEMBL1813251 | — | — | 1 | 5.48 |
| CHEMBL1813234 | — | — | 1 | - |
| CHEMBL1813235 | — | — | 1 | - |
| CHEMBL1813236 | — | — | 1 | - |
| CHEMBL1813237 | — | — | 1 | - |
| CHEMBL1813228 | — | — | 1 | - |
| CHEMBL1813241 | — | — | 1 | - |
| CHEMBL1813229 | — | — | 1 | - |
| CHEMBL1813255 | — | — | 1 | - |
| CHEMBL1813254 | — | — | 1 | - |
| CHEMBL1813253 | — | — | 1 | - |
| CHEMBL1813252 | — | — | 1 | - |
| CHEMBL1813250 | — | — | 1 | - |
| CHEMBL1813242 | — | — | 1 | - |
| CHEMBL1813247 | — | — | 1 | - |
| CHEMBL1813246 | — | — | 1 | - |
| CHEMBL1813248 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL325041 | BORTEZOMIB | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL490055 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL1813238 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL1813226 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL272906 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL1813239 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL1813249 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1813245 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1813240 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL1813227 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL1813244 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL1813225 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1813243 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL1813251 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL1813230 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1813231 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1813232 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1813233 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1813234 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1813235 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1813236 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1813237 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1813228 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1813241 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1813229 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1813255 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1813254 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1813253 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1813252 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1813250 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1813242 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1813247 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1813246 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1813248 | — | IC50 | > | 10000.0 | nM | - |