Assay Detail
Functional
CHEMBL2383108
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Vasorelaxant activity in Wistar rat endothelium-denuded aortic rings assessed as reduction of KCl-induced contraction
12
Total Activities
12
Compounds Tested
1
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 | 12 | 6.91 | 10.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL121402 | — | — | 1 | 10.38 |
| CHEMBL2381499 | — | — | 1 | 8.84 |
| CHEMBL2381493 | — | — | 1 | 8.08 |
| CHEMBL2381495 | — | — | 1 | 7.18 |
| CHEMBL2381500 | — | — | 1 | 6.81 |
| CHEMBL100 | LEVCROMAKALIM | 2.0 | 1 | 6.49 |
| CHEMBL2381494 | — | — | 1 | 6.27 |
| CHEMBL2381496 | — | — | 1 | 6.14 |
| CHEMBL2381498 | — | — | 1 | 6.10 |
| CHEMBL2381497 | — | — | 1 | 6.03 |
| CHEMBL2381501 | — | — | 1 | 5.40 |
| CHEMBL2381502 | — | — | 1 | 5.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL121402 | — | IC50 | = | 0.04169 | nM | 10.38 |
| CHEMBL2381499 | — | IC50 | = | 1.445 | nM | 8.84 |
| CHEMBL2381493 | — | IC50 | = | 8.318 | nM | 8.08 |
| CHEMBL2381495 | — | IC50 | = | 66.07 | nM | 7.18 |
| CHEMBL2381500 | — | IC50 | = | 154.88 | nM | 6.81 |
| CHEMBL100 | LEVCROMAKALIM | IC50 | = | 323.59 | nM | 6.49 |
| CHEMBL2381494 | — | IC50 | = | 537.03 | nM | 6.27 |
| CHEMBL2381496 | — | IC50 | = | 724.44 | nM | 6.14 |
| CHEMBL2381498 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL2381497 | — | IC50 | = | 933.25 | nM | 6.03 |
| CHEMBL2381501 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL2381502 | — | IC50 | = | 6606.93 | nM | 5.18 |