Assay Detail
Binding
CHEMBL645682
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Intrinsic activity towards Alpha-1 adrenergic receptor by the displacement of [3H]prazosin from rat cerebral cortex membrane in presence of 1 nM GTP.
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Alpha1-adrenoceptor antagonists. 6. Structural optimization of pyridazinone-arylpiperazines. Study of the influence on affinity and selectivity of cyclic substituents at the pyridazinone ring and alkoxy groups at the arylpiperazine moiety.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 9.68 | 10.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL47792 | — | — | 1 | 10.09 |
| CHEMBL300093 | — | — | 1 | 9.66 |
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 9.49 |
| CHEMBL117996 | — | — | 1 | 9.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL47792 | — | Ki | = | 0.081 | nM | 10.09 |
| CHEMBL300093 | — | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL2 | PRAZOSIN | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL117996 | — | Ki | = | 0.33 | nM | 9.48 |