Assay Detail
Functional
CHEMBL798079
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Alpha-1-Adrenoceptor blocking activity as antagonism of (-)-norepinephrine induced contractions of epididymal vas deferens
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Vas deferens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
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 | 7.80 | 8.83 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL556001 | 2- (2,6-DIMETHOXYPHENOXYETHYL)AMINOMETHYL-1,4-BENZODIOXANE HYDROCHLORIDE (WB 4101) | — | 1 | 8.83 |
| CHEMBL538219 | — | — | 1 | 8.81 |
| CHEMBL1558 | PRAZOSIN HYDROCHLORIDE | 4.0 | 1 | 8.74 |
| CHEMBL542075 | — | — | 1 | 7.88 |
| CHEMBL545387 | — | — | 1 | 7.86 |
| CHEMBL543984 | — | — | 1 | 7.22 |
| CHEMBL554232 | — | — | 1 | 7.19 |
| CHEMBL555983 | — | — | 1 | 7.18 |
| CHEMBL544221 | — | — | 1 | 6.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL556001 | 2- (2,6-DIMETHOXYPHENOXYETHYL)AMINOMETHYL-1,4-BENZODIOXANE HYDROCHLORIDE (WB 4101) | Kd | = | 1.479 | nM | 8.83 |
| CHEMBL538219 | — | Kd | = | 1.549 | nM | 8.81 |
| CHEMBL1558 | PRAZOSIN HYDROCHLORIDE | Kd | = | 1.82 | nM | 8.74 |
| CHEMBL542075 | — | Kd | = | 13.18 | nM | 7.88 |
| CHEMBL545387 | — | Kd | = | 13.8 | nM | 7.86 |
| CHEMBL543984 | — | Kd | = | 60.26 | nM | 7.22 |
| CHEMBL554232 | — | Kd | = | 64.57 | nM | 7.19 |
| CHEMBL555983 | — | Kd | = | 66.07 | nM | 7.18 |
| CHEMBL544221 | — | Kd | = | 354.81 | nM | 6.45 |