Assay Detail
Binding
CHEMBL5388152
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Inhibition of human 20S proteasome chymotrypsin-like activity using Suc-Leu-Leu-Val-Tyr-AMC as fluorogenic peptide pre-incubated for 10 mins with compound followed by substrate addition for 60 mins by spectrofluorimetric analysis
22
Total Activities
22
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
Design and discovery of novel dipeptide boronic acid ester proteasome inhibitors, an oral slowly-released prodrug for the treatment of multiple myeloma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 7.91 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5419917 | — | — | 1 | 8.66 |
| CHEMBL5413513 | — | — | 1 | 8.62 |
| CHEMBL5394365 | — | — | 1 | 8.57 |
| CHEMBL5406440 | — | — | 1 | 8.40 |
| CHEMBL5398681 | — | — | 1 | 8.30 |
| CHEMBL5429323 | — | — | 1 | 8.28 |
| CHEMBL5431451 | — | — | 1 | 8.28 |
| CHEMBL5423645 | — | — | 1 | 8.25 |
| CHEMBL5412037 | — | — | 1 | 8.22 |
| CHEMBL5440712 | — | — | 1 | 8.20 |
| CHEMBL2141296 | IXAZOMIB | 3.0 | 1 | 8.19 |
| CHEMBL5403296 | — | — | 1 | 8.11 |
| CHEMBL5434607 | — | — | 1 | 8.08 |
| CHEMBL5394458 | — | — | 1 | 8.02 |
| CHEMBL5433735 | — | — | 1 | 8.01 |
| CHEMBL5433547 | — | — | 1 | 7.80 |
| CHEMBL5410630 | — | — | 1 | 7.69 |
| CHEMBL5402052 | — | — | 1 | 7.65 |
| CHEMBL5439342 | — | — | 1 | 7.06 |
| CHEMBL5405358 | — | — | 1 | 6.91 |
| CHEMBL5407355 | — | — | 1 | 6.54 |
| CHEMBL1813227 | — | — | 1 | 6.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5419917 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL5413513 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL5394365 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL5406440 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5398681 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5429323 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL5431451 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL5423645 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL5412037 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5440712 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL2141296 | IXAZOMIB | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL5403296 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL5434607 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL5394458 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL5433735 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL5433547 | — | IC50 | = | 15.8 | nM | 7.80 |
| CHEMBL5410630 | — | IC50 | = | 20.6 | nM | 7.69 |
| CHEMBL5402052 | — | IC50 | = | 22.4 | nM | 7.65 |
| CHEMBL5439342 | — | IC50 | = | 86.7 | nM | 7.06 |
| CHEMBL5405358 | — | IC50 | = | 124.2 | nM | 6.91 |
| CHEMBL5407355 | — | IC50 | = | 284.8 | nM | 6.54 |
| CHEMBL1813227 | — | IC50 | = | 768.4 | nM | 6.11 |