Assay Detail
Binding
CHEMBL645995
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Binding affinity towards Alpha-1D adrenergic receptor in rat brain using [3H]prazosin as radioligand
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| 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 | 6 | 7.48 | 8.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL25554 | — | — | 1 | 8.20 |
| CHEMBL72657 | — | — | 1 | 8.18 |
| CHEMBL42539 | — | — | 1 | 7.93 |
| CHEMBL405355 | NIGULDIPINE | 2.0 | 1 | 7.08 |
| CHEMBL76168 | — | — | 1 | 6.76 |
| CHEMBL286565 | — | — | 1 | 6.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL25554 | — | Ki | = | 6.26 | nM | 8.20 |
| CHEMBL72657 | — | Ki | = | 6.57 | nM | 8.18 |
| CHEMBL42539 | — | Ki | = | 11.76 | nM | 7.93 |
| CHEMBL405355 | NIGULDIPINE | Ki | = | 82.41 | nM | 7.08 |
| CHEMBL76168 | — | Ki | = | 175.1 | nM | 6.76 |
| CHEMBL286565 | — | Ki | = | 191.1 | nM | 6.72 |