Assay Detail
Binding
CHEMBL646333
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Displacement of [3H]clonidine from Alpha-2 adrenergic receptor of rat brain membranes
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
alpha 2 adrenoceptors: classification, localization, mechanisms, and targets for drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 7.26 | 8.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL32573 | TRAMAZOLINE | 2.0 | 1 | 8.38 |
| CHEMBL761 | NAPHAZOLINE | 4.0 | 1 | 8.24 |
| CHEMBL134 | CLONIDINE | 4.0 | 1 | 8.24 |
| CHEMBL677 | LEVONORDEFRIN | 4.0 | 1 | 8.11 |
| CHEMBL1437 | NOREPINEPHRINE | 4.0 | 1 | 7.77 |
| CHEMBL597 | PHENTOLAMINE | 4.0 | 1 | 7.66 |
| CHEMBL31836 | PIPEROXAN | 2.0 | 1 | 7.02 |
| CHEMBL10347 | RAUWOLSCINE | — | 1 | 6.83 |
| CHEMBL15245 | YOHIMBINE | 3.0 | 1 | 6.82 |
| CHEMBL770 | TOLAZOLINE | 4.0 | 1 | 6.75 |
| CHEMBL25554 | — | — | 1 | 6.70 |
| CHEMBL1215 | PHENYLEPHRINE | 4.0 | 1 | 6.57 |
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 5.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL32573 | TRAMAZOLINE | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL761 | NAPHAZOLINE | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL134 | CLONIDINE | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL677 | LEVONORDEFRIN | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL1437 | NOREPINEPHRINE | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL597 | PHENTOLAMINE | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL31836 | PIPEROXAN | Ki | = | 95.0 | nM | 7.02 |
| CHEMBL10347 | RAUWOLSCINE | Ki | = | 149.0 | nM | 6.83 |
| CHEMBL15245 | YOHIMBINE | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL770 | TOLAZOLINE | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL25554 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL1215 | PHENYLEPHRINE | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL2 | PRAZOSIN | Ki | = | 4500.0 | nM | 5.35 |