Assay Detail
Binding
CHEMBL643883
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in vitro alpha-2A adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligand
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
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 | 8 | 7.06 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL778 | DEXMEDETOMIDINE | 4.0 | 1 | 8.30 |
| CHEMBL284795 | — | — | 1 | 7.60 |
| CHEMBL284213 | — | — | 1 | 7.57 |
| CHEMBL30739 | — | — | 1 | 7.17 |
| CHEMBL30955 | — | — | 1 | 6.65 |
| CHEMBL286246 | — | — | 1 | 6.59 |
| CHEMBL30534 | — | — | 1 | 6.56 |
| CHEMBL134 | CLONIDINE | 4.0 | 1 | 6.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL778 | DEXMEDETOMIDINE | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL284795 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL284213 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL30739 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL30955 | — | Ki | = | 224.0 | nM | 6.65 |
| CHEMBL286246 | — | Ki | = | 254.0 | nM | 6.59 |
| CHEMBL30534 | — | Ki | = | 277.0 | nM | 6.56 |
| CHEMBL134 | CLONIDINE | Ki | = | 853.0 | nM | 6.07 |