Assay Detail
Functional
CHEMBL795985
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Antagonist activity against phenylephrine-induced alpha1- adrenoceptor mediated vasoconstriction in pithed normotensive rats.
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 5 — Multiple protein complex / RNA |
| 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 | 10 | 6.15 | 8.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 8.33 |
| CHEMBL597 | PHENTOLAMINE | 4.0 | 1 | 6.95 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 6.29 |
| CHEMBL31410 | CORYNANTHEINE | — | 1 | 6.25 |
| CHEMBL2110596 | AZAPETINE | -1.0 | 1 | 6.09 |
| CHEMBL15245 | YOHIMBINE | 3.0 | 1 | 5.72 |
| CHEMBL31836 | PIPEROXAN | 2.0 | 1 | 5.71 |
| CHEMBL770 | TOLAZOLINE | 4.0 | 1 | 5.66 |
| CHEMBL6437 | MIANSERIN | 4.0 | 1 | 5.41 |
| CHEMBL10347 | RAUWOLSCINE | — | 1 | 5.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | Kd | = | 4.677 | nM | 8.33 |
| CHEMBL597 | PHENTOLAMINE | Kd | = | 112.2 | nM | 6.95 |
| CHEMBL42 | CLOZAPINE | Kd | = | 512.86 | nM | 6.29 |
| CHEMBL31410 | CORYNANTHEINE | Kd | = | 562.34 | nM | 6.25 |
| CHEMBL2110596 | AZAPETINE | Kd | = | 812.83 | nM | 6.09 |
| CHEMBL15245 | YOHIMBINE | Kd | = | 1905.46 | nM | 5.72 |
| CHEMBL31836 | PIPEROXAN | Kd | = | 1949.84 | nM | 5.71 |
| CHEMBL770 | TOLAZOLINE | Kd | = | 2187.76 | nM | 5.66 |
| CHEMBL6437 | MIANSERIN | Kd | = | 3890.45 | nM | 5.41 |
| CHEMBL10347 | RAUWOLSCINE | Kd | = | 7585.78 | nM | 5.12 |