Assay Detail
Binding
CHEMBL647022
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Binding affinity for Alpha-1 adrenergic receptor in rat cortex membranes using [3H]-prazosin as radioligand
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 | 18 | 9.40 | 10.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL47792 | — | — | 1 | 10.28 |
| CHEMBL118770 | — | — | 1 | 10.10 |
| CHEMBL118704 | — | — | 1 | 9.64 |
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 9.62 |
| CHEMBL300093 | — | — | 1 | 9.59 |
| CHEMBL117996 | — | — | 1 | 9.51 |
| CHEMBL118910 | — | — | 1 | 9.49 |
| CHEMBL118661 | — | — | 1 | 9.43 |
| CHEMBL331049 | — | — | 1 | 9.38 |
| CHEMBL264731 | — | — | 1 | 9.37 |
| CHEMBL300094 | — | — | 1 | 9.37 |
| CHEMBL45726 | — | — | 1 | 9.30 |
| CHEMBL119680 | — | — | 1 | 9.27 |
| CHEMBL48163 | — | — | 1 | 9.26 |
| CHEMBL300092 | — | — | 1 | 9.24 |
| CHEMBL49152 | — | — | 1 | 8.84 |
| CHEMBL116323 | — | — | 1 | 8.78 |
| CHEMBL46172 | — | — | 1 | 8.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL47792 | — | Ki | = | 0.052 | nM | 10.28 |
| CHEMBL118770 | — | Ki | = | 0.08 | nM | 10.10 |
| CHEMBL118704 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL2 | PRAZOSIN | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL300093 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL117996 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL118910 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL118661 | — | Ki | = | 0.37 | nM | 9.43 |
| CHEMBL331049 | — | Ki | = | 0.42 | nM | 9.38 |
| CHEMBL264731 | — | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL300094 | — | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL45726 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL119680 | — | Ki | = | 0.54 | nM | 9.27 |
| CHEMBL48163 | — | Ki | = | 0.55 | nM | 9.26 |
| CHEMBL300092 | — | Ki | = | 0.58 | nM | 9.24 |
| CHEMBL49152 | — | Ki | = | 1.45 | nM | 8.84 |
| CHEMBL116323 | — | Ki | = | 1.68 | nM | 8.78 |
| CHEMBL46172 | — | Ki | = | 1.9 | nM | 8.72 |