Assay Detail
Binding
CHEMBL4329571
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Binding affinity to 80S ribosome in human HeLa cells lysates using human full length PCSK9 encoding mRNAs assessed as inhibition of PCSK9 mRNA translation after 45 mins by Steady-Glo luciferase reporter gene assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Discovery of N-(piperidin-3-yl)-N-(pyridin-2-yl)piperidine/piperazine-1-carboxamides as small molecule inhibitors of PCSK9.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 5.73 | 6.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4574496 | — | — | 1 | 6.30 |
| CHEMBL4560206 | — | — | 1 | 6.30 |
| CHEMBL4554909 | — | — | 1 | 6.04 |
| CHEMBL4534859 | — | — | 1 | 5.81 |
| CHEMBL4446635 | — | — | 1 | 5.68 |
| CHEMBL4533299 | — | — | 1 | 5.64 |
| CHEMBL4566239 | — | — | 1 | 5.63 |
| CHEMBL4469712 | — | — | 1 | 5.44 |
| CHEMBL4527910 | — | — | 1 | 5.36 |
| CHEMBL4128250 | — | — | 1 | 5.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4574496 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4560206 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4554909 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL4534859 | — | IC50 | = | 1540.0 | nM | 5.81 |
| CHEMBL4446635 | — | IC50 | = | 2080.0 | nM | 5.68 |
| CHEMBL4533299 | — | IC50 | = | 2270.0 | nM | 5.64 |
| CHEMBL4566239 | — | IC50 | = | 2330.0 | nM | 5.63 |
| CHEMBL4469712 | — | IC50 | = | 3630.0 | nM | 5.44 |
| CHEMBL4527910 | — | IC50 | = | 4380.0 | nM | 5.36 |
| CHEMBL4128250 | — | IC50 | = | 8040.0 | nM | 5.09 |