Assay Detail
Binding
CHEMBL1246630
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Displacement [3H]prazosin of human recombinant Alpha-1B adrenergic receptor expressed in CHO cells by rapid filtration technique
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 7.23 | 8.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1242352 | — | — | 1 | 8.17 |
| CHEMBL1242912 | — | — | 1 | 8.03 |
| CHEMBL1241557 | — | — | 1 | 8.00 |
| CHEMBL1242633 | — | — | 1 | 7.74 |
| CHEMBL1242818 | — | — | 1 | 7.33 |
| CHEMBL1242542 | — | — | 1 | 7.29 |
| CHEMBL31354 | WAY-100,635 | — | 1 | 7.18 |
| CHEMBL1242445 | — | — | 1 | 7.15 |
| CHEMBL1242632 | — | — | 1 | 7.14 |
| CHEMBL1242724 | — | — | 1 | 7.07 |
| CHEMBL1242541 | — | — | 1 | 6.89 |
| CHEMBL1242819 | — | — | 1 | 6.88 |
| CHEMBL1242444 | — | — | 1 | 6.76 |
| CHEMBL1242725 | — | — | 1 | 6.65 |
| CHEMBL13647 | BMY-7378 | — | 1 | 6.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1242352 | — | Ki | = | 6.761 | nM | 8.17 |
| CHEMBL1242912 | — | Ki | = | 9.333 | nM | 8.03 |
| CHEMBL1241557 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1242633 | — | Ki | = | 18.2 | nM | 7.74 |
| CHEMBL1242818 | — | Ki | = | 46.77 | nM | 7.33 |
| CHEMBL1242542 | — | Ki | = | 51.29 | nM | 7.29 |
| CHEMBL31354 | WAY-100,635 | Ki | = | 66.07 | nM | 7.18 |
| CHEMBL1242445 | — | Ki | = | 70.79 | nM | 7.15 |
| CHEMBL1242632 | — | Ki | = | 72.44 | nM | 7.14 |
| CHEMBL1242724 | — | Ki | = | 85.11 | nM | 7.07 |
| CHEMBL1242541 | — | Ki | = | 128.82 | nM | 6.89 |
| CHEMBL1242819 | — | Ki | = | 131.83 | nM | 6.88 |
| CHEMBL1242444 | — | Ki | = | 173.78 | nM | 6.76 |
| CHEMBL1242725 | — | Ki | = | 223.87 | nM | 6.65 |
| CHEMBL13647 | BMY-7378 | Ki | = | 707.95 | nM | 6.15 |