Assay Detail
Binding
CHEMBL646819
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In vitro binding affinity against alpha-2D adrenergic receptor of male Wistar rat
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Alpha(2) adrenoceptor agonists as potential analgesic agents. 3. Imidazolylmethylthiophenes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 36 | 9.10 | 10.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL778 | DEXMEDETOMIDINE | 4.0 | 1 | 10.82 |
| CHEMBL1203855 | — | — | 1 | 10.15 |
| CHEMBL1744288 | — | — | 1 | 10.15 |
| CHEMBL1788145 | — | — | 1 | 10.10 |
| CHEMBL1744273 | — | — | 1 | 10.06 |
| CHEMBL1744270 | — | — | 1 | 10.05 |
| CHEMBL1744272 | — | — | 1 | 10.00 |
| CHEMBL1203846 | — | — | 1 | 9.77 |
| CHEMBL355784 | — | — | 1 | 9.74 |
| CHEMBL1744289 | — | — | 1 | 9.64 |
| CHEMBL1744263 | — | — | 1 | 9.55 |
| CHEMBL1744278 | — | — | 1 | 9.54 |
| CHEMBL1203850 | — | — | 1 | 9.46 |
| CHEMBL1744271 | — | — | 1 | 9.41 |
| CHEMBL1744276 | — | — | 1 | 9.40 |
| CHEMBL1744280 | — | — | 1 | 9.37 |
| CHEMBL1744294 | — | — | 1 | 9.36 |
| CHEMBL1203848 | — | — | 1 | 9.35 |
| CHEMBL1744291 | — | — | 1 | 9.33 |
| CHEMBL1744277 | — | — | 1 | 9.16 |
| CHEMBL1744281 | — | — | 1 | 9.12 |
| CHEMBL170960 | — | — | 1 | 9.11 |
| CHEMBL1237159 | — | — | 1 | 9.02 |
| CHEMBL1744287 | — | — | 1 | 9.01 |
| CHEMBL1203851 | — | — | 1 | 8.96 |
| CHEMBL1237160 | — | — | 1 | 8.68 |
| CHEMBL1744269 | — | — | 1 | 8.64 |
| CHEMBL1744292 | — | — | 1 | 8.51 |
| CHEMBL1203847 | — | — | 1 | 8.44 |
| CHEMBL1203856 | — | — | 1 | 8.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL778 | DEXMEDETOMIDINE | Ki | = | 0.015 | nM | 10.82 |
| CHEMBL1203855 | — | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL1744288 | — | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL1788145 | — | Ki | = | 0.08 | nM | 10.10 |
| CHEMBL1744273 | — | Ki | = | 0.088 | nM | 10.06 |
| CHEMBL1744270 | — | Ki | = | 0.09 | nM | 10.05 |
| CHEMBL1744272 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL1203846 | — | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL355784 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL1744289 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL1744263 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL1744278 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL1203850 | — | Ki | = | 0.35 | nM | 9.46 |
| CHEMBL1744271 | — | Ki | = | 0.39 | nM | 9.41 |
| CHEMBL1744276 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL1744280 | — | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL1744294 | — | Ki | = | 0.44 | nM | 9.36 |
| CHEMBL1203848 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL1744291 | — | Ki | = | 0.47 | nM | 9.33 |
| CHEMBL1744277 | — | Ki | = | 0.69 | nM | 9.16 |
| CHEMBL1744281 | — | Ki | = | 0.75 | nM | 9.12 |
| CHEMBL170960 | — | Ki | = | 0.78 | nM | 9.11 |
| CHEMBL1237159 | — | Ki | = | 0.96 | nM | 9.02 |
| CHEMBL1744287 | — | Ki | = | 0.97 | nM | 9.01 |
| CHEMBL1203851 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL1237160 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL1744269 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL1744292 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL1203847 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL1203856 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL1744267 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL1203849 | — | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL1744274 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL1744286 | — | Ki | = | 15.9 | nM | 7.80 |
| CHEMBL1744266 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL1744265 | — | Ki | = | 1000.0 | nM | 6.00 |