Assay Detail
Binding
CHEMBL641151
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Binding affinity to the alpha-2 adrenergic receptor of rat cerebral cortex assayed using [3H]idazoxan as radioligand
24
Total Activities
24
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 | 24 | 7.45 | 8.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1203556 | — | — | 1 | 8.39 |
| CHEMBL2448022 | — | — | 1 | 8.38 |
| CHEMBL1203560 | — | — | 1 | 8.27 |
| CHEMBL10316 | IDAZOXAN | 3.0 | 1 | 8.12 |
| CHEMBL2448025 | — | — | 1 | 8.12 |
| CHEMBL1203559 | — | — | 1 | 8.00 |
| CHEMBL2448027 | — | — | 1 | 7.80 |
| CHEMBL1203571 | — | — | 1 | 7.80 |
| CHEMBL1203553 | — | — | 1 | 7.77 |
| CHEMBL2448023 | — | — | 1 | 7.68 |
| CHEMBL2448024 | — | — | 1 | 7.67 |
| CHEMBL2448026 | — | — | 1 | 7.62 |
| CHEMBL1203561 | — | — | 1 | 7.38 |
| CHEMBL1203555 | — | — | 1 | 7.38 |
| CHEMBL1203554 | — | — | 1 | 7.32 |
| CHEMBL15245 | YOHIMBINE | 3.0 | 1 | 7.25 |
| CHEMBL1203569 | — | — | 1 | 7.20 |
| CHEMBL1203558 | — | — | 1 | 7.14 |
| CHEMBL10347 | RAUWOLSCINE | — | 1 | 7.09 |
| CHEMBL1203557 | — | — | 1 | 6.99 |
| CHEMBL1203562 | — | — | 1 | 6.68 |
| CHEMBL1203552 | — | — | 1 | 6.41 |
| CHEMBL1203564 | — | — | 1 | 6.31 |
| CHEMBL1203570 | — | — | 1 | 6.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1203556 | — | Ki | = | 4.074 | nM | 8.39 |
| CHEMBL2448022 | — | Ki | = | 4.169 | nM | 8.38 |
| CHEMBL1203560 | — | Ki | = | 5.37 | nM | 8.27 |
| CHEMBL10316 | IDAZOXAN | Ki | = | 7.586 | nM | 8.12 |
| CHEMBL2448025 | — | Ki | = | 7.586 | nM | 8.12 |
| CHEMBL1203559 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL2448027 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL1203571 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL1203553 | — | Ki | = | 16.98 | nM | 7.77 |
| CHEMBL2448023 | — | Ki | = | 20.89 | nM | 7.68 |
| CHEMBL2448024 | — | Ki | = | 21.38 | nM | 7.67 |
| CHEMBL2448026 | — | Ki | = | 23.99 | nM | 7.62 |
| CHEMBL1203561 | — | Ki | = | 41.69 | nM | 7.38 |
| CHEMBL1203555 | — | Ki | = | 41.69 | nM | 7.38 |
| CHEMBL1203554 | — | Ki | = | 47.86 | nM | 7.32 |
| CHEMBL15245 | YOHIMBINE | Ki | = | 56.23 | nM | 7.25 |
| CHEMBL1203569 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL1203558 | — | Ki | = | 72.44 | nM | 7.14 |
| CHEMBL10347 | RAUWOLSCINE | Ki | = | 81.28 | nM | 7.09 |
| CHEMBL1203557 | — | Ki | = | 102.33 | nM | 6.99 |
| CHEMBL1203562 | — | Ki | = | 208.93 | nM | 6.68 |
| CHEMBL1203552 | — | Ki | = | 389.05 | nM | 6.41 |
| CHEMBL1203564 | — | Ki | = | 489.78 | nM | 6.31 |
| CHEMBL1203570 | — | Ki | = | 741.31 | nM | 6.13 |