Assay Detail
Binding
CHEMBL1274492
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Inhibition of chymotrypsin-like activity of human 20s proteasome beta5 subunit in human erythrocyte assessed as hydrolysis of Ac-WLA-AMC fluorogenic substrate
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Optimization of a series of dipeptides with a P3 threonine residue as non-covalent inhibitors of the chymotrypsin-like activity of the human 20S proteasome.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 7.02 | 8.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1270724 | — | — | 1 | 8.14 |
| CHEMBL1269196 | — | — | 1 | 8.13 |
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 8.09 |
| CHEMBL1269195 | — | — | 1 | 7.89 |
| CHEMBL184693 | — | — | 1 | 7.82 |
| CHEMBL1269181 | — | — | 1 | 7.80 |
| CHEMBL1269188 | — | — | 1 | 7.70 |
| CHEMBL1269186 | — | — | 1 | 7.70 |
| CHEMBL1269187 | — | — | 1 | 7.60 |
| CHEMBL1271031 | — | — | 1 | 7.51 |
| CHEMBL1269193 | — | — | 1 | 7.17 |
| CHEMBL1269185 | — | — | 1 | 7.13 |
| CHEMBL1270523 | — | — | 1 | 7.12 |
| CHEMBL1270931 | — | — | 1 | 7.00 |
| CHEMBL1270625 | — | — | 1 | 6.92 |
| CHEMBL1269194 | — | — | 1 | 6.68 |
| CHEMBL1270829 | — | — | 1 | 6.36 |
| CHEMBL1269184 | — | — | 1 | 6.35 |
| CHEMBL1269183 | — | — | 1 | 6.26 |
| CHEMBL1269182 | — | — | 1 | 5.96 |
| CHEMBL1269189 | — | — | 1 | 5.51 |
| CHEMBL1269192 | — | — | 1 | 5.50 |
| CHEMBL1269190 | — | — | 1 | 5.04 |
| CHEMBL1269191 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1270724 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL1269196 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL325041 | BORTEZOMIB | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL1269195 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL184693 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1269181 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1269188 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1269186 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1269187 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1271031 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL1269193 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL1269185 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL1270523 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL1270931 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1270625 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1269194 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL1270829 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL1269184 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL1269183 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL1269182 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1269189 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL1269192 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL1269190 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL1269191 | — | IC50 | > | 100000.0 | nM | - |