Assay Detail
Binding
CHEMBL643584
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Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Pyridinylpiperazines, a new class of selective alpha 2-adrenoceptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 5.93 | 7.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6437 | MIANSERIN | 4.0 | 1 | 7.37 |
| CHEMBL50017 | — | — | 1 | 6.80 |
| CHEMBL9841 | — | — | 1 | 6.80 |
| CHEMBL47415 | — | — | 1 | 6.67 |
| CHEMBL15245 | YOHIMBINE | 3.0 | 1 | 6.66 |
| CHEMBL45773 | — | — | 1 | 6.43 |
| CHEMBL280514 | — | — | 1 | 6.31 |
| CHEMBL10316 | IDAZOXAN | 3.0 | 1 | 6.30 |
| CHEMBL47471 | — | — | 1 | 6.16 |
| CHEMBL50016 | — | — | 1 | 6.10 |
| CHEMBL296787 | — | — | 1 | 6.05 |
| CHEMBL10347 | RAUWOLSCINE | — | 1 | 6.03 |
| CHEMBL295921 | — | — | 1 | 5.83 |
| CHEMBL295764 | — | — | 1 | 5.80 |
| CHEMBL298004 | — | — | 1 | 5.75 |
| CHEMBL48137 | — | — | 1 | 5.70 |
| CHEMBL18094 | — | — | 1 | 5.62 |
| CHEMBL48833 | — | — | 1 | 5.60 |
| CHEMBL45663 | — | — | 1 | 5.54 |
| CHEMBL296653 | — | — | 1 | 5.42 |
| CHEMBL299007 | — | — | 1 | 5.37 |
| CHEMBL47740 | — | — | 1 | 5.17 |
| CHEMBL45665 | — | — | 1 | 4.51 |
| CHEMBL47688 | — | — | 1 | 4.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6437 | MIANSERIN | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL50017 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL9841 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL47415 | — | Ki | = | 215.0 | nM | 6.67 |
| CHEMBL15245 | YOHIMBINE | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL45773 | — | Ki | = | 375.0 | nM | 6.43 |
| CHEMBL280514 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL10316 | IDAZOXAN | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL47471 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL50016 | — | Ki | = | 800.0 | nM | 6.10 |
| CHEMBL296787 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL10347 | RAUWOLSCINE | Ki | = | 940.0 | nM | 6.03 |
| CHEMBL295921 | — | Ki | = | 1480.0 | nM | 5.83 |
| CHEMBL295764 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL298004 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL48137 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL18094 | — | Ki | = | 2400.0 | nM | 5.62 |
| CHEMBL48833 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL45663 | — | Ki | = | 2850.0 | nM | 5.54 |
| CHEMBL296653 | — | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL299007 | — | Ki | = | 4300.0 | nM | 5.37 |
| CHEMBL47740 | — | Ki | = | 6800.0 | nM | 5.17 |
| CHEMBL45665 | — | Ki | = | 31000.0 | nM | 4.51 |
| CHEMBL47688 | — | Ki | = | 62000.0 | nM | 4.21 |