Assay Detail
Binding
CHEMBL649223
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Displacement of [3H]rauwolscine from Alpha-2 adrenergic receptor of rat brain membranes
14
Total Activities
14
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
Medetomidine analogs as alpha 2-adrenergic ligands. 3. Synthesis and biological evaluation of a new series of medetomidine analogs and their potential binding interactions with alpha 2-adrenoceptors involving a "methyl pocket".
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 6.78 | 8.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL102763 | — | — | 1 | 8.06 |
| CHEMBL77921 | MEDETOMIDINE | 3.0 | 1 | 7.60 |
| CHEMBL322907 | — | — | 1 | 7.51 |
| CHEMBL317912 | — | — | 1 | 7.20 |
| CHEMBL105347 | — | — | 1 | 7.02 |
| CHEMBL330185 | — | — | 1 | 7.01 |
| CHEMBL319221 | — | — | 1 | 6.99 |
| CHEMBL319984 | — | — | 1 | 6.77 |
| CHEMBL103448 | — | — | 1 | 6.70 |
| CHEMBL422247 | — | — | 1 | 6.63 |
| CHEMBL103500 | — | — | 1 | 6.24 |
| CHEMBL321964 | — | — | 1 | 5.85 |
| CHEMBL102538 | — | — | 1 | 5.80 |
| CHEMBL103438 | — | — | 1 | 5.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL102763 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL77921 | MEDETOMIDINE | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL322907 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL317912 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL105347 | — | Ki | = | 95.0 | nM | 7.02 |
| CHEMBL330185 | — | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL319221 | — | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL319984 | — | Ki | = | 169.0 | nM | 6.77 |
| CHEMBL103448 | — | Ki | = | 201.0 | nM | 6.70 |
| CHEMBL422247 | — | Ki | = | 232.0 | nM | 6.63 |
| CHEMBL103500 | — | Ki | = | 580.0 | nM | 6.24 |
| CHEMBL321964 | — | Ki | = | 1420.0 | nM | 5.85 |
| CHEMBL102538 | — | Ki | = | 1570.0 | nM | 5.80 |
| CHEMBL103438 | — | Ki | = | 2670.0 | nM | 5.57 |