Assay Detail
Binding
CHEMBL647662
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Binding affinity towards Alpha-2 adrenergic receptor in rat cerebral cortex using [3H]rauwolscine as radioligand
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Synthesis, absolute configuration, and biological profile of the enantiomers of trans-[2-(2,6-dimethoxyphenoxy)ethyl] [(3-p-tolyl-2,3-dihydro-1,4-benzodioxin-2-yl)methyl]amine (mephendioxan), a potent competitive alpha 1A-adrenoreceptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 6.20 | 7.83 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL25554 | — | — | 1 | 7.83 |
| CHEMBL76168 | — | — | 1 | 6.36 |
| CHEMBL405355 | NIGULDIPINE | 2.0 | 1 | 5.79 |
| CHEMBL286565 | — | — | 1 | 5.67 |
| CHEMBL72657 | — | — | 1 | 5.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL25554 | — | Ki | = | 14.72 | nM | 7.83 |
| CHEMBL76168 | — | Ki | = | 432.4 | nM | 6.36 |
| CHEMBL405355 | NIGULDIPINE | Ki | = | 1611.0 | nM | 5.79 |
| CHEMBL286565 | — | Ki | = | 2142.0 | nM | 5.67 |
| CHEMBL72657 | — | Ki | = | 4293.0 | nM | 5.37 |