Assay Detail
Binding
CHEMBL986171
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Kca2.3 channel expressed in HEK293 cells by electrophysiology assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Small conductance calcium-activated potassium channel protein 3 (CHEMBL3381) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Initial SAR studies on apamin-displacing 2-aminothiazole blockers of calcium-activated small conductance potassium channels.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 7.42 | 10.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL525408 | APAMIN | — | 1 | 10.19 |
| CHEMBL476339 | — | — | 1 | 7.25 |
| CHEMBL489770 | — | — | 1 | 6.54 |
| CHEMBL121663 | DEQUALINIUM CHLORIDE | 4.0 | 1 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL525408 | APAMIN | IC50 | = | 0.064 | nM | 10.19 |
| CHEMBL476339 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL489770 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL121663 | DEQUALINIUM CHLORIDE | IC50 | = | 2000.0 | nM | 5.70 |