Assay Detail
Binding
CHEMBL4829384
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human 20S proteasome LMP2 activity in human RPMI-8226 cells overexpressing ABCB1 using Ac-PAL-AMC as fluorogenic substrate incubated for 72 hrs by fluorescence assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | RPMI-8226 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Macrocyclic Immunoproteasome Inhibitors as a Potential Therapy for Alzheimer's Disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 6.79 | 6.98 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4877277 | — | — | 1 | 6.98 |
| CHEMBL4867231 | — | — | 1 | 6.83 |
| CHEMBL4879354 | — | — | 1 | 6.79 |
| CHEMBL4845896 | — | — | 1 | 6.69 |
| CHEMBL4646371 | — | — | 1 | 6.67 |
| CHEMBL4867229 | — | — | 1 | - |
| CHEMBL4870740 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4877277 | — | IC50 | = | 105.6 | nM | 6.98 |
| CHEMBL4867231 | — | IC50 | = | 146.8 | nM | 6.83 |
| CHEMBL4879354 | — | IC50 | = | 160.7 | nM | 6.79 |
| CHEMBL4845896 | — | IC50 | = | 204.4 | nM | 6.69 |
| CHEMBL4646371 | — | IC50 | = | 213.0 | nM | 6.67 |
| CHEMBL4867229 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4870740 | — | IC50 | > | 10000.0 | nM | - |