Assay Detail
Binding
CHEMBL5553040
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Inhibition of human LMP2 beta-1i subunit using Ac-PAL-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 | 7.55 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4437785 | — | — | 1 | 8.52 |
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 8.40 |
| CHEMBL5566972 | — | — | 1 | 8.30 |
| CHEMBL5566401 | — | — | 1 | 8.30 |
| CHEMBL5590335 | — | — | 1 | 8.05 |
| CHEMBL5573016 | — | — | 1 | 8.00 |
| CHEMBL5573034 | — | — | 1 | 8.00 |
| CHEMBL5574862 | — | — | 1 | 7.75 |
| CHEMBL5573898 | — | — | 1 | 7.21 |
| CHEMBL5568778 | — | — | 1 | 6.88 |
| CHEMBL5575455 | — | — | 1 | 6.73 |
| CHEMBL5573623 | — | — | 1 | 6.72 |
| CHEMBL5563419 | — | — | 1 | 6.65 |
| CHEMBL4297468 | ZETOMIPZOMIB | 2.0 | 1 | 6.25 |
| CHEMBL5573399 | — | — | 1 | - |
| CHEMBL5569848 | — | — | 1 | - |
| CHEMBL5571311 | — | — | 1 | - |
| CHEMBL5572485 | — | — | 1 | - |
| CHEMBL5184466 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4437785 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL325041 | BORTEZOMIB | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5566972 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5566401 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5590335 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5573016 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5573034 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5574862 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5573898 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL5568778 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL5575455 | — | IC50 | = | 188.0 | nM | 6.73 |
| CHEMBL5573623 | — | IC50 | = | 189.0 | nM | 6.72 |
| CHEMBL5563419 | — | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL4297468 | ZETOMIPZOMIB | IC50 | = | 557.0 | nM | 6.25 |
| CHEMBL5573399 | — | IC50 | < | 5.0 | nM | - |
| CHEMBL5569848 | — | IC50 | < | 5.0 | nM | - |
| CHEMBL5571311 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL5572485 | — | IC50 | < | 5.0 | nM | - |
| CHEMBL5184466 | — | IC50 | > | 80000.0 | nM | - |