Assay Detail
Functional
CHEMBL800389
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Alpha-2-adrenoceptor blocking activity was determined by antagonism of clonidine induced depression of the twitch responses of the field stimulated prostatic portion of the vas deferens and the potency was expressed as pA2.
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Vas deferens |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Structure-activity relationships for prazosin and WB 4101 analogues as alpha 1-adrenoreceptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 9 | 5.74 | 6.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL556001 | 2- (2,6-DIMETHOXYPHENOXYETHYL)AMINOMETHYL-1,4-BENZODIOXANE HYDROCHLORIDE (WB 4101) | — | 1 | 6.29 |
| CHEMBL544690 | — | — | 1 | 6.28 |
| CHEMBL543984 | — | — | 1 | 6.17 |
| CHEMBL542075 | — | — | 1 | 5.94 |
| CHEMBL554232 | — | — | 1 | 5.85 |
| CHEMBL1558 | PRAZOSIN HYDROCHLORIDE | 4.0 | 1 | 5.81 |
| CHEMBL555983 | — | — | 1 | 5.37 |
| CHEMBL538219 | — | — | 1 | 5.22 |
| CHEMBL544221 | — | — | 1 | 4.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL556001 | 2- (2,6-DIMETHOXYPHENOXYETHYL)AMINOMETHYL-1,4-BENZODIOXANE HYDROCHLORIDE (WB 4101) | Kd | = | 512.86 | nM | 6.29 |
| CHEMBL544690 | — | Kd | = | 524.81 | nM | 6.28 |
| CHEMBL543984 | — | Kd | = | 676.08 | nM | 6.17 |
| CHEMBL542075 | — | Kd | = | 1148.15 | nM | 5.94 |
| CHEMBL554232 | — | Kd | = | 1412.54 | nM | 5.85 |
| CHEMBL1558 | PRAZOSIN HYDROCHLORIDE | Kd | = | 1548.82 | nM | 5.81 |
| CHEMBL555983 | — | Kd | = | 4265.8 | nM | 5.37 |
| CHEMBL538219 | — | Kd | = | 6025.6 | nM | 5.22 |
| CHEMBL544221 | — | Kd | = | 19498.45 | nM | 4.71 |