Assay Detail
Functional
CHEMBL772607
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In vitro antagonist activity against (-)-phenylephrine or (-)-norepinephrine-induced alpha1-adrenoceptor-mediated vasoconstriction of rabbit isolated pulmonary artery.
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Oryctolagus cuniculus |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 3 | 6.80 | 7.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1732 | DIHYDROERGOTAMINE | 4.0 | 1 | 7.55 |
| CHEMBL2110596 | AZAPETINE | -1.0 | 1 | 6.96 |
| CHEMBL10347 | RAUWOLSCINE | — | 1 | 5.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1732 | DIHYDROERGOTAMINE | Kd | = | 28.18 | nM | 7.55 |
| CHEMBL2110596 | AZAPETINE | Kd | = | 109.65 | nM | 6.96 |
| CHEMBL10347 | RAUWOLSCINE | Kd | = | 1288.25 | nM | 5.89 |