Assay Detail
Binding
CHEMBL2422339
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Antagonist activity at alpha-2 adrenoreceptor in Sprague-Dawley rat prostatic vas deferens assessed as reversal of clonidine-inhibited twitch responses of field-stimulated prostatic portion of vas deferens after 30 mins by Schild plot analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Vas deferens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
6-methoxy-7-benzofuranoxy and 6-methoxy-7-indolyloxy analogues of 2-[2-(2,6-Dimethoxyphenoxy)ethyl]aminomethyl-1,4-benzodioxane (WB4101):1 discovery of a potent and selective α1D-adrenoceptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 4 | 6.33 | 6.63 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2419771 | — | — | 1 | 6.63 |
| CHEMBL2419769 | — | — | 1 | 6.55 |
| CHEMBL2419765 | — | — | 1 | 6.09 |
| CHEMBL3216590 | — | — | 1 | 6.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2419771 | — | Kd | = | 234.42 | nM | 6.63 |
| CHEMBL2419769 | — | Kd | = | 281.84 | nM | 6.55 |
| CHEMBL2419765 | — | Kd | = | 812.83 | nM | 6.09 |
| CHEMBL3216590 | — | Kd | = | 891.25 | nM | 6.05 |