Assay Detail
Binding
CHEMBL4423848
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Inhibition of human 20S proteasome preincubated for 15 mins followed by substrate addition
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Covalent docking modelling-based discovery of tripeptidyl epoxyketone proteasome inhibitors composed of aliphatic-heterocycles.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 7.63 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4460323 | — | — | 1 | 8.82 |
| CHEMBL4517600 | — | — | 1 | 8.62 |
| CHEMBL4444107 | — | — | 1 | 8.47 |
| CHEMBL4541038 | — | — | 1 | 8.44 |
| CHEMBL4547405 | — | — | 1 | 8.41 |
| CHEMBL4558648 | — | — | 1 | 8.34 |
| CHEMBL4542373 | — | — | 1 | 8.34 |
| CHEMBL4467618 | — | — | 1 | 8.32 |
| CHEMBL4436430 | — | — | 1 | 8.19 |
| CHEMBL4435814 | — | — | 1 | 8.19 |
| CHEMBL4559271 | — | — | 1 | 8.11 |
| CHEMBL451887 | CARFILZOMIB | 4.0 | 1 | 8.07 |
| CHEMBL4572638 | — | — | 1 | 8.03 |
| CHEMBL4441018 | — | — | 1 | 8.02 |
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 7.97 |
| CHEMBL4578081 | — | — | 1 | 7.86 |
| CHEMBL4443333 | — | — | 1 | 7.84 |
| CHEMBL4557130 | — | — | 1 | 7.78 |
| CHEMBL4580845 | — | — | 1 | 7.62 |
| CHEMBL4455910 | — | — | 1 | 7.59 |
| CHEMBL4569571 | — | — | 1 | 7.53 |
| CHEMBL4452330 | — | — | 1 | 7.50 |
| CHEMBL4541610 | — | — | 1 | 7.40 |
| CHEMBL4531582 | — | — | 1 | 7.22 |
| CHEMBL4571909 | — | — | 1 | 7.20 |
| CHEMBL4528925 | — | — | 1 | 7.12 |
| CHEMBL4435997 | — | — | 1 | 7.04 |
| CHEMBL4574045 | — | — | 1 | 6.63 |
| CHEMBL4438551 | — | — | 1 | 6.45 |
| CHEMBL4452953 | — | — | 1 | 6.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4460323 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4517600 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4444107 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4541038 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4547405 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4558648 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL4542373 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL4467618 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL4436430 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL4435814 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL4559271 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL451887 | CARFILZOMIB | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL4572638 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL4441018 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL325041 | BORTEZOMIB | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL4578081 | — | IC50 | = | 13.7 | nM | 7.86 |
| CHEMBL4443333 | — | IC50 | = | 14.5 | nM | 7.84 |
| CHEMBL4557130 | — | IC50 | = | 16.7 | nM | 7.78 |
| CHEMBL4580845 | — | IC50 | = | 24.1 | nM | 7.62 |
| CHEMBL4455910 | — | IC50 | = | 25.6 | nM | 7.59 |
| CHEMBL4569571 | — | IC50 | = | 29.8 | nM | 7.53 |
| CHEMBL4452330 | — | IC50 | = | 31.6 | nM | 7.50 |
| CHEMBL4541610 | — | IC50 | = | 40.1 | nM | 7.40 |
| CHEMBL4531582 | — | IC50 | = | 59.9 | nM | 7.22 |
| CHEMBL4571909 | — | IC50 | = | 63.8 | nM | 7.20 |
| CHEMBL4528925 | — | IC50 | = | 75.8 | nM | 7.12 |
| CHEMBL4435997 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL4574045 | — | IC50 | = | 232.2 | nM | 6.63 |
| CHEMBL4438551 | — | IC50 | = | 355.2 | nM | 6.45 |
| CHEMBL4452953 | — | IC50 | = | 484.1 | nM | 6.32 |
| CHEMBL4464750 | — | IC50 | = | 743.1 | nM | 6.13 |
| CHEMBL4439907 | — | IC50 | = | 782.6 | nM | 6.11 |
| CHEMBL4586405 | — | IC50 | = | 1089.6 | nM | 5.96 |
| CHEMBL4545717 | — | IC50 | - | — | - | |
| CHEMBL4448845 | — | IC50 | - | — | - |