Assay Detail
Binding
CHEMBL1016925
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activation of BK channel in Wistar rat thoracic aorta assessed as relaxation of KCl-induced contraction
23
Total Activities
19
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Thoracic aorta |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Calcium-activated potassium channel subunit alpha-1 (CHEMBL5505) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
1,2,3-Triazol-carboxanilides and 1,2,3-triazol-(N-benzyl)-carboxamides as BK-potassium channel activators. XII.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Emax | 19 | - | - |
| IC50 | 4 | 4.85 | 5.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL384903 | — | — | 2 | 5.29 |
| CHEMBL511502 | — | — | 2 | 4.75 |
| CHEMBL511864 | — | — | 2 | 4.69 |
| CHEMBL517023 | — | — | 2 | 4.66 |
| CHEMBL464760 | — | — | 1 | - |
| CHEMBL461877 | — | — | 1 | - |
| CHEMBL459755 | — | — | 1 | - |
| CHEMBL445299 | — | — | 1 | - |
| CHEMBL459754 | — | — | 1 | - |
| CHEMBL458863 | — | — | 1 | - |
| CHEMBL456036 | — | — | 1 | - |
| CHEMBL456897 | — | — | 1 | - |
| CHEMBL456896 | — | — | 1 | - |
| CHEMBL456273 | — | — | 1 | - |
| CHEMBL456060 | — | — | 1 | - |
| CHEMBL456061 | — | — | 1 | - |
| CHEMBL456274 | — | — | 1 | - |
| CHEMBL457346 | — | — | 1 | - |
| CHEMBL456895 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL384903 | — | IC50 | = | 5128.61 | nM | 5.29 |
| CHEMBL511502 | — | IC50 | = | 17782.79 | nM | 4.75 |
| CHEMBL511864 | — | IC50 | = | 20417.38 | nM | 4.69 |
| CHEMBL517023 | — | IC50 | = | 21877.62 | nM | 4.66 |
| CHEMBL384903 | — | Emax | = | 94.0 | % | - |
| CHEMBL517023 | — | Emax | = | 76.0 | % | - |
| CHEMBL464760 | — | Emax | = | 24.0 | % | - |
| CHEMBL461877 | — | Emax | = | 49.0 | % | - |
| CHEMBL459755 | — | Emax | = | 51.0 | % | - |
| CHEMBL445299 | — | Emax | = | 48.0 | % | - |
| CHEMBL511864 | — | Emax | = | 81.0 | % | - |
| CHEMBL459754 | — | Emax | = | 35.0 | % | - |
| CHEMBL458863 | — | Emax | = | 52.0 | % | - |
| CHEMBL456036 | — | Emax | = | 53.0 | % | - |
| CHEMBL457346 | — | Emax | = | 39.0 | % | - |
| CHEMBL456897 | — | Emax | = | 43.0 | % | - |
| CHEMBL456896 | — | Emax | < | 20.0 | % | - |
| CHEMBL456273 | — | Emax | = | 37.0 | % | - |
| CHEMBL456060 | — | Emax | = | 25.0 | % | - |
| CHEMBL456061 | — | Emax | < | 20.0 | % | - |
| CHEMBL456274 | — | Emax | < | 20.0 | % | - |
| CHEMBL456895 | — | Emax | < | 20.0 | % | - |
| CHEMBL511502 | — | Emax | = | 89.0 | % | - |