Assay Detail
Functional
CHEMBL2155390
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at alpha1D adrenoceptor in Sprague-Dawley rat thoracic aorta 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 | Thoracic aorta |
| 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 | 8.20 | 9.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL215421 | — | — | 1 | 9.20 |
| CHEMBL2153555 | — | — | 1 | 8.52 |
| CHEMBL2153559 | — | — | 1 | 8.24 |
| CHEMBL2153557 | — | — | 1 | 8.03 |
| CHEMBL2153553 | — | — | 1 | 7.93 |
| CHEMBL2153551 | — | — | 1 | 7.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL215421 | — | Kd | = | 0.631 | nM | 9.20 |
| CHEMBL2153555 | — | Kd | = | 3.02 | nM | 8.52 |
| CHEMBL2153559 | — | Kd | = | 5.754 | nM | 8.24 |
| CHEMBL2153557 | — | Kd | = | 9.333 | nM | 8.03 |
| CHEMBL2153553 | — | Kd | = | 11.75 | nM | 7.93 |
| CHEMBL2153551 | — | Kd | = | 51.29 | nM | 7.29 |