Assay Detail
Binding
CHEMBL649636
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Displacement of [3H]clonidine from Alpha-2 adrenergic receptor of rat cortical 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
3,7-Disubstituted-1,2,3,4-tetrahydroisoquinolines display remarkable potency and selectivity as inhibitors of phenylethanolamine N-methyltransferase versus the alpha2-adrenoceptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 4.85 | 5.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL294562 | — | — | 1 | 5.55 |
| CHEMBL61490 | — | — | 1 | 5.36 |
| CHEMBL60068 | — | — | 1 | 5.18 |
| CHEMBL273939 | — | — | 1 | 4.96 |
| CHEMBL62034 | — | — | 1 | 4.89 |
| CHEMBL61489 | — | — | 1 | 4.77 |
| CHEMBL57966 | — | — | 1 | 4.72 |
| CHEMBL59441 | — | — | 1 | 4.72 |
| CHEMBL59719 | — | — | 1 | 4.51 |
| CHEMBL293700 | — | — | 1 | 4.42 |
| CHEMBL304872 | — | — | 1 | 4.28 |
| CHEMBL41647 | — | — | 1 | - |
| CHEMBL60724 | — | — | 1 | - |
| CHEMBL43021 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL294562 | — | Ki | = | 2800.0 | nM | 5.55 |
| CHEMBL61490 | — | Ki | = | 4400.0 | nM | 5.36 |
| CHEMBL60068 | — | Ki | = | 6600.0 | nM | 5.18 |
| CHEMBL273939 | — | Ki | = | 11000.0 | nM | 4.96 |
| CHEMBL62034 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL61489 | — | Ki | = | 17000.0 | nM | 4.77 |
| CHEMBL57966 | — | Ki | = | 19000.0 | nM | 4.72 |
| CHEMBL59441 | — | Ki | = | 19000.0 | nM | 4.72 |
| CHEMBL59719 | — | Ki | = | 31000.0 | nM | 4.51 |
| CHEMBL293700 | — | Ki | = | 38000.0 | nM | 4.42 |
| CHEMBL304872 | — | Ki | = | 53000.0 | nM | 4.28 |
| CHEMBL41647 | — | Ki | = | 1400000.0 | nM | - |
| CHEMBL60724 | — | Ki | = | 250000.0 | nM | - |
| CHEMBL43021 | — | Ki | = | 660000.0 | nM | - |