Assay Detail
Binding
CHEMBL859778
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Inhibitory activity against Adrenergic alpha-1 receptor
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Synthesis and SAR of highly potent dual 5-HT1A and 5-HT1B antagonists as potential antidepressant drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 31 | 8.48 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL196961 | — | — | 1 | 10.00 |
| CHEMBL196958 | — | — | 1 | 10.00 |
| CHEMBL198462 | — | — | 1 | 10.00 |
| CHEMBL371094 | — | — | 1 | 9.70 |
| CHEMBL197338 | — | — | 1 | 9.70 |
| CHEMBL200315 | — | — | 1 | 9.70 |
| CHEMBL199049 | — | — | 1 | 9.40 |
| CHEMBL197344 | — | — | 1 | 9.30 |
| CHEMBL198792 | — | — | 1 | 9.30 |
| CHEMBL196962 | — | — | 1 | 9.30 |
| CHEMBL198696 | — | — | 1 | 9.00 |
| CHEMBL197007 | — | — | 1 | 8.96 |
| CHEMBL438619 | — | — | 1 | 8.92 |
| CHEMBL199443 | — | — | 1 | 8.92 |
| CHEMBL197078 | — | — | 1 | 8.77 |
| CHEMBL196862 | — | — | 1 | 8.74 |
| CHEMBL198999 | — | — | 1 | 8.40 |
| CHEMBL200950 | — | — | 1 | 8.35 |
| CHEMBL196914 | — | — | 1 | 8.15 |
| CHEMBL197011 | — | — | 1 | 8.08 |
| CHEMBL197064 | — | — | 1 | 7.92 |
| CHEMBL198836 | — | — | 1 | 7.88 |
| CHEMBL370110 | — | — | 1 | 7.86 |
| CHEMBL197445 | — | — | 1 | 7.83 |
| CHEMBL200949 | — | — | 1 | 7.75 |
| CHEMBL197240 | — | — | 1 | 7.57 |
| CHEMBL371221 | — | — | 1 | 7.39 |
| CHEMBL198463 | — | — | 1 | 6.93 |
| CHEMBL200951 | — | — | 1 | 6.92 |
| CHEMBL199269 | — | — | 1 | 6.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL196961 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL196958 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL198462 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL371094 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL197338 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL200315 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL199049 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL197344 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL198792 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL196962 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL198696 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL197007 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL438619 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL199443 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL197078 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL196862 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL198999 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL200950 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL196914 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL197011 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL197064 | — | Ki | = | 12.1 | nM | 7.92 |
| CHEMBL198836 | — | Ki | = | 13.2 | nM | 7.88 |
| CHEMBL370110 | — | Ki | = | 13.7 | nM | 7.86 |
| CHEMBL197445 | — | Ki | = | 14.8 | nM | 7.83 |
| CHEMBL200949 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL197240 | — | Ki | = | 26.7 | nM | 7.57 |
| CHEMBL371221 | — | Ki | = | 41.1 | nM | 7.39 |
| CHEMBL198463 | — | Ki | = | 118.1 | nM | 6.93 |
| CHEMBL200951 | — | Ki | = | 121.1 | nM | 6.92 |
| CHEMBL199269 | — | Ki | = | 129.1 | nM | 6.89 |
| CHEMBL196907 | — | Ki | = | 6780.0 | nM | 5.17 |