Assay Detail
Binding
CHEMBL643956
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Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine 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 | 7.42 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL10316 | IDAZOXAN | 3.0 | 1 | 8.82 |
| CHEMBL47415 | — | — | 1 | 8.57 |
| CHEMBL50017 | — | — | 1 | 8.54 |
| CHEMBL280514 | — | — | 1 | 8.30 |
| CHEMBL298004 | — | — | 1 | 8.10 |
| CHEMBL48833 | — | — | 1 | 8.09 |
| CHEMBL295921 | — | — | 1 | 7.96 |
| CHEMBL48137 | — | — | 1 | 7.85 |
| CHEMBL6437 | MIANSERIN | 4.0 | 1 | 7.77 |
| CHEMBL45773 | — | — | 1 | 7.75 |
| CHEMBL10347 | RAUWOLSCINE | — | 1 | 7.75 |
| CHEMBL9841 | — | — | 1 | 7.60 |
| CHEMBL296653 | — | — | 1 | 7.58 |
| CHEMBL18094 | — | — | 1 | 7.43 |
| CHEMBL295764 | — | — | 1 | 7.38 |
| CHEMBL15245 | YOHIMBINE | 3.0 | 1 | 7.31 |
| CHEMBL299007 | — | — | 1 | 7.13 |
| CHEMBL45663 | — | — | 1 | 7.01 |
| CHEMBL47471 | — | — | 1 | 6.92 |
| CHEMBL47740 | — | — | 1 | 6.41 |
| CHEMBL45665 | — | — | 1 | 6.36 |
| CHEMBL50016 | — | — | 1 | 6.30 |
| CHEMBL296787 | — | — | 1 | 5.87 |
| CHEMBL47688 | — | — | 1 | 5.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL10316 | IDAZOXAN | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL47415 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL50017 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL280514 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL298004 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL48833 | — | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL295921 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL48137 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL6437 | MIANSERIN | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL45773 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL10347 | RAUWOLSCINE | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL9841 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL296653 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL18094 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL295764 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL15245 | YOHIMBINE | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL299007 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL45663 | — | Ki | = | 97.0 | nM | 7.01 |
| CHEMBL47471 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL47740 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL45665 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL50016 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL296787 | — | Ki | = | 1340.0 | nM | 5.87 |
| CHEMBL47688 | — | Ki | = | 5200.0 | nM | 5.28 |