Assay Detail
Binding
CHEMBL4124682
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Binding affinity to 80S ribosome in human HuH7 cells harboring pCMV-truncated human PCSK9 (1 to 152 residues)-proLuc assessed as inhibition of PCSK9 mRNA translation after overnight incubation by luciferase reporter gene assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Huh-7 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Small Molecule Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitors: Hit to Lead Optimization of Systemic Agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.02 | 6.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4109308 | — | — | 1 | 6.42 |
| CHEMBL4126894 | — | — | 1 | 6.41 |
| CHEMBL4114159 | — | — | 1 | 6.39 |
| CHEMBL4126496 | — | — | 1 | 6.35 |
| CHEMBL4130157 | — | — | 1 | 6.16 |
| CHEMBL4108338 | — | — | 1 | 6.15 |
| CHEMBL4107559 | — | — | 1 | 6.07 |
| CHEMBL4128388 | — | — | 1 | 5.97 |
| CHEMBL4128250 | — | — | 1 | 5.58 |
| CHEMBL4128560 | — | — | 1 | 5.39 |
| CHEMBL4127016 | — | — | 1 | 5.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4109308 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL4126894 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4114159 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4126496 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4130157 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL4108338 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL4107559 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL4128388 | — | IC50 | = | 1060.0 | nM | 5.97 |
| CHEMBL4128250 | — | IC50 | = | 2630.0 | nM | 5.58 |
| CHEMBL4128560 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL4127016 | — | IC50 | = | 4300.0 | nM | 5.37 |