Assay Detail
Binding
CHEMBL5236433
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PCSK9 preincubated for 30 mins followed by EGF(A) addition and measured after 2 hrs by TR-FRET assay
5
Total Activities
5
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 |
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 |
|---|---|---|---|
| IC50 | 5 | 5.61 | 6.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5278470 | — | — | 1 | 6.14 |
| CHEMBL4227325 | — | — | 1 | 5.08 |
| CHEMBL5280306 | — | — | 1 | - |
| CHEMBL5275906 | — | — | 1 | - |
| CHEMBL5290775 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5278470 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL4227325 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL5280306 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL5275906 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL5290775 | — | IC50 | > | 50000.0 | nM | - |