Assay Detail
Binding
CHEMBL3865248
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Inhibition of chymotrypsin like activity of mouse spleen 20S proteasome beta5i subunit using Suc-Leu-Leu-Val-Tyr-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 2 hrs by fluorescence-based assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
New Peptidomimetic Boronates for Selective Inhibition of the Chymotrypsin-like Activity of the 26S Proteasome.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 7.17 | 7.86 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3907636 | — | — | 1 | 7.86 |
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 7.78 |
| CHEMBL3898621 | — | — | 1 | 6.95 |
| CHEMBL3972546 | — | — | 1 | 6.93 |
| CHEMBL3978175 | — | — | 1 | 6.32 |
| CHEMBL451887 | CARFILZOMIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3907636 | — | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL325041 | BORTEZOMIB | IC50 | = | 16.8 | nM | 7.78 |
| CHEMBL3898621 | — | IC50 | = | 113.3 | nM | 6.95 |
| CHEMBL3972546 | — | IC50 | = | 117.8 | nM | 6.93 |
| CHEMBL3978175 | — | IC50 | = | 483.0 | nM | 6.32 |
| CHEMBL451887 | CARFILZOMIB | IC50 | - | — | - |