Assay Detail
Binding
CHEMBL5504541
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Binding affinity to human alpha1A-adrenoceptor
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Designing Chromane Derivatives as α<sub>2A</sub>-Adrenoceptor Selective Agonists via Conformation Constraint.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 6.03 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5517941 | — | — | 1 | 8.40 |
| CHEMBL5542211 | — | — | 1 | 6.35 |
| CHEMBL134 | CLONIDINE | 4.0 | 1 | 6.06 |
| CHEMBL778 | DEXMEDETOMIDINE | 4.0 | 1 | 5.88 |
| CHEMBL5542553 | — | — | 1 | 5.88 |
| CHEMBL4594267 | TASIPIMIDINE | 2.0 | 1 | 5.51 |
| CHEMBL862 | GUANFACINE | 4.0 | 1 | 5.33 |
| CHEMBL1437 | NOREPINEPHRINE | 4.0 | 1 | 4.81 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5517941 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL5542211 | — | Ki | = | 446.68 | nM | 6.35 |
| CHEMBL134 | CLONIDINE | Ki | = | 870.96 | nM | 6.06 |
| CHEMBL778 | DEXMEDETOMIDINE | Ki | = | 1318.26 | nM | 5.88 |
| CHEMBL5542553 | — | Ki | = | 1318.26 | nM | 5.88 |
| CHEMBL4594267 | TASIPIMIDINE | Ki | = | 3090.3 | nM | 5.51 |
| CHEMBL862 | GUANFACINE | Ki | = | 4677.35 | nM | 5.33 |
| CHEMBL1437 | NOREPINEPHRINE | Ki | = | 15488.17 | nM | 4.81 |