Assay Detail
Binding
CHEMBL5236437
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Inhibition of PCSK9-LDLR protein-protein interaction in human HepG2 cells assessed as increase in LDL uptake
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HepG2 |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Recent Update on the Development of PCSK9 Inhibitors for Hypercholesterolemia Treatment.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 3 | 6.32 | 6.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5271747 | — | — | 1 | 6.97 |
| CHEMBL5278292 | — | — | 1 | 6.77 |
| CHEMBL4228379 | — | — | 1 | 5.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5271747 | — | EC50 | = | 106.0 | nM | 6.97 |
| CHEMBL5278292 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4228379 | — | EC50 | = | 6000.0 | nM | 5.22 |