Assay Detail
Binding
CHEMBL5035795
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PCSK9 using Alexa Fluor 674 as substrate incubated for 2 hrs by FRET plus assay
10
Total Activities
10
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
A Series of Novel, Highly Potent, and Orally Bioavailable Next-Generation Tricyclic Peptide PCSK9 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 9.78 | 10.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5084416 | — | — | 1 | 10.94 |
| CHEMBL5082483 | — | — | 1 | 10.43 |
| CHEMBL5081587 | — | — | 1 | 9.80 |
| CHEMBL5087487 | — | — | 1 | 9.64 |
| CHEMBL5086286 | — | — | 1 | 9.60 |
| CHEMBL5091040 | — | — | 1 | 9.41 |
| CHEMBL5094648 | — | — | 1 | 8.65 |
| CHEMBL5086475 | — | — | 1 | - |
| CHEMBL5081349 | — | — | 1 | - |
| CHEMBL5085124 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5084416 | — | Ki | = | 0.01136 | nM | 10.94 |
| CHEMBL5082483 | — | Ki | = | 0.037 | nM | 10.43 |
| CHEMBL5081587 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL5087487 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL5086286 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL5091040 | — | Ki | = | 0.39 | nM | 9.41 |
| CHEMBL5094648 | — | Ki | = | 2.25 | nM | 8.65 |
| CHEMBL5086475 | — | Ki | = | 0.00826 | nM | - |
| CHEMBL5081349 | — | Ki | = | 0.00736 | nM | - |
| CHEMBL5085124 | — | Ki | < | 0.01 | nM | - |