Assay Detail
Binding
CHEMBL640335
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement.
21
Total Activities
21
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 | 21 | 8.97 | 9.67 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL351483 | — | — | 1 | 9.67 |
| CHEMBL162682 | — | — | 1 | 9.62 |
| CHEMBL163190 | — | — | 1 | 9.54 |
| CHEMBL162490 | — | — | 1 | 9.53 |
| CHEMBL162232 | — | — | 1 | 9.47 |
| CHEMBL162370 | — | — | 1 | 9.46 |
| CHEMBL165350 | — | — | 1 | 9.45 |
| CHEMBL165796 | — | — | 1 | 9.35 |
| CHEMBL162501 | LUSAPERIDONE | 2.0 | 1 | 9.26 |
| CHEMBL163247 | — | — | 1 | 9.23 |
| CHEMBL351200 | — | — | 1 | 9.22 |
| CHEMBL162826 | — | — | 1 | 9.16 |
| CHEMBL164612 | — | — | 1 | 9.05 |
| CHEMBL162147 | — | — | 1 | 8.93 |
| CHEMBL165181 | — | — | 1 | 8.76 |
| CHEMBL162436 | — | — | 1 | 8.66 |
| CHEMBL162058 | — | — | 1 | 8.45 |
| CHEMBL165677 | — | — | 1 | 8.41 |
| CHEMBL10316 | IDAZOXAN | 3.0 | 1 | 8.08 |
| CHEMBL165776 | — | — | 1 | 7.99 |
| CHEMBL654 | MIRTAZAPINE | 4.0 | 1 | 7.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL351483 | — | IC50 | = | 0.2138 | nM | 9.67 |
| CHEMBL162682 | — | IC50 | = | 0.2399 | nM | 9.62 |
| CHEMBL163190 | — | IC50 | = | 0.2884 | nM | 9.54 |
| CHEMBL162490 | — | IC50 | = | 0.2951 | nM | 9.53 |
| CHEMBL162232 | — | IC50 | = | 0.3388 | nM | 9.47 |
| CHEMBL162370 | — | IC50 | = | 0.3467 | nM | 9.46 |
| CHEMBL165350 | — | IC50 | = | 0.3548 | nM | 9.45 |
| CHEMBL165796 | — | IC50 | = | 0.4467 | nM | 9.35 |
| CHEMBL162501 | LUSAPERIDONE | IC50 | = | 0.5495 | nM | 9.26 |
| CHEMBL163247 | — | IC50 | = | 0.5888 | nM | 9.23 |
| CHEMBL351200 | — | IC50 | = | 0.6026 | nM | 9.22 |
| CHEMBL162826 | — | IC50 | = | 0.6918 | nM | 9.16 |
| CHEMBL164612 | — | IC50 | = | 0.8913 | nM | 9.05 |
| CHEMBL162147 | — | IC50 | = | 1.175 | nM | 8.93 |
| CHEMBL165181 | — | IC50 | = | 1.738 | nM | 8.76 |
| CHEMBL162436 | — | IC50 | = | 2.188 | nM | 8.66 |
| CHEMBL162058 | — | IC50 | = | 3.548 | nM | 8.45 |
| CHEMBL165677 | — | IC50 | = | 3.89 | nM | 8.41 |
| CHEMBL10316 | IDAZOXAN | IC50 | = | 8.318 | nM | 8.08 |
| CHEMBL165776 | — | IC50 | = | 10.23 | nM | 7.99 |
| CHEMBL654 | MIRTAZAPINE | IC50 | = | 85.11 | nM | 7.07 |