Assay Detail
Binding
CHEMBL1817340
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Inhibition of chymotrypsin-like activity of 20S proteasome using suc-LLVY-AMC as substrate preincubated for 10 mins before substrate addition at pH 7.6 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 | 6.62 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 7.85 |
| CHEMBL1813225 | — | — | 1 | 7.75 |
| CHEMBL272906 | — | — | 1 | 7.60 |
| CHEMBL1813226 | — | — | 1 | 7.55 |
| CHEMBL1813239 | — | — | 1 | 7.00 |
| CHEMBL1813229 | — | — | 1 | 7.00 |
| CHEMBL1813245 | — | — | 1 | 6.96 |
| CHEMBL1813231 | — | — | 1 | 6.92 |
| CHEMBL490055 | — | — | 1 | 6.92 |
| CHEMBL1813241 | — | — | 1 | 6.89 |
| CHEMBL1813230 | — | — | 1 | 6.85 |
| CHEMBL1813243 | — | — | 1 | 6.85 |
| CHEMBL1813247 | — | — | 1 | 6.82 |
| CHEMBL1813246 | — | — | 1 | 6.82 |
| CHEMBL1813244 | — | — | 1 | 6.82 |
| CHEMBL1813234 | — | — | 1 | 6.77 |
| CHEMBL1813227 | — | — | 1 | 6.75 |
| CHEMBL1813238 | — | — | 1 | 6.66 |
| CHEMBL1813242 | — | — | 1 | 6.52 |
| CHEMBL1813248 | — | — | 1 | 6.52 |
| CHEMBL1813249 | — | — | 1 | 6.46 |
| CHEMBL1813232 | — | — | 1 | 6.44 |
| CHEMBL1813240 | — | — | 1 | 6.40 |
| CHEMBL1813228 | — | — | 1 | 6.37 |
| CHEMBL1813235 | — | — | 1 | 6.35 |
| CHEMBL1813251 | — | — | 1 | 6.33 |
| CHEMBL1813250 | — | — | 1 | 6.27 |
| CHEMBL1813254 | — | — | 1 | 6.21 |
| CHEMBL1813233 | — | — | 1 | 6.11 |
| CHEMBL1813252 | — | — | 1 | 6.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL325041 | BORTEZOMIB | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1813225 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL272906 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1813226 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL1813239 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1813229 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1813245 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1813231 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL490055 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1813241 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1813230 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1813243 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1813247 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL1813246 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL1813244 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL1813234 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL1813227 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL1813238 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL1813242 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL1813248 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL1813249 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL1813232 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL1813240 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL1813228 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL1813235 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL1813251 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL1813250 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL1813254 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL1813233 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL1813252 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL1813236 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1813255 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL1813253 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL1813237 | — | IC50 | = | 5200.0 | nM | 5.28 |