Assay Detail
Binding
CHEMBL4124698
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Binding affinity to 80S ribosome in human HuH7 cells assessed as inhibition of PCSK9 mRNA translation after overnight incubation by ELISA
14
Total Activities
14
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 | 14 | 5.66 | 6.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4114159 | — | — | 1 | 6.11 |
| CHEMBL4109308 | — | — | 1 | 6.09 |
| CHEMBL4126894 | — | — | 1 | 6.05 |
| CHEMBL4126496 | — | — | 1 | 6.05 |
| CHEMBL4130157 | — | — | 1 | 5.89 |
| CHEMBL4107559 | — | — | 1 | 5.86 |
| CHEMBL4108338 | — | — | 1 | 5.84 |
| CHEMBL4128388 | — | — | 1 | 5.62 |
| CHEMBL4127458 | — | — | 1 | 5.55 |
| CHEMBL4127311 | — | — | 1 | 5.53 |
| CHEMBL4126072 | — | — | 1 | 5.51 |
| CHEMBL4128250 | — | — | 1 | 5.08 |
| CHEMBL4127016 | — | — | 1 | 5.03 |
| CHEMBL4128560 | — | — | 1 | 5.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4114159 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL4109308 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL4126894 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL4126496 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL4130157 | — | IC50 | = | 1290.0 | nM | 5.89 |
| CHEMBL4107559 | — | IC50 | = | 1370.0 | nM | 5.86 |
| CHEMBL4108338 | — | IC50 | = | 1440.0 | nM | 5.84 |
| CHEMBL4128388 | — | IC50 | = | 2380.0 | nM | 5.62 |
| CHEMBL4127458 | — | IC50 | = | 2820.0 | nM | 5.55 |
| CHEMBL4127311 | — | IC50 | = | 2970.0 | nM | 5.53 |
| CHEMBL4126072 | — | IC50 | = | 3080.0 | nM | 5.51 |
| CHEMBL4128250 | — | IC50 | = | 8370.0 | nM | 5.08 |
| CHEMBL4127016 | — | IC50 | = | 9320.0 | nM | 5.03 |
| CHEMBL4128560 | — | IC50 | = | 9240.0 | nM | 5.03 |