Assay Detail
Binding
CHEMBL4124683
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of dofetilide binding to human ERG by fluorescence polarization assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 |
|---|---|---|---|
| Ki | 15 | 4.89 | 5.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4129620 | — | — | 1 | 5.66 |
| CHEMBL4114159 | — | — | 1 | 5.48 |
| CHEMBL4130157 | — | — | 1 | 5.27 |
| CHEMBL4107559 | — | — | 1 | 5.23 |
| CHEMBL4128560 | — | — | 1 | 4.90 |
| CHEMBL4128250 | — | — | 1 | 4.89 |
| CHEMBL4127311 | — | — | 1 | 4.85 |
| CHEMBL4128388 | — | — | 1 | 4.80 |
| CHEMBL4126894 | — | — | 1 | 4.80 |
| CHEMBL4109308 | — | — | 1 | 4.74 |
| CHEMBL4108338 | — | — | 1 | 4.54 |
| CHEMBL4126496 | — | — | 1 | 4.47 |
| CHEMBL4127458 | — | — | 1 | 4.42 |
| CHEMBL4126072 | — | — | 1 | 4.42 |
| CHEMBL4127016 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4129620 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL4114159 | — | Ki | = | 3300.0 | nM | 5.48 |
| CHEMBL4130157 | — | Ki | = | 5400.0 | nM | 5.27 |
| CHEMBL4107559 | — | Ki | = | 5900.0 | nM | 5.23 |
| CHEMBL4128560 | — | Ki | = | 12700.0 | nM | 4.90 |
| CHEMBL4128250 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL4127311 | — | Ki | = | 14100.0 | nM | 4.85 |
| CHEMBL4128388 | — | Ki | = | 16000.0 | nM | 4.80 |
| CHEMBL4126894 | — | Ki | = | 15800.0 | nM | 4.80 |
| CHEMBL4109308 | — | Ki | = | 18100.0 | nM | 4.74 |
| CHEMBL4108338 | — | Ki | = | 28800.0 | nM | 4.54 |
| CHEMBL4126496 | — | Ki | = | 34000.0 | nM | 4.47 |
| CHEMBL4127458 | — | Ki | = | 38200.0 | nM | 4.42 |
| CHEMBL4126072 | — | Ki | = | 38400.0 | nM | 4.42 |
| CHEMBL4127016 | — | Ki | > | 40000.0 | nM | - |