Assay Detail
Functional
CHEMBL2383109
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Vasorelaxant activity in Wistar rat endothelium-denuded aortic rings assessed as reduction of KCl-induced contraction in presence of glibenclamide
12
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Aorta |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
1,4-Benzothiazine ATP-sensitive potassium channel openers: modifications at the C-2 and C-6 positions.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.79 | 8.08 |
| pIC50 | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL121402 | — | — | 1 | 8.08 |
| CHEMBL2381499 | — | — | 1 | 7.25 |
| CHEMBL2381493 | — | — | 1 | 6.15 |
| CHEMBL100 | LEVCROMAKALIM | 2.0 | 1 | 5.60 |
| CHEMBL2381500 | — | — | 1 | 5.19 |
| CHEMBL2381497 | — | — | 1 | 4.71 |
| CHEMBL2381496 | — | — | 1 | 4.68 |
| CHEMBL2381494 | — | — | 1 | 4.63 |
| CHEMBL2381502 | — | — | 1 | - |
| CHEMBL2381501 | — | — | 1 | - |
| CHEMBL2381498 | — | — | 1 | - |
| CHEMBL2381495 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL121402 | — | IC50 | = | 8.318 | nM | 8.08 |
| CHEMBL2381499 | — | IC50 | = | 56.23 | nM | 7.25 |
| CHEMBL2381493 | — | IC50 | = | 707.95 | nM | 6.15 |
| CHEMBL100 | LEVCROMAKALIM | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL2381500 | — | IC50 | = | 6456.54 | nM | 5.19 |
| CHEMBL2381497 | — | IC50 | = | 19498.45 | nM | 4.71 |
| CHEMBL2381496 | — | IC50 | = | 20892.96 | nM | 4.68 |
| CHEMBL2381494 | — | IC50 | = | 23442.29 | nM | 4.63 |
| CHEMBL2381502 | — | pIC50 | - | — | - | |
| CHEMBL2381501 | — | pIC50 | - | — | - | |
| CHEMBL2381498 | — | pIC50 | - | — | - | |
| CHEMBL2381495 | — | pIC50 | - | — | - |