Assay Detail
Binding
CHEMBL649427
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Displacement of [3H]-prazosin from Alpha-1 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 | 6.10 | 7.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL102763 | — | — | 1 | 7.14 |
| CHEMBL317912 | — | — | 1 | 6.90 |
| CHEMBL319221 | — | — | 1 | 6.88 |
| CHEMBL105347 | — | — | 1 | 6.72 |
| CHEMBL319984 | — | — | 1 | 6.70 |
| CHEMBL330185 | — | — | 1 | 6.61 |
| CHEMBL322907 | — | — | 1 | 6.00 |
| CHEMBL77921 | MEDETOMIDINE | 3.0 | 1 | 5.96 |
| CHEMBL103500 | — | — | 1 | 5.79 |
| CHEMBL103448 | — | — | 1 | 5.75 |
| CHEMBL321964 | — | — | 1 | 5.53 |
| CHEMBL422247 | — | — | 1 | 5.53 |
| CHEMBL103438 | — | — | 1 | 5.08 |
| CHEMBL102538 | — | — | 1 | 4.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL102763 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL317912 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL319221 | — | Ki | = | 131.0 | nM | 6.88 |
| CHEMBL105347 | — | Ki | = | 191.0 | nM | 6.72 |
| CHEMBL319984 | — | Ki | = | 198.0 | nM | 6.70 |
| CHEMBL330185 | — | Ki | = | 243.0 | nM | 6.61 |
| CHEMBL322907 | — | Ki | = | 992.0 | nM | 6.00 |
| CHEMBL77921 | MEDETOMIDINE | Ki | = | 1110.0 | nM | 5.96 |
| CHEMBL103500 | — | Ki | = | 1630.0 | nM | 5.79 |
| CHEMBL103448 | — | Ki | = | 1770.0 | nM | 5.75 |
| CHEMBL321964 | — | Ki | = | 2970.0 | nM | 5.53 |
| CHEMBL422247 | — | Ki | = | 2960.0 | nM | 5.53 |
| CHEMBL103438 | — | Ki | = | 8250.0 | nM | 5.08 |
| CHEMBL102538 | — | Ki | = | 14200.0 | nM | 4.85 |