Assay Detail
Functional
CHEMBL832384
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Inhibition of after hyperpolarization (AHP) of cultured rat sympathetic neurons as SKCa channel blocking activity
26
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Cell Type | Sympathetic neuron |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Small conductance calcium-activated potassium channel (CHEMBL2096673) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
Bis-quinolinium cyclophanes: toward a pharmacophore model for the blockade of apamin-sensitive SKCa channels in sympathetic neurons.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 7.31 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL420873 | — | — | 1 | 8.70 |
| CHEMBL117908 | — | — | 1 | 8.52 |
| CHEMBL184300 | — | — | 1 | 8.05 |
| CHEMBL185146 | — | — | 1 | 8.00 |
| CHEMBL181911 | — | — | 1 | 7.92 |
| CHEMBL183644 | — | — | 1 | 7.82 |
| CHEMBL184858 | — | — | 1 | 7.80 |
| CHEMBL181912 | — | — | 1 | 7.60 |
| CHEMBL430146 | — | — | 1 | 7.55 |
| CHEMBL184891 | — | — | 1 | 7.52 |
| CHEMBL182716 | — | — | 1 | 7.51 |
| CHEMBL360624 | — | — | 1 | 7.46 |
| CHEMBL1180184 | — | — | 1 | 7.40 |
| CHEMBL186139 | — | — | 1 | 7.22 |
| CHEMBL360621 | — | — | 1 | 7.22 |
| CHEMBL185258 | — | — | 1 | 7.19 |
| CHEMBL137175 | — | — | 1 | 7.16 |
| CHEMBL185106 | — | — | 1 | 6.89 |
| CHEMBL341700 | — | — | 1 | 6.89 |
| CHEMBL185137 | — | — | 1 | 6.82 |
| CHEMBL425707 | — | — | 1 | 6.82 |
| CHEMBL119859 | — | — | 1 | 6.72 |
| CHEMBL185230 | — | — | 1 | 6.58 |
| CHEMBL185006 | — | — | 2 | 6.42 |
| CHEMBL121663 | DEQUALINIUM CHLORIDE | 4.0 | 1 | 6.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL420873 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL117908 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL184300 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL185146 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL181911 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL183644 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL184858 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL181912 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL430146 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL184891 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL182716 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL360624 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL1180184 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL186139 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL360621 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL185258 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL137175 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL341700 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL185106 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL185137 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL425707 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL119859 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL185230 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL185006 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL185006 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL121663 | DEQUALINIUM CHLORIDE | IC50 | = | 900.0 | nM | 6.05 |