Assay Detail
Functional
CHEMBL795987
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Antagonist activity against B-HT 933-induced alpha-2-adrenoceptor-mediated vasoconstriction in pithed normotensive rats
8
Total Activities
8
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 | 8 | 5.76 | 7.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1732 | DIHYDROERGOTAMINE | 4.0 | 1 | 7.25 |
| CHEMBL597 | PHENTOLAMINE | 4.0 | 1 | 6.47 |
| CHEMBL31836 | PIPEROXAN | 2.0 | 1 | 6.23 |
| CHEMBL770 | TOLAZOLINE | 4.0 | 1 | 5.82 |
| CHEMBL6437 | MIANSERIN | 4.0 | 1 | 5.67 |
| CHEMBL31410 | CORYNANTHEINE | — | 1 | 5.03 |
| CHEMBL2110596 | AZAPETINE | -1.0 | 1 | 4.88 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 4.69 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1732 | DIHYDROERGOTAMINE | Kd | = | 56.23 | nM | 7.25 |
| CHEMBL597 | PHENTOLAMINE | Kd | = | 338.84 | nM | 6.47 |
| CHEMBL31836 | PIPEROXAN | Kd | = | 588.84 | nM | 6.23 |
| CHEMBL770 | TOLAZOLINE | Kd | = | 1513.56 | nM | 5.82 |
| CHEMBL6437 | MIANSERIN | Kd | = | 2137.96 | nM | 5.67 |
| CHEMBL31410 | CORYNANTHEINE | Kd | = | 9332.54 | nM | 5.03 |
| CHEMBL2110596 | AZAPETINE | Kd | = | 13182.57 | nM | 4.88 |
| CHEMBL42 | CLOZAPINE | Kd | = | 20417.38 | nM | 4.69 |