Assay Detail
Binding
CHEMBL643604
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Affinity to Alpha-1 adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: the discovery of alpha1a subtype selective 2'-alkylsulfonyl-substituted analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 6.58 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL762 | OXYMETAZOLINE | 4.0 | 1 | 7.80 |
| CHEMBL70751 | — | — | 1 | 7.73 |
| CHEMBL72441 | — | — | 1 | 7.68 |
| CHEMBL306792 | — | — | 1 | 7.68 |
| CHEMBL72768 | — | — | 1 | 7.48 |
| CHEMBL540035 | — | — | 1 | 7.36 |
| CHEMBL540542 | — | — | 1 | 7.36 |
| CHEMBL553276 | — | — | 1 | 7.24 |
| CHEMBL70692 | — | — | 1 | 6.83 |
| CHEMBL70691 | — | — | 1 | 6.76 |
| CHEMBL74114 | — | — | 1 | 6.38 |
| CHEMBL70563 | — | — | 1 | 6.34 |
| CHEMBL70634 | — | — | 1 | 6.27 |
| CHEMBL419448 | — | — | 1 | 6.26 |
| CHEMBL544290 | — | — | 1 | 6.23 |
| CHEMBL72724 | — | — | 1 | 6.23 |
| CHEMBL70740 | — | — | 1 | 6.21 |
| CHEMBL70326 | — | — | 1 | 6.18 |
| CHEMBL71479 | — | — | 1 | 6.11 |
| CHEMBL74467 | — | — | 1 | 6.09 |
| CHEMBL72958 | NS-49 | — | 1 | 5.95 |
| CHEMBL70973 | — | — | 1 | 5.92 |
| CHEMBL542402 | — | — | 1 | 5.89 |
| CHEMBL71001 | — | — | 1 | 5.79 |
| CHEMBL554416 | — | — | 1 | 5.66 |
| CHEMBL74071 | — | — | 1 | 5.57 |
| CHEMBL302698 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL762 | OXYMETAZOLINE | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL70751 | — | Ki | = | 18.62 | nM | 7.73 |
| CHEMBL72441 | — | Ki | = | 20.89 | nM | 7.68 |
| CHEMBL306792 | — | Ki | = | 20.89 | nM | 7.68 |
| CHEMBL72768 | — | Ki | = | 33.11 | nM | 7.48 |
| CHEMBL540035 | — | Ki | = | 43.65 | nM | 7.36 |
| CHEMBL540542 | — | Ki | = | 43.65 | nM | 7.36 |
| CHEMBL553276 | — | Ki | = | 57.54 | nM | 7.24 |
| CHEMBL70692 | — | Ki | = | 147.91 | nM | 6.83 |
| CHEMBL70691 | — | Ki | = | 173.78 | nM | 6.76 |
| CHEMBL74114 | — | Ki | = | 416.87 | nM | 6.38 |
| CHEMBL70563 | — | Ki | = | 457.09 | nM | 6.34 |
| CHEMBL70634 | — | Ki | = | 537.03 | nM | 6.27 |
| CHEMBL419448 | — | Ki | = | 549.54 | nM | 6.26 |
| CHEMBL544290 | — | Ki | = | 588.84 | nM | 6.23 |
| CHEMBL72724 | — | Ki | = | 588.84 | nM | 6.23 |
| CHEMBL70740 | — | Ki | = | 616.6 | nM | 6.21 |
| CHEMBL70326 | — | Ki | = | 660.69 | nM | 6.18 |
| CHEMBL71479 | — | Ki | = | 776.25 | nM | 6.11 |
| CHEMBL74467 | — | Ki | = | 812.83 | nM | 6.09 |
| CHEMBL72958 | NS-49 | Ki | = | 1122.02 | nM | 5.95 |
| CHEMBL70973 | — | Ki | = | 1202.26 | nM | 5.92 |
| CHEMBL542402 | — | Ki | = | 1288.25 | nM | 5.89 |
| CHEMBL71001 | — | Ki | = | 1621.81 | nM | 5.79 |
| CHEMBL554416 | — | Ki | = | 2187.76 | nM | 5.66 |
| CHEMBL74071 | — | Ki | = | 2691.53 | nM | 5.57 |
| CHEMBL302698 | — | Ki | < | 12589.25 | nM | - |