Assay Detail
Functional
CHEMBL647209
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Compound was tested for concentration that produced 50% contractile relative response to maximum response to norepinephrine for Alpha-1 adrenergic receptor
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Oryctolagus cuniculus |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Synthesis and evaluation of 2-[(5-methylbenz-1-ox-4-azin-6-yl)imino]imidazoline, a potent, peripherally acting alpha 2 adrenoceptor agonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 6.21 | 6.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL647 | APRACLONIDINE | 4.0 | 1 | 6.75 |
| CHEMBL134 | CLONIDINE | 4.0 | 1 | 6.54 |
| CHEMBL298936 | — | — | 1 | 6.32 |
| CHEMBL49284 | — | — | 1 | 6.10 |
| CHEMBL49137 | — | — | 1 | 5.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL647 | APRACLONIDINE | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL134 | CLONIDINE | EC50 | = | 290.0 | nM | 6.54 |
| CHEMBL298936 | — | EC50 | = | 480.0 | nM | 6.32 |
| CHEMBL49284 | — | EC50 | = | 790.0 | nM | 6.10 |
| CHEMBL49137 | — | EC50 | = | 4700.0 | nM | 5.33 |