Assay Detail
Binding
CHEMBL660002
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Binding affinity was determined by displacement of [3H]P1075 from its binding sites in canine cardiac membranes
16
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Canis lupus familiaris |
| Tissue | Heart |
| Subcellular | Membrane |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Binding of ATP-sensitive potassium channel (KATP) openers to cardiac membranes: correlation of binding affinities with cardioprotective and smooth muscle relaxing potencies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 6.41 | 7.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL11458 | — | — | 1 | 7.57 |
| CHEMBL93344 | — | — | 1 | 7.24 |
| CHEMBL328308 | — | — | 1 | 7.13 |
| CHEMBL19169 | — | — | 1 | 7.00 |
| CHEMBL472 | GLYBURIDE | 4.0 | 1 | 6.89 |
| CHEMBL93196 | — | — | 1 | 6.80 |
| CHEMBL1159 | PINACIDIL ANHYDROUS | 4.0 | 1 | 6.50 |
| CHEMBL93834 | — | — | 1 | 6.46 |
| CHEMBL328082 | — | — | 1 | 6.32 |
| CHEMBL93835 | — | — | 1 | 6.17 |
| CHEMBL11684 | (-)-CROMAKALIM | — | 2 | 5.96 |
| CHEMBL90665 | — | — | 1 | 5.14 |
| CHEMBL96267 | — | — | 1 | - |
| CHEMBL90631 | — | — | 1 | - |
| CHEMBL327884 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL11458 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL93344 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL328308 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL19169 | — | Ki | = | 99.0 | nM | 7.00 |
| CHEMBL472 | GLYBURIDE | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL93196 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL1159 | PINACIDIL ANHYDROUS | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL93834 | — | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL328082 | — | Ki | = | 480.0 | nM | 6.32 |
| CHEMBL93835 | — | Ki | = | 680.0 | nM | 6.17 |
| CHEMBL11684 | (-)-CROMAKALIM | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL90665 | — | Ki | = | 7300.0 | nM | 5.14 |
| CHEMBL11684 | (-)-CROMAKALIM | Ki | = | 72000.0 | nM | 4.14 |
| CHEMBL96267 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL90631 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL327884 | — | Ki | > | 30000.0 | nM | - |