Assay Detail
Binding
CHEMBL894698
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Displacement of [3H]RX821002 from adrenergic alpha2 receptor in human brain frontal cortex
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Frontal cortex |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Guanidine and 2-aminoimidazoline aromatic derivatives as alpha(2)-adrenoceptor antagonists, 1: toward new antidepressants with heteroatomic linkers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 6.85 | 9.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL10332 | — | — | 1 | 9.04 |
| CHEMBL75389 | — | — | 1 | 8.80 |
| CHEMBL244987 | — | — | 1 | 7.74 |
| CHEMBL134 | CLONIDINE | 4.0 | 1 | 7.68 |
| CHEMBL10316 | IDAZOXAN | 3.0 | 1 | 7.29 |
| CHEMBL242102 | — | — | 1 | 7.24 |
| CHEMBL244986 | — | — | 1 | 7.00 |
| CHEMBL428395 | — | — | 1 | 6.57 |
| CHEMBL77633 | — | — | 1 | 6.38 |
| CHEMBL535858 | — | — | 1 | 6.33 |
| CHEMBL242759 | — | — | 1 | 6.00 |
| CHEMBL552780 | — | — | 1 | 5.97 |
| CHEMBL73758 | — | — | 1 | 5.80 |
| CHEMBL243288 | — | — | 1 | 5.78 |
| CHEMBL308767 | — | — | 1 | 5.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL10332 | — | Ki | = | 0.912 | nM | 9.04 |
| CHEMBL75389 | — | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL244987 | — | Ki | = | 18.2 | nM | 7.74 |
| CHEMBL134 | CLONIDINE | Ki | = | 20.89 | nM | 7.68 |
| CHEMBL10316 | IDAZOXAN | Ki | = | 51.29 | nM | 7.29 |
| CHEMBL242102 | — | Ki | = | 57.54 | nM | 7.24 |
| CHEMBL244986 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL428395 | — | Ki | = | 269.15 | nM | 6.57 |
| CHEMBL77633 | — | Ki | = | 416.87 | nM | 6.38 |
| CHEMBL535858 | — | Ki | = | 467.74 | nM | 6.33 |
| CHEMBL242759 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL552780 | — | Ki | = | 1071.52 | nM | 5.97 |
| CHEMBL73758 | — | Ki | = | 1584.89 | nM | 5.80 |
| CHEMBL243288 | — | Ki | = | 1659.59 | nM | 5.78 |
| CHEMBL308767 | — | Ki | = | 6309.57 | nM | 5.20 |