Assay Detail
Functional
CHEMBL701216
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Evaluated for K-ATP activity in terms of stable twitch response through field-stimulated landrace pig detrusor assay
37
Total Activities
36
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 | 37 | 5.97 | 7.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3138586 | — | — | 1 | 7.51 |
| CHEMBL11458 | — | — | 1 | 7.07 |
| CHEMBL3138548 | — | — | 1 | 6.96 |
| CHEMBL3138581 | — | — | 1 | 6.67 |
| CHEMBL3138607 | — | — | 1 | 6.63 |
| CHEMBL11684 | (-)-CROMAKALIM | — | 1 | 6.59 |
| CHEMBL420483 | — | — | 1 | 6.57 |
| CHEMBL3138560 | — | — | 1 | 6.55 |
| CHEMBL3138587 | — | — | 1 | 6.51 |
| CHEMBL3138565 | — | — | 1 | 6.48 |
| CHEMBL3138603 | — | — | 1 | 6.47 |
| CHEMBL3138561 | — | — | 2 | 6.44 |
| CHEMBL3138545 | — | — | 1 | 6.35 |
| CHEMBL3138596 | — | — | 1 | 6.27 |
| CHEMBL3138554 | — | — | 1 | 6.27 |
| CHEMBL3138564 | — | — | 1 | 6.18 |
| CHEMBL2062142 | — | — | 1 | 6.17 |
| CHEMBL3138588 | — | — | 1 | 6.17 |
| CHEMBL3138549 | — | — | 1 | 6.14 |
| CHEMBL324190 | — | — | 1 | 6.10 |
| CHEMBL3138592 | — | — | 1 | 6.01 |
| CHEMBL3138611 | — | — | 1 | 6.01 |
| CHEMBL3138555 | — | — | 1 | 5.77 |
| CHEMBL321982 | — | — | 1 | 5.65 |
| CHEMBL3138582 | — | — | 1 | 5.63 |
| CHEMBL3138570 | — | — | 1 | 5.61 |
| CHEMBL2112479 | — | — | 1 | 5.57 |
| CHEMBL18861 | ZD-6169 | — | 1 | 5.56 |
| CHEMBL3138577 | — | — | 1 | 5.25 |
| CHEMBL109159 | — | — | 1 | 5.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3138586 | — | EC50 | = | 30.9 | nM | 7.51 |
| CHEMBL11458 | — | EC50 | = | 85.11 | nM | 7.07 |
| CHEMBL3138548 | — | EC50 | = | 109.65 | nM | 6.96 |
| CHEMBL3138581 | — | EC50 | = | 213.8 | nM | 6.67 |
| CHEMBL3138607 | — | EC50 | = | 234.42 | nM | 6.63 |
| CHEMBL11684 | (-)-CROMAKALIM | EC50 | = | 257.04 | nM | 6.59 |
| CHEMBL420483 | — | EC50 | = | 269.15 | nM | 6.57 |
| CHEMBL3138560 | — | EC50 | = | 281.84 | nM | 6.55 |
| CHEMBL3138587 | — | EC50 | = | 309.03 | nM | 6.51 |
| CHEMBL3138565 | — | EC50 | = | 331.13 | nM | 6.48 |
| CHEMBL3138603 | — | EC50 | = | 338.84 | nM | 6.47 |
| CHEMBL3138561 | — | EC50 | = | 363.08 | nM | 6.44 |
| CHEMBL3138545 | — | EC50 | = | 446.68 | nM | 6.35 |
| CHEMBL3138596 | — | EC50 | = | 537.03 | nM | 6.27 |
| CHEMBL3138554 | — | EC50 | = | 537.03 | nM | 6.27 |
| CHEMBL3138564 | — | EC50 | = | 660.69 | nM | 6.18 |
| CHEMBL2062142 | — | EC50 | = | 676.08 | nM | 6.17 |
| CHEMBL3138588 | — | EC50 | = | 676.08 | nM | 6.17 |
| CHEMBL3138549 | — | EC50 | = | 724.44 | nM | 6.14 |
| CHEMBL324190 | — | EC50 | = | 794.33 | nM | 6.10 |
| CHEMBL3138592 | — | EC50 | = | 977.24 | nM | 6.01 |
| CHEMBL3138611 | — | EC50 | = | 977.24 | nM | 6.01 |
| CHEMBL3138555 | — | EC50 | = | 1698.24 | nM | 5.77 |
| CHEMBL321982 | — | EC50 | = | 2238.72 | nM | 5.65 |
| CHEMBL3138582 | — | EC50 | = | 2344.23 | nM | 5.63 |
| CHEMBL3138570 | — | EC50 | = | 2454.71 | nM | 5.61 |
| CHEMBL2112479 | — | EC50 | = | 2691.53 | nM | 5.57 |
| CHEMBL18861 | ZD-6169 | EC50 | = | 2754.23 | nM | 5.56 |
| CHEMBL3138577 | — | EC50 | = | 5623.41 | nM | 5.25 |
| CHEMBL3138561 | — | EC50 | = | 6760.83 | nM | 5.17 |
| CHEMBL109159 | — | EC50 | = | 8709.64 | nM | 5.06 |
| CHEMBL3138568 | — | EC50 | = | 9549.93 | nM | 5.02 |
| CHEMBL2052025 | — | EC50 | = | 9772.37 | nM | 5.01 |
| CHEMBL3138597 | — | EC50 | = | 11748.98 | nM | 4.93 |
| CHEMBL325805 | — | EC50 | = | 11748.98 | nM | 4.93 |
| CHEMBL3138557 | — | EC50 | = | 12882.5 | nM | 4.89 |
| CHEMBL3138566 | — | EC50 | = | 26302.68 | nM | 4.58 |