Assay Detail
Functional
CHEMBL891160
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Antagonist activity against adrenergic alpha-1A receptor in rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contraction
9
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Vas deferens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis and alpha(1)-adrenoceptor antagonist activity of derivatives and isosters of the furan portion of (+)-cyclazosin.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| pKb | 5 | - | - |
| Kd | 4 | 7.15 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL423294 | CYCLAZOSIN | — | 1 | 7.77 |
| CHEMBL242934 | — | — | 1 | 7.51 |
| CHEMBL242508 | — | — | 1 | 6.85 |
| CHEMBL242507 | — | — | 1 | 6.48 |
| CHEMBL242725 | — | — | 1 | - |
| CHEMBL389978 | — | — | 1 | - |
| CHEMBL242724 | — | — | 1 | - |
| CHEMBL242723 | — | — | 1 | - |
| CHEMBL388884 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL423294 | CYCLAZOSIN | Kd | = | 16.98 | nM | 7.77 |
| CHEMBL242934 | — | Kd | = | 30.9 | nM | 7.51 |
| CHEMBL242508 | — | Kd | = | 141.25 | nM | 6.85 |
| CHEMBL242507 | — | Kd | = | 331.13 | nM | 6.48 |
| CHEMBL242725 | — | pKb | = | 7.04 | — | - |
| CHEMBL389978 | — | pKb | = | 7.06 | — | - |
| CHEMBL242724 | — | pKb | = | 7.44 | — | - |
| CHEMBL242723 | — | pKb | = | 7.05 | — | - |
| CHEMBL388884 | — | pKb | = | 7.53 | — | - |