Assay Detail
Functional
CHEMBL699660
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
31
Total Activities
31
Compounds Tested
2
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 |
|---|---|---|---|
| Log EC50 | 29 | - | - |
| EC50 | 2 | 5.51 | 6.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3138593 | — | — | 1 | 6.32 |
| CHEMBL3138591 | — | — | 1 | 4.69 |
| CHEMBL3138567 | — | — | 1 | - |
| CHEMBL3138559 | — | — | 1 | - |
| CHEMBL3138589 | — | — | 1 | - |
| CHEMBL3138585 | — | — | 1 | - |
| CHEMBL3138594 | — | — | 1 | - |
| CHEMBL3138605 | — | — | 1 | - |
| CHEMBL3138550 | — | — | 1 | - |
| CHEMBL3138556 | — | — | 1 | - |
| CHEMBL3138590 | — | — | 1 | - |
| CHEMBL3138602 | — | — | 1 | - |
| CHEMBL3138604 | — | — | 1 | - |
| CHEMBL3138569 | — | — | 1 | - |
| CHEMBL3138601 | — | — | 1 | - |
| CHEMBL3138576 | — | — | 1 | - |
| CHEMBL2111691 | — | — | 1 | - |
| CHEMBL3138563 | — | — | 1 | - |
| CHEMBL3138584 | — | — | 1 | - |
| CHEMBL3138571 | — | — | 1 | - |
| CHEMBL108586 | — | — | 1 | - |
| CHEMBL110710 | — | — | 1 | - |
| CHEMBL3138583 | — | — | 1 | - |
| CHEMBL3138547 | — | — | 1 | - |
| CHEMBL3138552 | — | — | 1 | - |
| CHEMBL3138572 | — | — | 1 | - |
| CHEMBL3138580 | — | — | 1 | - |
| CHEMBL3138606 | — | — | 1 | - |
| CHEMBL3138598 | — | — | 1 | - |
| CHEMBL3138546 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3138593 | — | EC50 | = | 478.63 | nM | 6.32 |
| CHEMBL3138591 | — | EC50 | = | 20417.38 | nM | 4.69 |
| CHEMBL3138612 | — | Log EC50 | - | — | - | |
| CHEMBL3138567 | — | Log EC50 | - | — | - | |
| CHEMBL3138559 | — | Log EC50 | - | — | - | |
| CHEMBL3138589 | — | Log EC50 | - | — | - | |
| CHEMBL3138585 | — | Log EC50 | - | — | - | |
| CHEMBL3138594 | — | Log EC50 | - | — | - | |
| CHEMBL3138605 | — | Log EC50 | - | — | - | |
| CHEMBL3138550 | — | Log EC50 | - | — | - | |
| CHEMBL3138556 | — | Log EC50 | = | - | — | - |
| CHEMBL3138590 | — | Log EC50 | - | — | - | |
| CHEMBL3138602 | — | Log EC50 | - | — | - | |
| CHEMBL3138604 | — | Log EC50 | - | — | - | |
| CHEMBL3138569 | — | Log EC50 | - | — | - | |
| CHEMBL3138601 | — | Log EC50 | - | — | - | |
| CHEMBL3138576 | — | Log EC50 | - | — | - | |
| CHEMBL2111691 | — | Log EC50 | - | — | - | |
| CHEMBL3138563 | — | Log EC50 | - | — | - | |
| CHEMBL3138584 | — | Log EC50 | - | — | - | |
| CHEMBL3138571 | — | Log EC50 | - | — | - | |
| CHEMBL108586 | — | Log EC50 | - | — | - | |
| CHEMBL110710 | — | Log EC50 | - | — | - | |
| CHEMBL3138583 | — | Log EC50 | - | — | - | |
| CHEMBL3138547 | — | Log EC50 | - | — | - | |
| CHEMBL3138552 | — | Log EC50 | - | — | - | |
| CHEMBL3138572 | — | Log EC50 | - | — | - | |
| CHEMBL3138580 | — | Log EC50 | - | — | - | |
| CHEMBL3138606 | — | Log EC50 | - | — | - | |
| CHEMBL3138598 | — | Log EC50 | - | — | - | |
| CHEMBL3138546 | — | Log EC50 | - | — | - |