Assay Detail
Binding
CHEMBL839653
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Inhibition of [125I]apamin binding to calcium-activated potassium (SK) channel of rat cortex
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Small conductance calcium-activated potassium channel (CHEMBL2096673) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
Synthesis and radioligand binding studies of C-5- and C-8-substituted 1-(3,4-dimethoxybenzyl)-2,2-dimethyl-1,2,3,4-tetrahydroisoquinoliniums as SK channel blockers related to N-methyl-laudanosine and N-methyl-noscapine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 5.39 | 5.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL215370 | LAUDANOSINE METHIODIDE | — | 1 | 5.80 |
| CHEMBL365744 | — | — | 1 | 5.80 |
| CHEMBL186011 | — | — | 1 | 5.58 |
| CHEMBL190220 | — | — | 1 | 5.44 |
| CHEMBL525408 | APAMIN | — | 1 | 5.42 |
| CHEMBL190992 | — | — | 1 | 5.31 |
| CHEMBL188644 | — | — | 1 | 5.26 |
| CHEMBL187736 | — | — | 1 | 5.17 |
| CHEMBL427162 | — | — | 1 | 5.12 |
| CHEMBL190003 | — | — | 1 | 5.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL215370 | LAUDANOSINE METHIODIDE | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL365744 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL186011 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL190220 | — | Ki | = | 3600.0 | nM | 5.44 |
| CHEMBL525408 | APAMIN | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL190992 | — | Ki | = | 4900.0 | nM | 5.31 |
| CHEMBL188644 | — | Ki | = | 5500.0 | nM | 5.26 |
| CHEMBL187736 | — | Ki | = | 6800.0 | nM | 5.17 |
| CHEMBL427162 | — | Ki | = | 7600.0 | nM | 5.12 |
| CHEMBL190003 | — | Ki | = | 9300.0 | nM | 5.03 |