Assay Detail
Binding
CHEMBL647841
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In vitro rat alpha-2D adrenergic receptor binding using p-aminoclonidine
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Alpha(2) adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-imidazo)-1,3-dimethyl-6,7-dihydro-thianaphthene as a high-affinity ligand for the alpha(2D) adrenergic receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 9.18 | 10.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL778 | DEXMEDETOMIDINE | 4.0 | 1 | 10.82 |
| CHEMBL286269 | — | — | 1 | 9.46 |
| CHEMBL134 | CLONIDINE | 4.0 | 1 | 9.41 |
| CHEMBL284213 | — | — | 1 | 9.25 |
| CHEMBL286246 | — | — | 1 | 8.82 |
| CHEMBL30534 | — | — | 1 | 8.59 |
| CHEMBL30739 | — | — | 1 | 8.54 |
| CHEMBL30955 | — | — | 1 | 8.52 |
| CHEMBL284795 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL778 | DEXMEDETOMIDINE | Ki | = | 0.015 | nM | 10.82 |
| CHEMBL286269 | — | Ki | = | 0.35 | nM | 9.46 |
| CHEMBL134 | CLONIDINE | Ki | = | 0.39 | nM | 9.41 |
| CHEMBL284213 | — | Ki | = | 0.56 | nM | 9.25 |
| CHEMBL286246 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL30534 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL30739 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL30955 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL284795 | — | Ki | = | 0.0086 | nM | - |