Assay Detail
Binding
CHEMBL984238
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Displacement of [3H]RX821002 from alpha2 adrenoceptor in human prefrontal cortex neural membrane after 30 mins by liquid scintillation spectrometry
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Prefrontal cortex |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Guanidine and 2-aminoimidazoline aromatic derivatives as alpha2-adrenoceptor ligands: searching for structure-activity relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 7.34 | 9.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL10332 | — | — | 1 | 9.04 |
| CHEMBL134 | CLONIDINE | 4.0 | 1 | 7.68 |
| CHEMBL473567 | — | — | 1 | 7.38 |
| CHEMBL10316 | IDAZOXAN | 3.0 | 1 | 7.29 |
| CHEMBL467525 | — | — | 1 | 7.27 |
| CHEMBL482359 | — | — | 1 | 7.12 |
| CHEMBL509581 | — | — | 1 | 6.95 |
| CHEMBL506313 | — | — | 1 | 6.75 |
| CHEMBL498849 | — | — | 1 | 6.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL10332 | — | Ki | = | 0.912 | nM | 9.04 |
| CHEMBL134 | CLONIDINE | Ki | = | 20.89 | nM | 7.68 |
| CHEMBL473567 | — | Ki | = | 41.69 | nM | 7.38 |
| CHEMBL10316 | IDAZOXAN | Ki | = | 51.29 | nM | 7.29 |
| CHEMBL467525 | — | Ki | = | 53.7 | nM | 7.27 |
| CHEMBL482359 | — | Ki | = | 75.86 | nM | 7.12 |
| CHEMBL509581 | — | Ki | = | 112.2 | nM | 6.95 |
| CHEMBL506313 | — | Ki | = | 177.83 | nM | 6.75 |
| CHEMBL498849 | — | Ki | = | 263.03 | nM | 6.58 |