Assay Detail
Functional
CHEMBL908308
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Activity against pig bladder KATP channel opening assessed as ability to relax field-stimulated pig detrusor
30
Total Activities
22
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Sus scrofa |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Effects of substitution on 9-(3-bromo-4-fluorophenyl)-5,9-dihydro-3H,4H-2,6-dioxa-4- azacyclopenta[b]naphthalene-1,8-dione, a dihydropyridine ATP-sensitive potassium channel opener.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 27 | 6.23 | 7.45 |
| Activity | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL426334 | — | — | 1 | 7.45 |
| CHEMBL11458 | — | — | 1 | 7.07 |
| CHEMBL386228 | — | — | 1 | 6.99 |
| CHEMBL320983 | — | — | 1 | 6.90 |
| CHEMBL384576 | — | — | 1 | 6.89 |
| CHEMBL214566 | — | — | 1 | 6.89 |
| CHEMBL217511 | — | — | 1 | 6.67 |
| CHEMBL426160 | — | — | 1 | 6.64 |
| CHEMBL11684 | (-)-CROMAKALIM | — | 1 | 6.59 |
| CHEMBL215375 | — | — | 4 | 6.55 |
| CHEMBL214841 | — | — | 3 | 6.29 |
| CHEMBL2112487 | — | — | 1 | 6.23 |
| CHEMBL2062142 | — | — | 1 | 6.17 |
| CHEMBL384078 | — | — | 3 | 6.05 |
| CHEMBL215681 | — | — | 2 | 6.05 |
| CHEMBL214616 | — | — | 1 | 5.92 |
| CHEMBL386628 | — | — | 1 | 5.89 |
| CHEMBL386843 | — | — | 1 | 5.78 |
| CHEMBL424909 | — | — | 1 | 5.69 |
| CHEMBL216256 | — | — | 1 | 5.64 |
| CHEMBL18861 | ZD-6169 | — | 1 | 5.56 |
| CHEMBL387063 | — | — | 1 | 4.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL426334 | — | EC50 | = | 35.48 | nM | 7.45 |
| CHEMBL11458 | — | EC50 | = | 85.11 | nM | 7.07 |
| CHEMBL386228 | — | EC50 | = | 102.33 | nM | 6.99 |
| CHEMBL320983 | — | EC50 | = | 125.89 | nM | 6.90 |
| CHEMBL384576 | — | EC50 | = | 128.82 | nM | 6.89 |
| CHEMBL214566 | — | EC50 | = | 128.82 | nM | 6.89 |
| CHEMBL217511 | — | EC50 | = | 213.8 | nM | 6.67 |
| CHEMBL426160 | — | EC50 | = | 229.09 | nM | 6.64 |
| CHEMBL11684 | (-)-CROMAKALIM | EC50 | = | 257.04 | nM | 6.59 |
| CHEMBL215375 | — | EC50 | = | 281.84 | nM | 6.55 |
| CHEMBL215375 | — | EC50 | = | 489.78 | nM | 6.31 |
| CHEMBL214841 | — | EC50 | = | 512.86 | nM | 6.29 |
| CHEMBL2112487 | — | EC50 | = | 588.84 | nM | 6.23 |
| CHEMBL2062142 | — | EC50 | = | 676.08 | nM | 6.17 |
| CHEMBL214841 | — | EC50 | = | 794.33 | nM | 6.10 |
| CHEMBL384078 | — | EC50 | = | 891.25 | nM | 6.05 |
| CHEMBL215681 | — | EC50 | = | 891.25 | nM | 6.05 |
| CHEMBL384078 | — | EC50 | = | 954.99 | nM | 6.02 |
| CHEMBL214616 | — | EC50 | = | 1202.26 | nM | 5.92 |
| CHEMBL386628 | — | EC50 | = | 1288.25 | nM | 5.89 |
| CHEMBL386843 | — | EC50 | = | 1659.59 | nM | 5.78 |
| CHEMBL424909 | — | EC50 | = | 2041.74 | nM | 5.69 |
| CHEMBL216256 | — | EC50 | = | 2290.87 | nM | 5.64 |
| CHEMBL215681 | — | EC50 | = | 2691.53 | nM | 5.57 |
| CHEMBL18861 | ZD-6169 | EC50 | = | 2754.23 | nM | 5.56 |
| CHEMBL215375 | — | EC50 | = | 2951.21 | nM | 5.53 |
| CHEMBL387063 | — | EC50 | = | 13489.63 | nM | 4.87 |
| CHEMBL215375 | — | Activity | - | — | - | |
| CHEMBL214841 | — | Activity | - | — | - | |
| CHEMBL384078 | — | Activity | - | — | - |