Assay Detail
Binding
CHEMBL986170
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Kca2.3 channel expressed in HEK293 cells by thallium flux assay
15
Total Activities
15
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 | 15 | 7.29 | 9.78 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL525408 | APAMIN | — | 1 | 9.78 |
| CHEMBL476339 | — | — | 1 | 7.23 |
| CHEMBL489770 | — | — | 1 | 6.26 |
| CHEMBL121663 | DEQUALINIUM CHLORIDE | 4.0 | 1 | 5.89 |
| CHEMBL510773 | — | — | 1 | - |
| CHEMBL491603 | — | — | 1 | - |
| CHEMBL489282 | — | — | 1 | - |
| CHEMBL476338 | — | — | 1 | - |
| CHEMBL503704 | — | — | 1 | - |
| CHEMBL523626 | — | — | 1 | - |
| CHEMBL510166 | — | — | 1 | - |
| CHEMBL490592 | — | — | 1 | - |
| CHEMBL523462 | — | — | 1 | - |
| CHEMBL452409 | — | — | 1 | - |
| CHEMBL492010 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL525408 | APAMIN | IC50 | = | 0.168 | nM | 9.78 |
| CHEMBL476339 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL489770 | — | IC50 | = | 543.0 | nM | 6.26 |
| CHEMBL121663 | DEQUALINIUM CHLORIDE | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL510773 | — | IC50 | - | — | - | |
| CHEMBL491603 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL489282 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL476338 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL503704 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL523626 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL510166 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL490592 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL523462 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL452409 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL492010 | — | IC50 | > | 30000.0 | nM | - |