Assay Detail
Functional
CHEMBL1638264
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Antagonist activity at Alpha-1D adrenoceptor in Wistar rat thoracic aorta assessed as noradrenaline induced contractions after 30 mins
6
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Thoracic aorta |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and α1-adrenoceptor antagonist activity of tamsulosin analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 4 | 8.30 | 9.30 |
| pKb | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1630938 | — | — | 1 | 9.30 |
| CHEMBL1630940 | — | — | 1 | 9.02 |
| CHEMBL1630942 | — | — | 1 | 7.67 |
| CHEMBL1630941 | — | — | 1 | 7.22 |
| CHEMBL1630939 | — | — | 1 | - |
| CHEMBL836 | TAMSULOSIN | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1630938 | — | Kd | = | 0.5012 | nM | 9.30 |
| CHEMBL1630940 | — | Kd | = | 0.955 | nM | 9.02 |
| CHEMBL1630942 | — | Kd | = | 21.38 | nM | 7.67 |
| CHEMBL1630941 | — | Kd | = | 60.26 | nM | 7.22 |
| CHEMBL1630939 | — | pKb | = | 9.2 | — | - |
| CHEMBL836 | TAMSULOSIN | pKb | = | 10.0 | — | - |