Assay Detail
Binding
CHEMBL646575
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In vitro binding affinity was measured as the inhibition of [3H]WB-4101 binding to alpha-1 adrenergic receptor of rat cortical membranes
31
Total Activities
31
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 | 31 | 6.65 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL753 | PHENOXYBENZAMINE | 4.0 | 1 | 8.74 |
| CHEMBL31576 | — | — | 1 | 8.40 |
| CHEMBL29001 | — | — | 1 | 7.38 |
| CHEMBL31488 | — | — | 1 | 7.17 |
| CHEMBL284188 | — | — | 1 | 7.12 |
| CHEMBL407641 | MEZILAMINE | 2.0 | 1 | 7.04 |
| CHEMBL28573 | — | — | 1 | 7.00 |
| CHEMBL414191 | — | — | 1 | 6.85 |
| CHEMBL32058 | — | — | 1 | 6.75 |
| CHEMBL285326 | — | — | 1 | 6.75 |
| CHEMBL29275 | — | — | 1 | 6.70 |
| CHEMBL31957 | — | — | 1 | 6.70 |
| CHEMBL29159 | — | — | 1 | 6.62 |
| CHEMBL31548 | — | — | 1 | 6.62 |
| CHEMBL31996 | — | — | 1 | 6.60 |
| CHEMBL416196 | — | — | 1 | 6.55 |
| CHEMBL31950 | — | — | 1 | 6.54 |
| CHEMBL31403 | — | — | 1 | 6.51 |
| CHEMBL134 | CLONIDINE | 4.0 | 1 | 6.51 |
| CHEMBL15245 | YOHIMBINE | 3.0 | 1 | 6.44 |
| CHEMBL441773 | — | — | 1 | 6.44 |
| CHEMBL284682 | — | — | 1 | 6.35 |
| CHEMBL28249 | — | — | 1 | 6.30 |
| CHEMBL31966 | — | — | 1 | 6.09 |
| CHEMBL28482 | — | — | 1 | 6.09 |
| CHEMBL287106 | — | — | 1 | 6.07 |
| CHEMBL284807 | — | — | 1 | 5.77 |
| CHEMBL283076 | — | — | 1 | 5.77 |
| CHEMBL28184 | — | — | 1 | 5.75 |
| CHEMBL27962 | — | — | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL753 | PHENOXYBENZAMINE | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL31576 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL29001 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL31488 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL284188 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL407641 | MEZILAMINE | Ki | = | 91.0 | nM | 7.04 |
| CHEMBL28573 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL414191 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL32058 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL285326 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL29275 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL31957 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL29159 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL31548 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL31996 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL416196 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL31950 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL31403 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL134 | CLONIDINE | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL15245 | YOHIMBINE | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL441773 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL284682 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL28249 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL31966 | — | Ki | = | 820.0 | nM | 6.09 |
| CHEMBL28482 | — | Ki | = | 820.0 | nM | 6.09 |
| CHEMBL287106 | — | Ki | = | 860.0 | nM | 6.07 |
| CHEMBL284807 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL283076 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL28184 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL27962 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL28448 | — | Ki | > | 180.0 | nM | - |