Assay Detail
Binding
CHEMBL643739
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Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement.
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
New 2-substituted 1,2,3,4-tetrahydrobenzofuro[3,2-c]pyridine having highly active and potent central alpha 2-antagonistic activity as potential antidepressants.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.22 | 6.95 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL165796 | — | — | 1 | 6.95 |
| CHEMBL162490 | — | — | 1 | 6.94 |
| CHEMBL162436 | — | — | 1 | 6.69 |
| CHEMBL165181 | — | — | 1 | 6.67 |
| CHEMBL162232 | — | — | 1 | 6.62 |
| CHEMBL162826 | — | — | 1 | 6.61 |
| CHEMBL164612 | — | — | 1 | 6.55 |
| CHEMBL162370 | — | — | 1 | 6.54 |
| CHEMBL162501 | LUSAPERIDONE | 2.0 | 1 | 6.46 |
| CHEMBL163190 | — | — | 1 | 6.40 |
| CHEMBL162682 | — | — | 1 | 6.32 |
| CHEMBL351200 | — | — | 1 | 6.16 |
| CHEMBL351483 | — | — | 1 | 6.14 |
| CHEMBL165776 | — | — | 1 | 6.09 |
| CHEMBL165350 | — | — | 1 | 6.05 |
| CHEMBL163247 | — | — | 1 | 5.59 |
| CHEMBL10316 | IDAZOXAN | 3.0 | 1 | 5.54 |
| CHEMBL654 | MIRTAZAPINE | 4.0 | 1 | 5.50 |
| CHEMBL162058 | — | — | 1 | 5.28 |
| CHEMBL162147 | — | — | 1 | 5.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL165796 | — | IC50 | = | 112.2 | nM | 6.95 |
| CHEMBL162490 | — | IC50 | = | 114.82 | nM | 6.94 |
| CHEMBL162436 | — | IC50 | = | 204.17 | nM | 6.69 |
| CHEMBL165181 | — | IC50 | = | 213.8 | nM | 6.67 |
| CHEMBL162232 | — | IC50 | = | 239.88 | nM | 6.62 |
| CHEMBL162826 | — | IC50 | = | 245.47 | nM | 6.61 |
| CHEMBL164612 | — | IC50 | = | 281.84 | nM | 6.55 |
| CHEMBL162370 | — | IC50 | = | 288.4 | nM | 6.54 |
| CHEMBL162501 | LUSAPERIDONE | IC50 | = | 346.74 | nM | 6.46 |
| CHEMBL163190 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL162682 | — | IC50 | = | 478.63 | nM | 6.32 |
| CHEMBL351200 | — | IC50 | = | 691.83 | nM | 6.16 |
| CHEMBL351483 | — | IC50 | = | 724.44 | nM | 6.14 |
| CHEMBL165776 | — | IC50 | = | 812.83 | nM | 6.09 |
| CHEMBL165350 | — | IC50 | = | 891.25 | nM | 6.05 |
| CHEMBL163247 | — | IC50 | = | 2570.4 | nM | 5.59 |
| CHEMBL10316 | IDAZOXAN | IC50 | = | 2884.03 | nM | 5.54 |
| CHEMBL654 | MIRTAZAPINE | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL162058 | — | IC50 | = | 5248.07 | nM | 5.28 |
| CHEMBL162147 | — | IC50 | = | 5888.44 | nM | 5.23 |