Assay Detail
Binding
CHEMBL640540
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Binding affinity against alpha-2 adrenergic receptor in rat cerebral cortical membrane using [3H]yohimbine as radioligand.
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
1,9-Alkano-bridged 2,3,4,5-tetrahydro-1H-3-benzazepines with affinity for the alpha 2-adrenoceptor and the 5-HT1A receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 37 | 6.38 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1202289 | — | — | 1 | 8.10 |
| CHEMBL123349 | — | — | 1 | 8.10 |
| CHEMBL1203601 | — | — | 1 | 7.50 |
| CHEMBL160607 | — | — | 1 | 7.00 |
| CHEMBL1202290 | — | — | 1 | 6.90 |
| CHEMBL345214 | — | — | 1 | 6.90 |
| CHEMBL1202291 | — | — | 1 | 6.80 |
| CHEMBL1203611 | — | — | 1 | 6.80 |
| CHEMBL156229 | — | — | 1 | 6.80 |
| CHEMBL1203603 | — | — | 1 | 6.80 |
| CHEMBL1202288 | — | — | 1 | 6.60 |
| CHEMBL345810 | — | — | 1 | 6.60 |
| CHEMBL346122 | — | — | 1 | 6.50 |
| CHEMBL158505 | — | — | 1 | 6.50 |
| CHEMBL160186 | — | — | 1 | 6.40 |
| CHEMBL348058 | — | — | 1 | 6.40 |
| CHEMBL1203644 | — | — | 1 | 6.40 |
| CHEMBL1237145 | — | — | 1 | 6.30 |
| CHEMBL1203602 | — | — | 1 | 6.20 |
| CHEMBL1203596 | — | — | 1 | 6.20 |
| CHEMBL1202292 | — | — | 1 | 6.20 |
| CHEMBL1203600 | — | — | 1 | 6.20 |
| CHEMBL156585 | — | — | 1 | 6.10 |
| CHEMBL1203631 | — | — | 1 | 6.10 |
| CHEMBL1203598 | — | — | 1 | 6.00 |
| CHEMBL348273 | — | — | 1 | 6.00 |
| CHEMBL1203597 | — | — | 1 | 6.00 |
| CHEMBL1203613 | — | — | 1 | 6.00 |
| CHEMBL1203595 | — | — | 1 | 5.90 |
| CHEMBL1203612 | — | — | 1 | 5.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1202289 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL123349 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL1203601 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL160607 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL1202290 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL345214 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL1202291 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL1203611 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL156229 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL1203603 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL1202288 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL345810 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL346122 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL158505 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL1203644 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL160186 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL348058 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL1237145 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL1203602 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL1203600 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL1203596 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL1202292 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL156585 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL1203631 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL1203598 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL348273 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL1203597 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL1203613 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL1203595 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL1203623 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL1203629 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL1203645 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL1203612 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL346276 | — | Ki | = | 1584.89 | nM | 5.80 |
| CHEMBL1203624 | — | Ki | = | 2511.89 | nM | 5.60 |
| CHEMBL160918 | — | Ki | = | 3162.28 | nM | 5.50 |
| CHEMBL1200399 | BUSPIRONE HYDROCHLORIDE | Ki | = | 5011.87 | nM | 5.30 |