Assay Detail
Binding
CHEMBL645686
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Tested for Binding affinity towards alpha-1 adrenergic receptor
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
alpha(2) Adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene [corrected] as a high-affinity ligand for the alpha(2D) adrenergic receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 6.97 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL778 | DEXMEDETOMIDINE | 4.0 | 1 | 8.30 |
| CHEMBL30739 | — | — | 1 | 7.32 |
| CHEMBL286269 | — | — | 1 | 7.04 |
| CHEMBL284795 | — | — | 1 | 6.96 |
| CHEMBL284213 | — | — | 1 | 6.96 |
| CHEMBL134 | CLONIDINE | 4.0 | 1 | 6.94 |
| CHEMBL30534 | — | — | 1 | 6.46 |
| CHEMBL30955 | — | — | 1 | 6.40 |
| CHEMBL286246 | — | — | 1 | 6.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL778 | DEXMEDETOMIDINE | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL30739 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL286269 | — | Ki | = | 91.0 | nM | 7.04 |
| CHEMBL284795 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL284213 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL134 | CLONIDINE | Ki | = | 116.0 | nM | 6.94 |
| CHEMBL30534 | — | Ki | = | 343.0 | nM | 6.46 |
| CHEMBL30955 | — | Ki | = | 399.0 | nM | 6.40 |
| CHEMBL286246 | — | Ki | = | 443.0 | nM | 6.35 |