Assay Detail
Binding
CHEMBL1817339
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of chymotrypsin-like activity of 20S proteasome using suc-LLVY-AMC as substrate preincubated for 10 mins before substrate addition at pH 2.0 by fluorescence assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 | 7.20 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 8.00 |
| CHEMBL272906 | — | — | 1 | 7.92 |
| CHEMBL1813225 | — | — | 1 | 7.80 |
| CHEMBL1813228 | — | — | 1 | 7.68 |
| CHEMBL490055 | — | — | 1 | 7.58 |
| CHEMBL1813229 | — | — | 1 | 7.54 |
| CHEMBL1813238 | — | — | 1 | 7.48 |
| CHEMBL1813226 | — | — | 1 | 7.47 |
| CHEMBL1813254 | — | — | 1 | 7.44 |
| CHEMBL1813230 | — | — | 1 | 7.43 |
| CHEMBL1813255 | — | — | 1 | 7.41 |
| CHEMBL1813231 | — | — | 1 | 7.38 |
| CHEMBL1813239 | — | — | 1 | 7.37 |
| CHEMBL1813232 | — | — | 1 | 7.30 |
| CHEMBL1813240 | — | — | 1 | 7.30 |
| CHEMBL1813241 | — | — | 1 | 7.22 |
| CHEMBL1813233 | — | — | 1 | 7.20 |
| CHEMBL1813234 | — | — | 1 | 7.18 |
| CHEMBL1813242 | — | — | 1 | 7.12 |
| CHEMBL1813243 | — | — | 1 | 7.12 |
| CHEMBL1813235 | — | — | 1 | 7.10 |
| CHEMBL1813244 | — | — | 1 | 7.09 |
| CHEMBL1813245 | — | — | 1 | 7.09 |
| CHEMBL1813246 | — | — | 1 | 7.05 |
| CHEMBL1813247 | — | — | 1 | 7.00 |
| CHEMBL1813248 | — | — | 1 | 6.96 |
| CHEMBL1813249 | — | — | 1 | 6.96 |
| CHEMBL1813250 | — | — | 1 | 6.96 |
| CHEMBL1813227 | — | — | 1 | 6.96 |
| CHEMBL1813251 | — | — | 1 | 6.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL325041 | BORTEZOMIB | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL272906 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1813225 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1813228 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL490055 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1813229 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL1813238 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL1813226 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL1813254 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL1813230 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL1813255 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL1813231 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL1813239 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL1813232 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1813240 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1813241 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL1813233 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL1813234 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL1813242 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL1813243 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL1813235 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1813244 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL1813245 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL1813246 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL1813247 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1813248 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1813249 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1813250 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1813227 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1813251 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL1813236 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL1813252 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL1813237 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL1813253 | — | IC50 | = | 600.0 | nM | 6.22 |