Assay Detail
Binding
CHEMBL649639
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro binding affinity was measured as the inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor of rat cortical membranes
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| 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 | 30 | 7.18 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL134 | CLONIDINE | 4.0 | 1 | 8.82 |
| CHEMBL29001 | — | — | 1 | 8.30 |
| CHEMBL287106 | — | — | 1 | 8.22 |
| CHEMBL31950 | — | — | 1 | 8.15 |
| CHEMBL407641 | MEZILAMINE | 2.0 | 1 | 8.05 |
| CHEMBL29275 | — | — | 1 | 7.80 |
| CHEMBL31957 | — | — | 1 | 7.80 |
| CHEMBL284188 | — | — | 1 | 7.66 |
| CHEMBL441773 | — | — | 1 | 7.58 |
| CHEMBL28249 | — | — | 1 | 7.44 |
| CHEMBL31576 | — | — | 1 | 7.36 |
| CHEMBL15245 | YOHIMBINE | 3.0 | 1 | 7.35 |
| CHEMBL283076 | — | — | 1 | 7.30 |
| CHEMBL31403 | — | — | 1 | 7.30 |
| CHEMBL416196 | — | — | 1 | 7.30 |
| CHEMBL31488 | — | — | 1 | 7.30 |
| CHEMBL28184 | — | — | 1 | 7.05 |
| CHEMBL31548 | — | — | 1 | 6.92 |
| CHEMBL28448 | — | — | 1 | 6.89 |
| CHEMBL31996 | — | — | 1 | 6.85 |
| CHEMBL285326 | — | — | 1 | 6.82 |
| CHEMBL284807 | — | — | 1 | 6.82 |
| CHEMBL284682 | — | — | 1 | 6.75 |
| CHEMBL414191 | — | — | 1 | 6.62 |
| CHEMBL29159 | — | — | 1 | 6.54 |
| CHEMBL27962 | — | — | 1 | 6.44 |
| CHEMBL28482 | — | — | 1 | 6.21 |
| CHEMBL32058 | — | — | 1 | 6.04 |
| CHEMBL28573 | — | — | 1 | 5.82 |
| CHEMBL31966 | — | — | 1 | 5.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL134 | CLONIDINE | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL29001 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL287106 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL31950 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL407641 | MEZILAMINE | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL29275 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL31957 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL284188 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL441773 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL28249 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL31576 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL15245 | YOHIMBINE | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL283076 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL31403 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL416196 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL31488 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL28184 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL31548 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL28448 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL31996 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL285326 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL284807 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL284682 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL414191 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL29159 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL27962 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL28482 | — | Ki | = | 620.0 | nM | 6.21 |
| CHEMBL32058 | — | Ki | = | 910.0 | nM | 6.04 |
| CHEMBL28573 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL31966 | — | Ki | = | 1600.0 | nM | 5.80 |