Assay Detail
Functional
CHEMBL2155388
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Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 mins
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Vas deferens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Affinity and activity profiling of unichiral 8-substituted 1,4-benzodioxane analogues of WB4101 reveals a potent and selective α1B-adrenoceptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 6 | 8.32 | 9.98 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL215421 | — | — | 1 | 9.98 |
| CHEMBL2153555 | — | — | 1 | 9.56 |
| CHEMBL2153553 | — | — | 1 | 8.77 |
| CHEMBL2153557 | — | — | 1 | 7.54 |
| CHEMBL2153559 | — | — | 1 | 7.27 |
| CHEMBL2153551 | — | — | 1 | 6.78 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL215421 | — | Kd | = | 0.1047 | nM | 9.98 |
| CHEMBL2153555 | — | Kd | = | 0.2754 | nM | 9.56 |
| CHEMBL2153553 | — | Kd | = | 1.698 | nM | 8.77 |
| CHEMBL2153557 | — | Kd | = | 28.84 | nM | 7.54 |
| CHEMBL2153559 | — | Kd | = | 53.7 | nM | 7.27 |
| CHEMBL2153551 | — | Kd | = | 165.96 | nM | 6.78 |