Assay Detail
Binding
CHEMBL643679
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Binding affinity towards alpha-2 adrenergic receptor in rat using [3H]rauwolscine as radioligand
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Conformationally defined adrenergic agents. 1. Design and synthesis of novel alpha 2 selective adrenergic agents: electrostatic repulsion based conformational prototypes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 33 | 6.56 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL31062 | — | — | 1 | 8.15 |
| CHEMBL31195 | — | — | 1 | 7.82 |
| CHEMBL31690 | — | — | 1 | 7.68 |
| CHEMBL281064 | — | — | 1 | 7.60 |
| CHEMBL134 | CLONIDINE | 4.0 | 1 | 7.52 |
| CHEMBL844 | BRIMONIDINE | 4.0 | 1 | 7.52 |
| CHEMBL281232 | — | — | 1 | 7.46 |
| CHEMBL288787 | — | — | 1 | 7.43 |
| CHEMBL31258 | — | — | 1 | 7.36 |
| CHEMBL281283 | — | — | 1 | 7.33 |
| CHEMBL32683 | — | — | 1 | 6.89 |
| CHEMBL31789 | — | — | 1 | 6.77 |
| CHEMBL281712 | — | — | 1 | 6.75 |
| CHEMBL281759 | — | — | 1 | 6.70 |
| CHEMBL31458 | — | — | 1 | 6.70 |
| CHEMBL284484 | — | — | 1 | 6.60 |
| CHEMBL285455 | — | — | 1 | 6.50 |
| CHEMBL31332 | — | — | 1 | 6.33 |
| CHEMBL442268 | — | — | 1 | 6.28 |
| CHEMBL418397 | — | — | 1 | 6.22 |
| CHEMBL31617 | — | — | 1 | 6.18 |
| CHEMBL281506 | — | — | 1 | 6.18 |
| CHEMBL285885 | — | — | 1 | 6.16 |
| CHEMBL31979 | — | — | 1 | 6.16 |
| CHEMBL31703 | — | — | 1 | 6.07 |
| CHEMBL280574 | — | — | 1 | 6.06 |
| CHEMBL29201 | — | — | 1 | 5.89 |
| CHEMBL287587 | — | — | 1 | 5.85 |
| CHEMBL31270 | — | — | 1 | 5.60 |
| CHEMBL31627 | — | — | 1 | 5.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL31062 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL31195 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL31690 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL281064 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL134 | CLONIDINE | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL844 | BRIMONIDINE | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL281232 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL288787 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL31258 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL281283 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL32683 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL31789 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL281712 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL281759 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL31458 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL284484 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL285455 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL31332 | — | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL442268 | — | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL418397 | — | Ki | = | 600.0 | nM | 6.22 |
| CHEMBL31617 | — | Ki | = | 660.0 | nM | 6.18 |
| CHEMBL281506 | — | Ki | = | 660.0 | nM | 6.18 |
| CHEMBL285885 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL31979 | — | Ki | = | 690.0 | nM | 6.16 |
| CHEMBL31703 | — | Ki | = | 860.0 | nM | 6.07 |
| CHEMBL280574 | — | Ki | = | 880.0 | nM | 6.06 |
| CHEMBL29201 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL287587 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL31270 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL31627 | — | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL31824 | — | Ki | = | 4700.0 | nM | 5.33 |
| CHEMBL31844 | — | Ki | = | 5100.0 | nM | 5.29 |
| CHEMBL30721 | — | Ki | = | 19000.0 | nM | 4.72 |