Assay Detail
Binding
CHEMBL875242
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Displacement of [3H]clonidine from adrenergic alpha 2 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 | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
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 | 6.58 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42359 | — | — | 1 | 8.05 |
| CHEMBL1437 | NOREPINEPHRINE | 4.0 | 1 | 7.42 |
| CHEMBL679 | EPINEPHRINE | 4.0 | 1 | 7.42 |
| CHEMBL43711 | — | — | 1 | 7.18 |
| CHEMBL281232 | — | — | 1 | 7.10 |
| CHEMBL129190 | — | — | 1 | 6.82 |
| CHEMBL61372 | — | — | 1 | 6.64 |
| CHEMBL1215 | PHENYLEPHRINE | 4.0 | 1 | 6.41 |
| CHEMBL435802 | — | — | 1 | 6.12 |
| CHEMBL340189 | — | — | 1 | 6.03 |
| CHEMBL126347 | — | — | 1 | 5.92 |
| CHEMBL302451 | — | — | 1 | 5.92 |
| CHEMBL287587 | — | — | 1 | 5.68 |
| CHEMBL338564 | — | — | 1 | 5.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42359 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL1437 | NOREPINEPHRINE | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL679 | EPINEPHRINE | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL43711 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL281232 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL129190 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL61372 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL1215 | PHENYLEPHRINE | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL435802 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL340189 | — | Ki | = | 940.0 | nM | 6.03 |
| CHEMBL126347 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL302451 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL287587 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL338564 | — | Ki | = | 3500.0 | nM | 5.46 |