Assay Detail
Binding
CHEMBL642097
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Binding affinity determined to alpha-1 adrenergic receptor of rat cerebral cortex using [3H]prazosin as radioligand
28
Total Activities
28
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 | 28 | 5.50 | 6.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL15245 | YOHIMBINE | 3.0 | 1 | 6.40 |
| CHEMBL10316 | IDAZOXAN | 3.0 | 1 | 6.10 |
| CHEMBL2448022 | — | — | 1 | 6.05 |
| CHEMBL2448029 | — | — | 1 | 5.80 |
| CHEMBL2448027 | — | — | 1 | 5.68 |
| CHEMBL1203553 | — | — | 1 | 5.67 |
| CHEMBL1203556 | — | — | 1 | 5.55 |
| CHEMBL1203560 | — | — | 1 | 5.50 |
| CHEMBL2448025 | — | — | 1 | 5.50 |
| CHEMBL1203563 | — | — | 1 | 5.43 |
| CHEMBL1203561 | — | — | 1 | 5.26 |
| CHEMBL2448026 | — | — | 1 | 5.20 |
| CHEMBL1203566 | — | — | 1 | 5.19 |
| CHEMBL1203554 | — | — | 1 | 5.14 |
| CHEMBL1203571 | — | — | 1 | 4.80 |
| CHEMBL1203559 | — | — | 1 | 4.72 |
| CHEMBL1203569 | — | — | 1 | - |
| CHEMBL1203552 | — | — | 1 | - |
| CHEMBL1203570 | — | — | 1 | - |
| CHEMBL1203558 | — | — | 1 | - |
| CHEMBL1203562 | — | — | 1 | - |
| CHEMBL1203557 | — | — | 1 | - |
| CHEMBL2448023 | — | — | 1 | - |
| CHEMBL2448028 | — | — | 1 | - |
| CHEMBL1203555 | — | — | 1 | - |
| CHEMBL2448024 | — | — | 1 | - |
| CHEMBL1203565 | — | — | 1 | - |
| CHEMBL1203564 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL15245 | YOHIMBINE | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL10316 | IDAZOXAN | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL2448022 | — | Ki | = | 891.25 | nM | 6.05 |
| CHEMBL2448029 | — | Ki | = | 1584.89 | nM | 5.80 |
| CHEMBL2448027 | — | Ki | = | 2089.3 | nM | 5.68 |
| CHEMBL1203553 | — | Ki | = | 2137.96 | nM | 5.67 |
| CHEMBL1203556 | — | Ki | = | 2818.38 | nM | 5.55 |
| CHEMBL1203560 | — | Ki | = | 3162.28 | nM | 5.50 |
| CHEMBL2448025 | — | Ki | = | 3162.28 | nM | 5.50 |
| CHEMBL1203563 | — | Ki | = | 3715.35 | nM | 5.43 |
| CHEMBL1203561 | — | Ki | = | 5495.41 | nM | 5.26 |
| CHEMBL2448026 | — | Ki | = | 6309.57 | nM | 5.20 |
| CHEMBL1203566 | — | Ki | = | 6456.54 | nM | 5.19 |
| CHEMBL1203554 | — | Ki | = | 7244.36 | nM | 5.14 |
| CHEMBL1203571 | — | Ki | = | 15848.93 | nM | 4.80 |
| CHEMBL1203559 | — | Ki | = | 19054.61 | nM | 4.72 |
| CHEMBL1203569 | — | Ki | < | 10000.0 | nM | - |
| CHEMBL1203552 | — | Ki | < | 10000.0 | nM | - |
| CHEMBL1203570 | — | Ki | < | 10000.0 | nM | - |
| CHEMBL1203558 | — | Ki | < | 10000.0 | nM | - |
| CHEMBL1203562 | — | Ki | < | 10000.0 | nM | - |
| CHEMBL1203557 | — | Ki | < | 10000.0 | nM | - |
| CHEMBL2448023 | — | Ki | < | 10000.0 | nM | - |
| CHEMBL2448028 | — | Ki | < | 10000.0 | nM | - |
| CHEMBL1203555 | — | Ki | < | 10000.0 | nM | - |
| CHEMBL2448024 | — | Ki | < | 10000.0 | nM | - |
| CHEMBL1203565 | — | Ki | < | 10000.0 | nM | - |
| CHEMBL1203564 | — | Ki | < | 10000.0 | nM | - |