Assay Detail
Binding
CHEMBL645521
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50% inhibition of specific [3H]clonidine binding (0.4 nM) to Alpha-2 adrenergic receptors in rat isolated brain membranes
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.90 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL420 | GUANABENZ | 4.0 | 1 | 8.77 |
| CHEMBL134 | CLONIDINE | 4.0 | 1 | 8.51 |
| CHEMBL762 | OXYMETAZOLINE | 4.0 | 1 | 8.30 |
| CHEMBL146419 | — | — | 1 | 7.77 |
| CHEMBL11845 | — | — | 1 | 7.10 |
| CHEMBL15887 | — | — | 1 | 7.06 |
| CHEMBL1215 | PHENYLEPHRINE | 4.0 | 1 | 6.28 |
| CHEMBL273273 | 5-OH-DPAT | — | 1 | 6.07 |
| CHEMBL285755 | — | — | 1 | 5.92 |
| CHEMBL524 | METHOXAMINE | 4.0 | 1 | 5.44 |
| CHEMBL146408 | AMIDEPHRINE MESYLATE | 2.0 | 1 | 4.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL420 | GUANABENZ | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL134 | CLONIDINE | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL762 | OXYMETAZOLINE | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL146419 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL11845 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL15887 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL1215 | PHENYLEPHRINE | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL273273 | 5-OH-DPAT | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL285755 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL524 | METHOXAMINE | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL146408 | AMIDEPHRINE MESYLATE | IC50 | = | 19000.0 | nM | 4.72 |