Assay Detail
Functional
CHEMBL2155387
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Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate 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 | Prostate gland |
| 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 | 8.45 | 9.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL215421 | — | — | 1 | 9.49 |
| CHEMBL2153555 | — | — | 1 | 9.04 |
| CHEMBL2153557 | — | — | 1 | 8.92 |
| CHEMBL2153553 | — | — | 1 | 8.55 |
| CHEMBL2153559 | — | — | 1 | 7.40 |
| CHEMBL2153551 | — | — | 1 | 7.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL215421 | — | Kd | = | 0.3236 | nM | 9.49 |
| CHEMBL2153555 | — | Kd | = | 0.912 | nM | 9.04 |
| CHEMBL2153557 | — | Kd | = | 1.202 | nM | 8.92 |
| CHEMBL2153553 | — | Kd | = | 2.818 | nM | 8.55 |
| CHEMBL2153559 | — | Kd | = | 39.81 | nM | 7.40 |
| CHEMBL2153551 | — | Kd | = | 50.12 | nM | 7.30 |