Assay Detail
Binding
CHEMBL4044273
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Inhibition of chymotrypsin-like activity of 20S proteasome in rabbit 20S proteasome pre-incubated for 10 mins before Suc-Leu-Leu-Val-Tyr-AMC substrate addition and measured after 2 hrs by fluorescence assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Oryctolagus cuniculus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Azobenzene-containing photoswitchable proteasome inhibitors with selective activity and cellular toxicity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.57 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 8.30 |
| CHEMBL4083741 | — | — | 1 | 8.00 |
| CHEMBL270515 | DELANZOMIB | 2.0 | 1 | 8.00 |
| CHEMBL4064758 | — | — | 1 | 7.96 |
| CHEMBL4101736 | — | — | 1 | 7.92 |
| CHEMBL4094006 | — | — | 1 | 7.77 |
| CHEMBL4088922 | — | — | 1 | 7.66 |
| CHEMBL4099066 | — | — | 1 | 7.54 |
| CHEMBL4063705 | — | — | 1 | 7.39 |
| CHEMBL4091522 | — | — | 1 | 7.28 |
| CHEMBL4086236 | — | — | 1 | 7.27 |
| CHEMBL4090606 | — | — | 1 | 7.26 |
| CHEMBL4069592 | — | — | 1 | 7.08 |
| CHEMBL4060704 | — | — | 1 | 6.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL325041 | BORTEZOMIB | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4083741 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL270515 | DELANZOMIB | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4064758 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4101736 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4094006 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4088922 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4099066 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4063705 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4091522 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4086236 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4090606 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4069592 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4060704 | — | IC50 | = | 249.0 | nM | 6.60 |