Assay Detail
Binding
CHEMBL2422342
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at alpha-1A adrenoreceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced tissue contraction after 30 mins by Schild plot analysis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Vas deferens |
| Confidence | 9 — Direct single protein target |
| 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 | 5 | 7.80 | 8.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2419765 | — | — | 1 | 8.31 |
| CHEMBL2419769 | — | — | 1 | 8.26 |
| CHEMBL3216590 | — | — | 1 | 8.03 |
| CHEMBL2419771 | — | — | 1 | 7.47 |
| CHEMBL543741 | — | — | 1 | 6.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2419765 | — | Kd | = | 4.898 | nM | 8.31 |
| CHEMBL2419769 | — | Kd | = | 5.495 | nM | 8.26 |
| CHEMBL3216590 | — | Kd | = | 9.333 | nM | 8.03 |
| CHEMBL2419771 | — | Kd | = | 33.88 | nM | 7.47 |
| CHEMBL543741 | — | Kd | = | 114.82 | nM | 6.94 |