Assay Detail
Binding
CHEMBL5236417
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PCSK9 mediated LDLR degradation in human HepG2 cells assessed as restoration of LDLR
3
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HepG2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Proprotein convertase subtilisin/kexin type 9 (CHEMBL2929) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Recent Update on the Development of PCSK9 Inhibitors for Hypercholesterolemia Treatment.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Inhibition | 2 | - | - |
| EC50 | 1 | 6.60 | 6.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5280306 | — | — | 1 | 6.60 |
| CHEMBL4227325 | — | — | 1 | - |
| CHEMBL5278470 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5280306 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4227325 | — | Inhibition | = | 70.0 | % | - |
| CHEMBL5278470 | — | Inhibition | = | 50.0 | % | - |