Assay Detail
Binding
CHEMBL969909
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Inhibition of trypsin like 20S proteasome activity in lymphoblastoid cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
C-terminal constrained phenylalanine as a pharmacophoric unit in peptide-based proteasome inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.07 | 7.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL188918 | — | — | 1 | 7.48 |
| CHEMBL447652 | — | — | 1 | 7.10 |
| CHEMBL488905 | — | — | 1 | 6.74 |
| CHEMBL207990 | EPOXOMYCIN | — | 1 | 6.55 |
| CHEMBL64925 | MG-132 | — | 1 | 5.97 |
| CHEMBL448088 | — | — | 1 | 5.88 |
| CHEMBL488718 | — | — | 1 | 5.75 |
| CHEMBL486860 | — | — | 1 | 5.55 |
| CHEMBL488029 | — | — | 1 | 5.43 |
| CHEMBL461005 | — | — | 1 | 5.23 |
| CHEMBL449736 | — | — | 1 | 5.10 |
| CHEMBL503692 | — | — | 1 | - |
| CHEMBL508164 | — | — | 1 | - |
| CHEMBL454820 | — | — | 1 | - |
| CHEMBL449107 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL188918 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL447652 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL488905 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL207990 | EPOXOMYCIN | IC50 | = | 284.0 | nM | 6.55 |
| CHEMBL64925 | MG-132 | IC50 | = | 1077.0 | nM | 5.97 |
| CHEMBL448088 | — | IC50 | = | 1315.0 | nM | 5.88 |
| CHEMBL488718 | — | IC50 | = | 1761.0 | nM | 5.75 |
| CHEMBL486860 | — | IC50 | = | 2787.0 | nM | 5.55 |
| CHEMBL488029 | — | IC50 | = | 3674.0 | nM | 5.43 |
| CHEMBL461005 | — | IC50 | = | 5839.0 | nM | 5.23 |
| CHEMBL449736 | — | IC50 | = | 7946.0 | nM | 5.10 |
| CHEMBL503692 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL508164 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL454820 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL449107 | — | IC50 | > | 10000.0 | nM | - |