Assay Detail
Binding
CHEMBL5035794
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 assay
17
Total Activities
17
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 | 17 | 8.63 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5081587 | — | — | 1 | 9.70 |
| CHEMBL5086286 | — | — | 1 | 9.37 |
| CHEMBL5087487 | — | — | 1 | 9.35 |
| CHEMBL5091040 | — | — | 1 | 9.32 |
| CHEMBL5094648 | — | — | 1 | 8.94 |
| CHEMBL4790764 | — | — | 1 | 8.87 |
| CHEMBL5084586 | — | — | 1 | 8.66 |
| CHEMBL5078356 | — | — | 1 | 8.36 |
| CHEMBL5081995 | — | — | 1 | 8.33 |
| CHEMBL5081260 | — | — | 1 | 8.32 |
| CHEMBL5084251 | — | — | 1 | 7.39 |
| CHEMBL5077616 | — | — | 1 | 6.99 |
| CHEMBL5086475 | — | — | 1 | - |
| CHEMBL5084902 | — | — | 1 | - |
| CHEMBL5084416 | — | — | 1 | - |
| CHEMBL5081349 | — | — | 1 | - |
| CHEMBL5085124 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5081587 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL5086286 | — | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL5087487 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL5091040 | — | Ki | = | 0.48 | nM | 9.32 |
| CHEMBL5094648 | — | Ki | = | 1.16 | nM | 8.94 |
| CHEMBL4790764 | — | Ki | = | 1.36 | nM | 8.87 |
| CHEMBL5084586 | — | Ki | = | 2.17 | nM | 8.66 |
| CHEMBL5078356 | — | Ki | = | 4.36 | nM | 8.36 |
| CHEMBL5081995 | — | Ki | = | 4.66 | nM | 8.33 |
| CHEMBL5081260 | — | Ki | = | 4.83 | nM | 8.32 |
| CHEMBL5084251 | — | Ki | = | 40.71 | nM | 7.39 |
| CHEMBL5077616 | — | Ki | = | 102.9 | nM | 6.99 |
| CHEMBL5086475 | — | Ki | > | 0.1285 | nM | - |
| CHEMBL5084902 | — | Ki | > | 0.1285 | nM | - |
| CHEMBL5084416 | — | Ki | > | 0.1285 | nM | - |
| CHEMBL5081349 | — | Ki | > | 0.1285 | nM | - |
| CHEMBL5085124 | — | Ki | > | 0.1285 | nM | - |