Assay Detail
Binding
CHEMBL876560
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Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Syntheses of 2,5- and 2,6-difluoronorepinephrine, 2,5-difluoroepinephrine, and 2,6-difluorophenylephrine: effect of disubstitution with fluorine on adrenergic activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 5.23 | 5.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL679 | EPINEPHRINE | 4.0 | 1 | 5.92 |
| CHEMBL129190 | — | — | 1 | 5.82 |
| CHEMBL1437 | NOREPINEPHRINE | 4.0 | 1 | 5.80 |
| CHEMBL43711 | — | — | 1 | 5.75 |
| CHEMBL126347 | — | — | 1 | 5.64 |
| CHEMBL287587 | — | — | 1 | 5.60 |
| CHEMBL302451 | — | — | 1 | 5.40 |
| CHEMBL338564 | — | — | 1 | 5.25 |
| CHEMBL1215 | PHENYLEPHRINE | 4.0 | 1 | 4.89 |
| CHEMBL281232 | — | — | 1 | 4.35 |
| CHEMBL42359 | — | — | 1 | 4.20 |
| CHEMBL340189 | — | — | 1 | 4.09 |
| CHEMBL61372 | — | — | 1 | - |
| CHEMBL435802 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL679 | EPINEPHRINE | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL129190 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL1437 | NOREPINEPHRINE | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL43711 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL126347 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL287587 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL302451 | — | Ki | = | 4000.0 | nM | 5.40 |
| CHEMBL338564 | — | Ki | = | 5600.0 | nM | 5.25 |
| CHEMBL1215 | PHENYLEPHRINE | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL281232 | — | Ki | = | 45000.0 | nM | 4.35 |
| CHEMBL42359 | — | Ki | = | 63000.0 | nM | 4.20 |
| CHEMBL340189 | — | Ki | = | 81000.0 | nM | 4.09 |
| CHEMBL61372 | — | Ki | = | 180000.0 | nM | - |
| CHEMBL435802 | — | Ki | > | 50000.0 | nM | - |