Assay Detail
Functional
CHEMBL699663
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Evaluated for K-ATP activity as in vitro bladder relaxation in spontaneous Landrace pig detrusor strips (SLPD)
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Sus scrofa |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Sulfonylurea receptors; K-ATP channels (CHEMBL2095152) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Homo sapiens |
Publication
Synthesis and structure-activity relationships of a novel series of 2,3,5,6,7,9-hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide K(ATP) channel openers: discovery of (-)-(9S)-9-(3-bromo-4-fluorophenyl)-2,3,5,6,7,9- hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide (A-278637), a potent K(ATP) opener that selectively inhibits spontaneous bladder contractions.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 6 | 7.36 | 7.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3138553 | — | — | 1 | 7.90 |
| CHEMBL11458 | — | — | 1 | 7.66 |
| CHEMBL3138607 | — | — | 1 | 7.64 |
| CHEMBL11684 | (-)-CROMAKALIM | — | 1 | 7.46 |
| CHEMBL2062142 | — | — | 1 | 6.99 |
| CHEMBL18861 | ZD-6169 | — | 1 | 6.53 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3138553 | — | EC50 | = | 12.59 | nM | 7.90 |
| CHEMBL11458 | — | EC50 | = | 21.88 | nM | 7.66 |
| CHEMBL3138607 | — | EC50 | = | 22.91 | nM | 7.64 |
| CHEMBL11684 | (-)-CROMAKALIM | EC50 | = | 34.67 | nM | 7.46 |
| CHEMBL2062142 | — | EC50 | = | 102.33 | nM | 6.99 |
| CHEMBL18861 | ZD-6169 | EC50 | = | 295.12 | nM | 6.53 |