Assay Detail
Functional
CHEMBL891161
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Antagonist activity against adrenergic Alpha-1B receptor in rat spleen assessed as inhibition of phenylephrine-induced response
9
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Spleen |
| 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 | 8 | - | - |
| Kd | 1 | 8.65 | 8.65 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL242507 | — | — | 1 | 8.65 |
| CHEMBL423294 | CYCLAZOSIN | — | 1 | - |
| CHEMBL242934 | — | — | 1 | - |
| CHEMBL242725 | — | — | 1 | - |
| CHEMBL389978 | — | — | 1 | - |
| CHEMBL242724 | — | — | 1 | - |
| CHEMBL242723 | — | — | 1 | - |
| CHEMBL242508 | — | — | 1 | - |
| CHEMBL388884 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL242507 | — | Kd | = | 2.239 | nM | 8.65 |
| CHEMBL423294 | CYCLAZOSIN | pKb | = | 8.86 | — | - |
| CHEMBL242934 | — | pKb | = | 8.83 | — | - |
| CHEMBL242725 | — | pKb | = | 8.64 | — | - |
| CHEMBL389978 | — | pKb | = | 8.05 | — | - |
| CHEMBL242724 | — | pKb | = | 8.78 | — | - |
| CHEMBL242723 | — | pKb | = | 8.13 | — | - |
| CHEMBL242508 | — | pKb | = | 8.5 | — | - |
| CHEMBL388884 | — | pKb | = | 8.5 | — | - |