Assay Detail
Functional
CHEMBL913009
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Activity at adrenergic alpha 1D receptor assessed as antagonism on noradrenaline-induced contraction of Sprague-Dawley rat thoracic aorta
12
Total Activities
12
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 | Expert |
Publication
WB4101-related compounds: new, subtype-selective alpha1-adrenoreceptor antagonists (or inverse agonists?).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 12 | 7.78 | 10.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL217469 | — | — | 1 | 10.68 |
| CHEMBL215421 | — | — | 1 | 9.20 |
| CHEMBL215151 | — | — | 1 | 8.99 |
| CHEMBL25554 | — | — | 1 | 8.60 |
| CHEMBL383938 | — | — | 1 | 8.39 |
| CHEMBL439346 | — | — | 1 | 8.00 |
| CHEMBL214986 | — | — | 1 | 7.65 |
| CHEMBL214694 | — | — | 1 | 7.21 |
| CHEMBL214762 | — | — | 1 | 6.97 |
| CHEMBL215188 | — | — | 1 | 6.74 |
| CHEMBL385371 | — | — | 1 | 5.59 |
| CHEMBL218079 | — | — | 1 | 5.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL217469 | — | Kd | = | 0.02089 | nM | 10.68 |
| CHEMBL215421 | — | Kd | = | 0.631 | nM | 9.20 |
| CHEMBL215151 | — | Kd | = | 1.023 | nM | 8.99 |
| CHEMBL25554 | — | Kd | = | 2.512 | nM | 8.60 |
| CHEMBL383938 | — | Kd | = | 4.074 | nM | 8.39 |
| CHEMBL439346 | — | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL214986 | — | Kd | = | 22.39 | nM | 7.65 |
| CHEMBL214694 | — | Kd | = | 61.66 | nM | 7.21 |
| CHEMBL214762 | — | Kd | = | 107.15 | nM | 6.97 |
| CHEMBL215188 | — | Kd | = | 181.97 | nM | 6.74 |
| CHEMBL385371 | — | Kd | = | 2570.4 | nM | 5.59 |
| CHEMBL218079 | — | Kd | = | 4365.16 | nM | 5.36 |