Assay Detail
Binding
CHEMBL4774177
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Modulation of PCSK9 in human HepG2 cells assessed as reduction in PCSK9 expression incubated for 24 hrs prior to compound washout followed by compound addition and measured after 24 hrs by ELISA
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HepG2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Proprotein convertase subtilisin/kexin type 9 (CHEMBL2929) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
From methylene bridged diindole to carbonyl linked benzimidazoleindole: Development of potent and metabolically stable PCSK9 modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 8.17 | 9.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4780905 | — | — | 1 | 9.82 |
| CHEMBL4785006 | — | — | 1 | 9.55 |
| CHEMBL4797870 | — | — | 1 | 9.16 |
| CHEMBL4783308 | — | — | 1 | 8.92 |
| CHEMBL4789986 | — | — | 1 | 8.61 |
| CHEMBL4788701 | — | — | 1 | 7.96 |
| CHEMBL4779800 | — | — | 1 | 7.40 |
| CHEMBL4783828 | — | — | 1 | 7.06 |
| CHEMBL4783880 | — | — | 1 | 6.79 |
| CHEMBL4779430 | — | — | 1 | 6.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4780905 | — | EC50 | = | 0.15 | nM | 9.82 |
| CHEMBL4785006 | — | EC50 | = | 0.28 | nM | 9.55 |
| CHEMBL4797870 | — | EC50 | = | 0.69 | nM | 9.16 |
| CHEMBL4783308 | — | EC50 | = | 1.21 | nM | 8.92 |
| CHEMBL4789986 | — | EC50 | = | 2.46 | nM | 8.61 |
| CHEMBL4788701 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4779800 | — | EC50 | = | 39.9 | nM | 7.40 |
| CHEMBL4783828 | — | EC50 | = | 88.0 | nM | 7.06 |
| CHEMBL4783880 | — | EC50 | = | 161.0 | nM | 6.79 |
| CHEMBL4779430 | — | EC50 | = | 348.0 | nM | 6.46 |