Assay Detail
Binding
CHEMBL641153
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Binding affinity was determined against alpha-2 adrenergic receptor of rat cerebral cortex using [3H]idazoxan as radioligand
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Affinity of 2-(tetrahydroisoquinolin-2-ylmethyl)- and 2-(isoindolin-2-ylmethyl)imidazolines for alpha-adrenoceptors. Differential affinity of imidazolines for the [3H]idazoxan-labeled alpha 2-adrenoceptor vs the [3H]yohimbine-labeled site.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 7.28 | 8.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2448029 | — | — | 1 | 8.23 |
| CHEMBL1203563 | — | — | 1 | 8.07 |
| CHEMBL1203566 | — | — | 1 | 7.02 |
| CHEMBL2448028 | — | — | 1 | 6.83 |
| CHEMBL1203565 | — | — | 1 | 6.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2448029 | — | Ki | = | 5.888 | nM | 8.23 |
| CHEMBL1203563 | — | Ki | = | 8.511 | nM | 8.07 |
| CHEMBL1203566 | — | Ki | = | 95.5 | nM | 7.02 |
| CHEMBL2448028 | — | Ki | = | 147.91 | nM | 6.83 |
| CHEMBL1203565 | — | Ki | = | 575.44 | nM | 6.24 |