Assay Detail
Binding
CHEMBL641152
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Binding affinity to alpha-2 adrenergic receptor of rat cerebral cortex assayed using [3H]yohimbine 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 | 6.88 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL10347 | RAUWOLSCINE | — | 1 | 8.15 |
| CHEMBL10316 | IDAZOXAN | 3.0 | 1 | 7.96 |
| CHEMBL15245 | YOHIMBINE | 3.0 | 1 | 7.90 |
| CHEMBL2448022 | — | — | 1 | 7.71 |
| CHEMBL2448027 | — | — | 1 | 7.65 |
| CHEMBL1203571 | — | — | 1 | 7.51 |
| CHEMBL1203556 | — | — | 1 | 7.48 |
| CHEMBL1203560 | — | — | 1 | 7.25 |
| CHEMBL1203554 | — | — | 1 | 7.19 |
| CHEMBL2448025 | — | — | 1 | 7.14 |
| CHEMBL1203559 | — | — | 1 | 7.07 |
| CHEMBL1203555 | — | — | 1 | 6.90 |
| CHEMBL2448026 | — | — | 1 | 6.74 |
| CHEMBL1203561 | — | — | 1 | 6.57 |
| CHEMBL2448023 | — | — | 1 | 6.52 |
| CHEMBL2448024 | — | — | 1 | 6.42 |
| CHEMBL1203553 | — | — | 1 | 6.32 |
| CHEMBL1203569 | — | — | 1 | 6.29 |
| CHEMBL1203557 | — | — | 1 | 6.17 |
| CHEMBL1203564 | — | — | 1 | 6.16 |
| CHEMBL1203558 | — | — | 1 | 6.13 |
| CHEMBL1203562 | — | — | 1 | 6.00 |
| CHEMBL1203552 | — | — | 1 | 5.97 |
| CHEMBL1203570 | — | — | 1 | 5.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL10347 | RAUWOLSCINE | Ki | = | 7.079 | nM | 8.15 |
| CHEMBL10316 | IDAZOXAN | Ki | = | 10.96 | nM | 7.96 |
| CHEMBL15245 | YOHIMBINE | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL2448022 | — | Ki | = | 19.5 | nM | 7.71 |
| CHEMBL2448027 | — | Ki | = | 22.39 | nM | 7.65 |
| CHEMBL1203571 | — | Ki | = | 30.9 | nM | 7.51 |
| CHEMBL1203556 | — | Ki | = | 33.11 | nM | 7.48 |
| CHEMBL1203560 | — | Ki | = | 56.23 | nM | 7.25 |
| CHEMBL1203554 | — | Ki | = | 64.57 | nM | 7.19 |
| CHEMBL2448025 | — | Ki | = | 72.44 | nM | 7.14 |
| CHEMBL1203559 | — | Ki | = | 85.11 | nM | 7.07 |
| CHEMBL1203555 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL2448026 | — | Ki | = | 181.97 | nM | 6.74 |
| CHEMBL1203561 | — | Ki | = | 269.15 | nM | 6.57 |
| CHEMBL2448023 | — | Ki | = | 302.0 | nM | 6.52 |
| CHEMBL2448024 | — | Ki | = | 380.19 | nM | 6.42 |
| CHEMBL1203553 | — | Ki | = | 478.63 | nM | 6.32 |
| CHEMBL1203569 | — | Ki | = | 512.86 | nM | 6.29 |
| CHEMBL1203557 | — | Ki | = | 676.08 | nM | 6.17 |
| CHEMBL1203564 | — | Ki | = | 691.83 | nM | 6.16 |
| CHEMBL1203558 | — | Ki | = | 741.31 | nM | 6.13 |
| CHEMBL1203562 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL1203552 | — | Ki | = | 1071.52 | nM | 5.97 |
| CHEMBL1203570 | — | Ki | = | 1348.96 | nM | 5.87 |