Assay Detail
Binding
CHEMBL5553041
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human 20S proteosome beta5c subunit using Ac-WLA-AMC as substrate preincubated with compound for 30 mins followed by substrate addition and measured after 1 hr by fluorescence based analysis
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Optimization of α-amido boronic acids via cryo-electron microscopy analysis: Discovery of a novel highly selective immunoproteasome subunit LMP7 (β5i)/LMP2 (β1i) dual inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 5.43 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 8.52 |
| CHEMBL5566972 | — | — | 1 | 6.52 |
| CHEMBL4297468 | ZETOMIPZOMIB | 2.0 | 1 | 6.14 |
| CHEMBL5184466 | — | — | 1 | 5.62 |
| CHEMBL5590335 | — | — | 1 | 5.53 |
| CHEMBL5573034 | — | — | 1 | 5.53 |
| CHEMBL4437785 | — | — | 1 | 5.49 |
| CHEMBL5566401 | — | — | 1 | 5.43 |
| CHEMBL5572485 | — | — | 1 | 5.31 |
| CHEMBL5574862 | — | — | 1 | 5.28 |
| CHEMBL5573898 | — | — | 1 | 5.20 |
| CHEMBL5573399 | — | — | 1 | 4.88 |
| CHEMBL5569848 | — | — | 1 | 4.81 |
| CHEMBL5563419 | — | — | 1 | 4.71 |
| CHEMBL5571311 | — | — | 1 | 4.71 |
| CHEMBL5573016 | — | — | 1 | 4.35 |
| CHEMBL5573623 | — | — | 1 | 4.33 |
| CHEMBL5575455 | — | — | 1 | - |
| CHEMBL5568778 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL325041 | BORTEZOMIB | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5566972 | — | IC50 | = | 302.0 | nM | 6.52 |
| CHEMBL4297468 | ZETOMIPZOMIB | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL5184466 | — | IC50 | = | 2413.0 | nM | 5.62 |
| CHEMBL5590335 | — | IC50 | = | 2983.0 | nM | 5.53 |
| CHEMBL5573034 | — | IC50 | = | 2952.0 | nM | 5.53 |
| CHEMBL4437785 | — | IC50 | = | 3221.0 | nM | 5.49 |
| CHEMBL5566401 | — | IC50 | = | 3693.0 | nM | 5.43 |
| CHEMBL5572485 | — | IC50 | = | 4947.0 | nM | 5.31 |
| CHEMBL5574862 | — | IC50 | = | 5196.0 | nM | 5.28 |
| CHEMBL5573898 | — | IC50 | = | 6313.0 | nM | 5.20 |
| CHEMBL5573399 | — | IC50 | = | 13056.0 | nM | 4.88 |
| CHEMBL5569848 | — | IC50 | = | 15351.0 | nM | 4.81 |
| CHEMBL5563419 | — | IC50 | = | 19486.0 | nM | 4.71 |
| CHEMBL5571311 | — | IC50 | = | 19542.0 | nM | 4.71 |
| CHEMBL5573016 | — | IC50 | = | 44613.0 | nM | 4.35 |
| CHEMBL5573623 | — | IC50 | = | 47340.0 | nM | 4.33 |
| CHEMBL5575455 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL5568778 | — | IC50 | > | 80000.0 | nM | - |