Assay Detail
Functional
CHEMBL785164
Review assay metadata, readout intent, target linkage, and publication context from the same page.
The blocking of apamin-sensitive [Ca2+]-activated K+ (SKCa) channel was assessed by the compounds ability to inhibit the after-hyperpolarization in cultured rat superior cervical ganglion neurons
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Tissue | Superior cervical ganglion |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Small conductance calcium-activated potassium channel (CHEMBL2096673) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
Synthesis, molecular modeling, and pharmacological testing of bis-quinolinium cyclophanes: potent, non-peptidic blockers of the apamin-sensitive Ca(2+)-activated K(+) channel.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 6.76 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL117908 | — | — | 1 | 8.52 |
| CHEMBL344807 | — | — | 1 | 7.60 |
| CHEMBL430146 | — | — | 1 | 7.55 |
| CHEMBL136488 | — | — | 1 | 7.22 |
| CHEMBL137175 | — | — | 1 | 7.16 |
| CHEMBL446445 | UCL-1530 | — | 1 | 7.10 |
| CHEMBL137155 | — | — | 1 | 7.05 |
| CHEMBL342213 | — | — | 1 | 7.00 |
| CHEMBL268556 | — | — | 1 | 6.96 |
| CHEMBL140380 | — | — | 1 | 6.92 |
| CHEMBL341700 | — | — | 1 | 6.89 |
| CHEMBL137266 | — | — | 1 | 6.82 |
| CHEMBL258254 | — | — | 1 | 6.82 |
| CHEMBL6266 | — | — | 1 | 6.77 |
| CHEMBL266885 | — | — | 1 | 6.75 |
| CHEMBL6361 | — | — | 1 | 6.72 |
| CHEMBL137116 | — | — | 1 | 6.68 |
| CHEMBL137256 | — | — | 1 | 6.60 |
| CHEMBL136303 | — | — | 1 | 6.58 |
| CHEMBL434234 | — | — | 1 | 6.55 |
| CHEMBL6354 | — | — | 1 | 6.54 |
| CHEMBL6356 | — | — | 1 | 6.51 |
| CHEMBL133311 | — | — | 1 | 6.44 |
| CHEMBL344620 | — | — | 1 | 6.42 |
| CHEMBL269729 | — | — | 1 | 6.42 |
| CHEMBL429017 | — | — | 1 | 6.39 |
| CHEMBL337108 | — | — | 1 | 6.37 |
| CHEMBL6315 | — | — | 1 | 6.35 |
| CHEMBL121663 | DEQUALINIUM CHLORIDE | 4.0 | 1 | 6.19 |
| CHEMBL422094 | — | — | 1 | 6.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL117908 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL344807 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL430146 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL136488 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL137175 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL446445 | UCL-1530 | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL137155 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL342213 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL268556 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL140380 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL341700 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL137266 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL258254 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL6266 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL266885 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL6361 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL137116 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL137256 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL136303 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL434234 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL6354 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL6356 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL133311 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL344620 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL269729 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL429017 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL337108 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL6315 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL121663 | DEQUALINIUM CHLORIDE | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL422094 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL135862 | — | IC50 | = | 2800.0 | nM | 5.55 |