Assay Detail
Functional
CHEMBL835455
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonistic activity for Alpha-1 adrenergic receptor was measured as inhibition of phenylephrine-reduced contractions in isolated Sprague-Dawley rat anacoccygeal muscles
23
Total Activities
23
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
Pharmacophore-based design, synthesis, biological evaluation, and 3D-QSAR studies of aryl-piperazines as alpha(1)-adrenoceptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 23 | 7.22 | 9.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL104204 | — | — | 1 | 9.12 |
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 8.82 |
| CHEMBL191678 | — | — | 1 | 8.56 |
| CHEMBL189787 | — | — | 1 | 8.56 |
| CHEMBL104593 | — | — | 1 | 7.91 |
| CHEMBL26447 | — | — | 1 | 7.87 |
| CHEMBL190187 | — | — | 1 | 7.85 |
| CHEMBL371799 | — | — | 1 | 7.74 |
| CHEMBL189422 | — | — | 1 | 7.72 |
| CHEMBL191209 | — | — | 1 | 7.71 |
| CHEMBL365534 | — | — | 1 | 7.36 |
| CHEMBL366218 | — | — | 1 | 7.31 |
| CHEMBL370486 | — | — | 1 | 7.18 |
| CHEMBL538154 | — | — | 1 | 7.07 |
| CHEMBL192732 | — | — | 1 | 6.92 |
| CHEMBL189682 | — | — | 1 | 6.53 |
| CHEMBL191026 | — | — | 1 | 6.50 |
| CHEMBL366226 | — | — | 1 | 6.47 |
| CHEMBL192242 | — | — | 1 | 5.95 |
| CHEMBL194105 | — | — | 1 | 5.94 |
| CHEMBL366061 | — | — | 1 | 5.79 |
| CHEMBL192465 | — | — | 1 | 5.63 |
| CHEMBL371994 | — | — | 1 | 5.56 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL104204 | — | Kd | = | 0.7586 | nM | 9.12 |
| CHEMBL2 | PRAZOSIN | Kd | = | 1.514 | nM | 8.82 |
| CHEMBL191678 | — | Kd | = | 2.754 | nM | 8.56 |
| CHEMBL189787 | — | Kd | = | 2.754 | nM | 8.56 |
| CHEMBL104593 | — | Kd | = | 12.3 | nM | 7.91 |
| CHEMBL26447 | — | Kd | = | 13.49 | nM | 7.87 |
| CHEMBL190187 | — | Kd | = | 14.13 | nM | 7.85 |
| CHEMBL371799 | — | Kd | = | 18.2 | nM | 7.74 |
| CHEMBL189422 | — | Kd | = | 19.05 | nM | 7.72 |
| CHEMBL191209 | — | Kd | = | 19.5 | nM | 7.71 |
| CHEMBL365534 | — | Kd | = | 43.65 | nM | 7.36 |
| CHEMBL366218 | — | Kd | = | 48.98 | nM | 7.31 |
| CHEMBL370486 | — | Kd | = | 66.07 | nM | 7.18 |
| CHEMBL538154 | — | Kd | = | 85.11 | nM | 7.07 |
| CHEMBL192732 | — | Kd | = | 120.23 | nM | 6.92 |
| CHEMBL189682 | — | Kd | = | 295.12 | nM | 6.53 |
| CHEMBL191026 | — | Kd | = | 316.23 | nM | 6.50 |
| CHEMBL366226 | — | Kd | = | 338.84 | nM | 6.47 |
| CHEMBL192242 | — | Kd | = | 1122.02 | nM | 5.95 |
| CHEMBL194105 | — | Kd | = | 1148.15 | nM | 5.94 |
| CHEMBL366061 | — | Kd | = | 1621.81 | nM | 5.79 |
| CHEMBL192465 | — | Kd | = | 2344.23 | nM | 5.63 |
| CHEMBL371994 | — | Kd | = | 2754.23 | nM | 5.56 |