Assay Detail
Binding
CHEMBL645694
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Binding affinity against alpha-1 adrenergic receptor in rat using [3H]prazosin 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 | 5.19 | 6.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL288787 | — | — | 1 | 6.41 |
| CHEMBL134 | CLONIDINE | 4.0 | 1 | 6.28 |
| CHEMBL281232 | — | — | 1 | 6.19 |
| CHEMBL844 | BRIMONIDINE | 4.0 | 1 | 6.13 |
| CHEMBL31062 | — | — | 1 | 5.70 |
| CHEMBL32683 | — | — | 1 | 5.60 |
| CHEMBL284484 | — | — | 1 | 5.51 |
| CHEMBL31690 | — | — | 1 | 5.48 |
| CHEMBL285455 | — | — | 1 | 5.44 |
| CHEMBL281506 | — | — | 1 | 5.34 |
| CHEMBL31458 | — | — | 1 | 5.30 |
| CHEMBL31824 | — | — | 1 | 5.18 |
| CHEMBL281064 | — | — | 1 | 5.16 |
| CHEMBL31332 | — | — | 1 | 5.13 |
| CHEMBL31258 | — | — | 1 | 5.10 |
| CHEMBL281712 | — | — | 1 | 5.10 |
| CHEMBL281759 | — | — | 1 | 5.10 |
| CHEMBL31195 | — | — | 1 | 5.07 |
| CHEMBL29201 | — | — | 1 | 5.06 |
| CHEMBL30721 | — | — | 1 | 4.96 |
| CHEMBL31627 | — | — | 1 | 4.96 |
| CHEMBL31617 | — | — | 1 | 4.89 |
| CHEMBL281283 | — | — | 1 | 4.89 |
| CHEMBL285885 | — | — | 1 | 4.89 |
| CHEMBL31703 | — | — | 1 | 4.89 |
| CHEMBL31270 | — | — | 1 | 4.85 |
| CHEMBL31844 | — | — | 1 | 4.82 |
| CHEMBL418397 | — | — | 1 | 4.80 |
| CHEMBL31789 | — | — | 1 | 4.80 |
| CHEMBL287587 | — | — | 1 | 4.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL288787 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL134 | CLONIDINE | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL281232 | — | Ki | = | 650.0 | nM | 6.19 |
| CHEMBL844 | BRIMONIDINE | Ki | = | 740.0 | nM | 6.13 |
| CHEMBL31062 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL32683 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL284484 | — | Ki | = | 3100.0 | nM | 5.51 |
| CHEMBL31690 | — | Ki | = | 3300.0 | nM | 5.48 |
| CHEMBL285455 | — | Ki | = | 3600.0 | nM | 5.44 |
| CHEMBL281506 | — | Ki | = | 4600.0 | nM | 5.34 |
| CHEMBL31458 | — | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL31824 | — | Ki | = | 6600.0 | nM | 5.18 |
| CHEMBL281064 | — | Ki | = | 6900.0 | nM | 5.16 |
| CHEMBL31332 | — | Ki | = | 7400.0 | nM | 5.13 |
| CHEMBL281712 | — | Ki | = | 7900.0 | nM | 5.10 |
| CHEMBL281759 | — | Ki | = | 7900.0 | nM | 5.10 |
| CHEMBL31258 | — | Ki | = | 7900.0 | nM | 5.10 |
| CHEMBL31195 | — | Ki | = | 8600.0 | nM | 5.07 |
| CHEMBL29201 | — | Ki | = | 8700.0 | nM | 5.06 |
| CHEMBL30721 | — | Ki | = | 11000.0 | nM | 4.96 |
| CHEMBL31627 | — | Ki | = | 11000.0 | nM | 4.96 |
| CHEMBL31703 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL285885 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL281283 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL31617 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL31270 | — | Ki | = | 14000.0 | nM | 4.85 |
| CHEMBL31844 | — | Ki | = | 15000.0 | nM | 4.82 |
| CHEMBL418397 | — | Ki | = | 16000.0 | nM | 4.80 |
| CHEMBL31789 | — | Ki | = | 16000.0 | nM | 4.80 |
| CHEMBL287587 | — | Ki | = | 25000.0 | nM | 4.60 |
| CHEMBL442268 | — | Ki | = | 26000.0 | nM | 4.58 |
| CHEMBL280574 | — | Ki | = | 27000.0 | nM | 4.57 |
| CHEMBL31979 | — | Ki | = | 29000.0 | nM | 4.54 |