Assay Detail
Binding
CHEMBL652747
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Alpha-1 adrenergic receptor binding affinity in rat brain membranes
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Brain membranes |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Medetomidine analogs as alpha 2-adrenergic ligands. 2. Design, synthesis, and biological activity of conformationally restricted naphthalene derivatives of medetomidine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 6.30 | 7.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL105328 | — | — | 1 | 7.26 |
| CHEMBL322844 | — | — | 1 | 7.24 |
| CHEMBL306751 | — | — | 1 | 6.65 |
| CHEMBL102669 | — | — | 1 | 6.41 |
| CHEMBL102076 | — | — | 1 | 6.24 |
| CHEMBL420652 | — | — | 1 | 6.18 |
| CHEMBL77921 | MEDETOMIDINE | 3.0 | 1 | 5.96 |
| CHEMBL105487 | — | — | 1 | 5.76 |
| CHEMBL677 | LEVONORDEFRIN | 4.0 | 1 | 5.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL105328 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL322844 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL306751 | — | Ki | = | 224.0 | nM | 6.65 |
| CHEMBL102669 | — | Ki | = | 387.0 | nM | 6.41 |
| CHEMBL102076 | — | Ki | = | 574.0 | nM | 6.24 |
| CHEMBL420652 | — | Ki | = | 655.0 | nM | 6.18 |
| CHEMBL77921 | MEDETOMIDINE | Ki | = | 1109.0 | nM | 5.96 |
| CHEMBL105487 | — | Ki | = | 1734.0 | nM | 5.76 |
| CHEMBL677 | LEVONORDEFRIN | Ki | = | 9221.0 | nM | 5.04 |