Assay Detail
Binding
CHEMBL5365867
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Inhibition of full length human PCSK9 expressed in human Huh-7 cells by ELISA analysis
31
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Huh-7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Proprotein convertase subtilisin/kexin type 9 (CHEMBL2929) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Small molecule inhibitors of PCSK9. SAR investigations of head and amine groups.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 5.55 | 6.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5431139 | — | — | 1 | 6.24 |
| CHEMBL5415107 | — | — | 1 | 6.21 |
| CHEMBL5414787 | — | — | 1 | 6.14 |
| CHEMBL4109308 | — | — | 1 | 6.12 |
| CHEMBL5400549 | — | — | 1 | 5.96 |
| CHEMBL4107559 | — | — | 1 | 5.84 |
| CHEMBL5408632 | — | — | 1 | 5.78 |
| CHEMBL5427421 | — | — | 1 | 5.75 |
| CHEMBL5394025 | — | — | 1 | 5.74 |
| CHEMBL5403420 | — | — | 1 | 5.71 |
| CHEMBL4107804 | — | — | 1 | 5.65 |
| CHEMBL5406095 | — | — | 1 | 5.64 |
| CHEMBL5401016 | — | — | 1 | 5.55 |
| CHEMBL5414767 | — | — | 1 | 5.48 |
| CHEMBL5397401 | — | — | 2 | 5.34 |
| CHEMBL5436376 | — | — | 1 | 5.27 |
| CHEMBL5421898 | — | — | 1 | 5.17 |
| CHEMBL5440847 | — | — | 1 | 5.11 |
| CHEMBL5398982 | — | — | 1 | 4.85 |
| CHEMBL5417992 | — | — | 1 | 4.77 |
| CHEMBL5414978 | — | — | 1 | 4.77 |
| CHEMBL5433750 | — | — | 1 | - |
| CHEMBL5407175 | — | — | 1 | - |
| CHEMBL5408894 | — | — | 1 | - |
| CHEMBL5406351 | — | — | 1 | - |
| CHEMBL5414972 | — | — | 1 | - |
| CHEMBL5420031 | — | — | 1 | - |
| CHEMBL5418395 | — | — | 1 | - |
| CHEMBL5403764 | — | — | 1 | - |
| CHEMBL5414993 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5431139 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL5415107 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL5414787 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL4109308 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL5400549 | — | IC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL4107559 | — | IC50 | = | 1460.0 | nM | 5.84 |
| CHEMBL5408632 | — | IC50 | = | 1660.0 | nM | 5.78 |
| CHEMBL5427421 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL5394025 | — | IC50 | = | 1840.0 | nM | 5.74 |
| CHEMBL5403420 | — | IC50 | = | 1970.0 | nM | 5.71 |
| CHEMBL4107804 | — | IC50 | = | 2250.0 | nM | 5.65 |
| CHEMBL5406095 | — | IC50 | = | 2280.0 | nM | 5.64 |
| CHEMBL5401016 | — | IC50 | = | 2790.0 | nM | 5.55 |
| CHEMBL5414767 | — | IC50 | = | 3310.0 | nM | 5.48 |
| CHEMBL5397401 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL5436376 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL5421898 | — | IC50 | = | 6840.0 | nM | 5.17 |
| CHEMBL5440847 | — | IC50 | = | 7740.0 | nM | 5.11 |
| CHEMBL5397401 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL5398982 | — | IC50 | = | 14100.0 | nM | 4.85 |
| CHEMBL5417992 | — | IC50 | = | 17100.0 | nM | 4.77 |
| CHEMBL5414978 | — | IC50 | = | 16900.0 | nM | 4.77 |
| CHEMBL5433750 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5407175 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5408894 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5406351 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5414972 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5420031 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5418395 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5403764 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5414993 | — | IC50 | > | 20000.0 | nM | - |