Assay Detail
Binding
CHEMBL649281
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Binding affinity against alpha-1 adrenergic receptor is the ability to inhibit the specific [3H]prazosin binding (0.4 nM) to rat isolated brain membranes by 50% was reported.
13
Total Activities
13
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 | 13 | 5.32 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL762 | OXYMETAZOLINE | 4.0 | 1 | 6.52 |
| CHEMBL420 | GUANABENZ | 4.0 | 1 | 6.35 |
| CHEMBL101340 | — | — | 1 | 6.33 |
| CHEMBL134 | CLONIDINE | 4.0 | 1 | 5.92 |
| CHEMBL1215 | PHENYLEPHRINE | 4.0 | 1 | 5.70 |
| CHEMBL146100 | — | — | 1 | 5.29 |
| CHEMBL11845 | — | — | 1 | 4.82 |
| CHEMBL285755 | — | — | 1 | 4.75 |
| CHEMBL273273 | 5-OH-DPAT | — | 1 | 4.75 |
| CHEMBL15887 | — | — | 1 | 4.62 |
| CHEMBL146419 | — | — | 1 | 4.41 |
| CHEMBL146408 | AMIDEPHRINE MESYLATE | 2.0 | 1 | 4.40 |
| CHEMBL524 | METHOXAMINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL762 | OXYMETAZOLINE | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL420 | GUANABENZ | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL101340 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL134 | CLONIDINE | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL1215 | PHENYLEPHRINE | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL146100 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL11845 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL285755 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL273273 | 5-OH-DPAT | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL15887 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL146419 | — | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL146408 | AMIDEPHRINE MESYLATE | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL524 | METHOXAMINE | IC50 | = | 170000.0 | nM | - |