Assay Detail
Binding
CHEMBL4622704
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PCSK9 by Alexa Fluor 647 staining based TR-FRET assay
6
Total Activities
6
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
Novel Cyclic Tetramer Compounds as PCSK9 Inhibitors for Treating Metabolic Disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 9.33 | 9.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4642977 | — | — | 1 | 9.82 |
| CHEMBL4635142 | — | — | 1 | 9.48 |
| CHEMBL4642595 | — | — | 1 | 9.36 |
| CHEMBL4641251 | — | — | 1 | 9.24 |
| CHEMBL4645450 | — | — | 1 | 9.07 |
| CHEMBL4638184 | — | — | 1 | 9.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4642977 | — | IC50 | = | 0.152 | nM | 9.82 |
| CHEMBL4635142 | — | IC50 | = | 0.327 | nM | 9.48 |
| CHEMBL4642595 | — | IC50 | = | 0.438 | nM | 9.36 |
| CHEMBL4641251 | — | IC50 | = | 0.57 | nM | 9.24 |
| CHEMBL4645450 | — | IC50 | = | 0.85 | nM | 9.07 |
| CHEMBL4638184 | — | IC50 | = | 0.93 | nM | 9.03 |