Assay Detail
Binding
CHEMBL669632
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Inhibition of [3H]ouabain binding to Digitalis receptor in dog heart microsomes
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Canis lupus familiaris |
| Tissue | Heart |
| Subcellular | Microsomes |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium/potassium-transporting ATPase subunit alpha-1 (CHEMBL4838) ↗| Type | SINGLE PROTEIN |
| Organism | Canis lupus familiaris |
Publication
Synthesis and structure-activity relationships of 17beta-substituted 14beta-hydroxysteroid 3-(alpha-L-rhamnopyranoside)s: steroids that bind to the digitalis receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.72 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL254219 | DIGITOXIN | 4.0 | 1 | 8.10 |
| CHEMBL2069115 | — | — | 1 | 8.08 |
| CHEMBL2069118 | — | — | 1 | 7.89 |
| CHEMBL2069066 | — | — | 1 | 7.52 |
| CHEMBL2069075 | — | — | 1 | 7.34 |
| CHEMBL2069070 | — | — | 1 | 6.64 |
| CHEMBL2069067 | — | — | 1 | 6.18 |
| CHEMBL2069069 | — | — | 1 | 5.72 |
| CHEMBL2069072 | — | — | 1 | 5.66 |
| CHEMBL2069074 | — | — | 1 | 5.49 |
| CHEMBL2069071 | — | — | 1 | 5.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL254219 | DIGITOXIN | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2069115 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL2069118 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2069066 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2069075 | — | IC50 | = | 45.5 | nM | 7.34 |
| CHEMBL2069070 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL2069067 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL2069069 | — | IC50 | = | 1890.0 | nM | 5.72 |
| CHEMBL2069072 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL2069074 | — | IC50 | = | 3220.0 | nM | 5.49 |
| CHEMBL2069071 | — | IC50 | = | 4730.0 | nM | 5.33 |