Assay Detail
Binding
CHEMBL649640
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]idazoxan binding to alpha-2 adrenergic receptor of rat cortical membranes
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
4-Amino-6-chloro-2-piperazinopyrimidines with selective affinity for alpha 2-adrenoceptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 7.26 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL407641 | MEZILAMINE | 2.0 | 1 | 7.92 |
| CHEMBL287106 | — | — | 1 | 7.89 |
| CHEMBL29275 | — | — | 1 | 7.55 |
| CHEMBL283076 | — | — | 1 | 7.54 |
| CHEMBL15245 | YOHIMBINE | 3.0 | 1 | 7.32 |
| CHEMBL28249 | — | — | 1 | 7.21 |
| CHEMBL416196 | — | — | 1 | 7.00 |
| CHEMBL31996 | — | — | 1 | 6.64 |
| CHEMBL414191 | — | — | 1 | 6.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL407641 | MEZILAMINE | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL287106 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL29275 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL283076 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL15245 | YOHIMBINE | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL28249 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL416196 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL31996 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL414191 | — | Ki | = | 500.0 | nM | 6.30 |