Assay Detail
Functional
CHEMBL2156103
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Antagonist activity at adrenergic alpha 1D receptor in rat thoracic aorta assessed as inhibition of noradrenaline-induced contraction after 1 hr
7
Total Activities
3
Compounds Tested
3
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
Discovery of LASSBio-772, a 1,3-benzodioxole N-phenylpiperazine derivative with potent alpha 1A/D-adrenergic receptor blocking properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 3 | 9.63 | 10.60 |
| Kb | 3 | - | - |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2153423 | — | — | 3 | 10.60 |
| CHEMBL2 | PRAZOSIN | 4.0 | 2 | 9.77 |
| CHEMBL13647 | BMY-7378 | — | 2 | 8.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2153423 | — | Kd | = | 0.02512 | nM | 10.60 |
| CHEMBL2 | PRAZOSIN | Kd | = | 0.1698 | nM | 9.77 |
| CHEMBL13647 | BMY-7378 | Kd | = | 3.02 | nM | 8.52 |
| CHEMBL2 | PRAZOSIN | Kb | = | 0.17 | nM | - |
| CHEMBL13647 | BMY-7378 | Kb | = | 3.02 | nM | - |
| CHEMBL2153423 | — | Kb | = | 0.025 | nM | - |
| CHEMBL2153423 | — | Inhibition | - | % | - |