Assay Detail
Binding
CHEMBL1000350
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activation of large-conductance calcium-activated potassium channel-mediated vasorelaxation in endothelium-denuded normotensive Wistar rat thoracic aorta assessed as potassium chloride-induced contractile tension
18
Total Activities
18
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
Novel 1,4-benzothiazine derivatives as large conductance Ca2+-activated potassium channel openers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Activity | 11 | - | - |
| IC50 | 7 | 5.41 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL496460 | — | — | 1 | 7.40 |
| CHEMBL498516 | — | — | 1 | 6.21 |
| CHEMBL384903 | — | — | 1 | 5.30 |
| CHEMBL498702 | — | — | 1 | 5.20 |
| CHEMBL525555 | — | — | 1 | 4.80 |
| CHEMBL526824 | — | — | 1 | 4.65 |
| CHEMBL525920 | — | — | 1 | 4.30 |
| CHEMBL442643 | — | — | 1 | - |
| CHEMBL497862 | — | — | 1 | - |
| CHEMBL449286 | — | — | 1 | - |
| CHEMBL497861 | — | — | 1 | - |
| CHEMBL450728 | — | — | 1 | - |
| CHEMBL498518 | — | — | 1 | - |
| CHEMBL498502 | — | — | 1 | - |
| CHEMBL496461 | — | — | 1 | - |
| CHEMBL454472 | — | — | 1 | - |
| CHEMBL507244 | — | — | 1 | - |
| CHEMBL498517 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL496460 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL498516 | — | IC50 | = | 616.6 | nM | 6.21 |
| CHEMBL384903 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL498702 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL525555 | — | IC50 | = | 15848.93 | nM | 4.80 |
| CHEMBL526824 | — | IC50 | = | 22387.21 | nM | 4.65 |
| CHEMBL525920 | — | IC50 | = | 50118.72 | nM | 4.30 |
| CHEMBL442643 | — | Activity | - | — | - | |
| CHEMBL497862 | — | Activity | - | — | - | |
| CHEMBL449286 | — | Activity | - | — | - | |
| CHEMBL497861 | — | Activity | - | — | - | |
| CHEMBL450728 | — | Activity | <= | 50.0 | % | - |
| CHEMBL498518 | — | Activity | <= | 50.0 | % | - |
| CHEMBL498502 | — | Activity | <= | 50.0 | % | - |
| CHEMBL496461 | — | Activity | <= | 50.0 | % | - |
| CHEMBL454472 | — | Activity | <= | 50.0 | % | - |
| CHEMBL507244 | — | Activity | <= | 50.0 | % | - |
| CHEMBL498517 | — | Activity | <= | 50.0 | % | - |