Assay Detail
Binding
CHEMBL4345633
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Inhibition of human proteasome pre-incubated for 30 mins before Suc-LLVY-AMC substrate addition and measured after 120 mins by fluorescence based assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 2 — Organism |
| Curated By | Autocuration |
Publication
Discovery of Peptide Boronate Derivatives as Histone Deacetylase and Proteasome Dual Inhibitors for Overcoming Bortezomib Resistance of Multiple Myeloma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.89 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4456886 | — | — | 1 | 8.96 |
| CHEMBL4527403 | — | — | 1 | 8.48 |
| CHEMBL4576202 | — | — | 1 | 8.25 |
| CHEMBL4463372 | — | — | 1 | 7.80 |
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 7.71 |
| CHEMBL4547369 | — | — | 1 | 7.51 |
| CHEMBL4527880 | — | — | 1 | 7.47 |
| CHEMBL4462775 | — | — | 1 | 6.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4456886 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4527403 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL4576202 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL4463372 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL325041 | BORTEZOMIB | IC50 | = | 19.4 | nM | 7.71 |
| CHEMBL4547369 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4527880 | — | IC50 | = | 33.8 | nM | 7.47 |
| CHEMBL4462775 | — | IC50 | = | 110.0 | nM | 6.96 |