Assay Detail
Binding
CHEMBL2422341
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at alpha-1B adrenoreceptor in Sprague-Dawley rat spleen assessed as inhibition of phenylephrine-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 | Spleen |
| 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 | 8.31 | 9.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3216590 | — | — | 1 | 9.08 |
| CHEMBL2419769 | — | — | 1 | 8.68 |
| CHEMBL2419771 | — | — | 1 | 8.49 |
| CHEMBL2419765 | — | — | 1 | 7.77 |
| CHEMBL543741 | — | — | 1 | 7.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3216590 | — | Kd | = | 0.8318 | nM | 9.08 |
| CHEMBL2419769 | — | Kd | = | 2.089 | nM | 8.68 |
| CHEMBL2419771 | — | Kd | = | 3.236 | nM | 8.49 |
| CHEMBL2419765 | — | Kd | = | 16.98 | nM | 7.77 |
| CHEMBL543741 | — | Kd | = | 28.18 | nM | 7.55 |