Assay Detail
Functional
CHEMBL684560
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Effective concentration for stimulation of [3H]phosphoinositide formation in guinea pig synaptoneurosomes expressing alpha-1 receptor
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
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 |
|---|---|---|---|
| EC50 | 14 | 5.29 | 6.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL679 | EPINEPHRINE | 4.0 | 1 | 6.40 |
| CHEMBL42359 | — | — | 1 | 6.10 |
| CHEMBL1437 | NOREPINEPHRINE | 4.0 | 1 | 5.82 |
| CHEMBL126347 | — | — | 1 | 5.58 |
| CHEMBL43711 | — | — | 1 | 5.48 |
| CHEMBL281232 | — | — | 1 | 5.38 |
| CHEMBL340189 | — | — | 1 | 5.37 |
| CHEMBL1215 | PHENYLEPHRINE | 4.0 | 1 | 5.22 |
| CHEMBL61372 | — | — | 1 | 5.10 |
| CHEMBL62072 | — | — | 1 | 4.80 |
| CHEMBL302451 | — | — | 1 | 4.10 |
| CHEMBL338564 | — | — | 1 | 4.08 |
| CHEMBL287587 | — | — | 1 | - |
| CHEMBL435802 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL679 | EPINEPHRINE | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL42359 | — | EC50 | = | 800.0 | nM | 6.10 |
| CHEMBL1437 | NOREPINEPHRINE | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL126347 | — | EC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL43711 | — | EC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL281232 | — | EC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL340189 | — | EC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL1215 | PHENYLEPHRINE | EC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL61372 | — | EC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL62072 | — | EC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL302451 | — | EC50 | = | 80000.0 | nM | 4.10 |
| CHEMBL338564 | — | EC50 | = | 83000.0 | nM | 4.08 |
| CHEMBL287587 | — | EC50 | > | 180000.0 | nM | - |
| CHEMBL435802 | — | EC50 | > | 100000.0 | nM | - |