Assay Detail
Functional
CHEMBL878707
Review assay metadata, readout intent, target linkage, and publication context from the same page.
K-ATP activity in terms of stable twitch response through field-stimulated landrace pig detrusor assay
28
Total Activities
26
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 tricyclic dihydropyridine-based KATP openers that potently inhibit bladder contractions in vitro.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 28 | 6.01 | 7.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL326901 | — | — | 1 | 7.03 |
| CHEMBL320983 | — | — | 1 | 6.90 |
| CHEMBL323159 | — | — | 1 | 6.87 |
| CHEMBL108969 | — | — | 1 | 6.75 |
| CHEMBL108547 | — | — | 1 | 6.69 |
| CHEMBL3138607 | — | — | 1 | 6.63 |
| CHEMBL11684 | (-)-CROMAKALIM | — | 1 | 6.59 |
| CHEMBL2111694 | — | — | 1 | 6.58 |
| CHEMBL107888 | — | — | 1 | 6.57 |
| CHEMBL109693 | — | — | 2 | 6.35 |
| CHEMBL110399 | — | — | 1 | 6.30 |
| CHEMBL326016 | — | — | 1 | 6.29 |
| CHEMBL2112487 | — | — | 1 | 6.23 |
| CHEMBL320931 | — | — | 1 | 6.18 |
| CHEMBL321455 | — | — | 1 | 6.07 |
| CHEMBL111204 | — | — | 1 | 6.02 |
| CHEMBL3138558 | — | — | 1 | 5.95 |
| CHEMBL323397 | — | — | 1 | 5.94 |
| CHEMBL108029 | — | — | 1 | 5.85 |
| CHEMBL110987 | — | — | 1 | 5.69 |
| CHEMBL325571 | — | — | 2 | 5.41 |
| CHEMBL106984 | — | — | 1 | 5.32 |
| CHEMBL106755 | — | — | 1 | 4.78 |
| CHEMBL432204 | — | — | 1 | 4.43 |
| CHEMBL3138562 | — | — | 1 | 4.30 |
| CHEMBL3138551 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL326901 | — | EC50 | = | 93.33 | nM | 7.03 |
| CHEMBL320983 | — | EC50 | = | 125.89 | nM | 6.90 |
| CHEMBL323159 | — | EC50 | = | 134.9 | nM | 6.87 |
| CHEMBL108969 | — | EC50 | = | 177.83 | nM | 6.75 |
| CHEMBL108547 | — | EC50 | = | 204.17 | nM | 6.69 |
| CHEMBL3138607 | — | EC50 | = | 234.42 | nM | 6.63 |
| CHEMBL11684 | (-)-CROMAKALIM | EC50 | = | 257.04 | nM | 6.59 |
| CHEMBL2111694 | — | EC50 | = | 263.03 | nM | 6.58 |
| CHEMBL107888 | — | EC50 | = | 269.15 | nM | 6.57 |
| CHEMBL109693 | — | EC50 | = | 446.68 | nM | 6.35 |
| CHEMBL110399 | — | EC50 | = | 501.19 | nM | 6.30 |
| CHEMBL326016 | — | EC50 | = | 512.86 | nM | 6.29 |
| CHEMBL2112487 | — | EC50 | = | 588.84 | nM | 6.23 |
| CHEMBL320931 | — | EC50 | = | 660.69 | nM | 6.18 |
| CHEMBL321455 | — | EC50 | = | 851.14 | nM | 6.07 |
| CHEMBL111204 | — | EC50 | = | 954.99 | nM | 6.02 |
| CHEMBL3138558 | — | EC50 | = | 1122.02 | nM | 5.95 |
| CHEMBL323397 | — | EC50 | = | 1148.15 | nM | 5.94 |
| CHEMBL108029 | — | EC50 | = | 1412.54 | nM | 5.85 |
| CHEMBL110987 | — | EC50 | = | 2041.74 | nM | 5.69 |
| CHEMBL325571 | — | EC50 | = | 3890.45 | nM | 5.41 |
| CHEMBL109693 | — | EC50 | = | 4466.84 | nM | 5.35 |
| CHEMBL106984 | — | EC50 | = | 4786.3 | nM | 5.32 |
| CHEMBL325571 | — | EC50 | = | 6918.31 | nM | 5.16 |
| CHEMBL106755 | — | EC50 | = | 16595.87 | nM | 4.78 |
| CHEMBL432204 | — | EC50 | = | 37153.52 | nM | 4.43 |
| CHEMBL3138562 | — | EC50 | = | 50118.72 | nM | 4.30 |
| CHEMBL3138551 | — | EC50 | = | 131825.67 | nM | - |