Assay Detail
Binding
CHEMBL1035000
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Displacement of [3H]prazosin from human cloned alpha1D adrenoceptor expressed in CHO cells
21
Total Activities
21
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
Structure-activity relationships in 1,4-benzodioxan-related compounds. 9. From 1,4-benzodioxane to 1,4-dioxane ring as a promising template of novel alpha1D-adrenoreceptor antagonists, 5-HT1A full agonists, and cytotoxic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 7.56 | 9.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL25554 | — | — | 1 | 9.29 |
| CHEMBL493486 | — | — | 1 | 8.94 |
| CHEMBL13647 | BMY-7378 | — | 1 | 8.89 |
| CHEMBL493285 | — | — | 1 | 8.44 |
| CHEMBL521665 | — | — | 1 | 7.79 |
| CHEMBL493041 | — | — | 1 | 7.50 |
| CHEMBL452437 | — | — | 1 | 7.36 |
| CHEMBL493697 | — | — | 1 | 7.18 |
| CHEMBL492835 | — | — | 1 | 7.14 |
| CHEMBL494908 | — | — | 1 | 7.01 |
| CHEMBL493283 | — | — | 1 | 6.99 |
| CHEMBL495289 | — | — | 1 | 6.90 |
| CHEMBL492785 | — | — | 1 | 6.81 |
| CHEMBL493284 | — | — | 1 | 6.77 |
| CHEMBL449057 | — | — | 1 | 6.45 |
| CHEMBL493661 | — | — | 1 | - |
| CHEMBL492834 | — | — | 1 | - |
| CHEMBL493042 | — | — | 1 | - |
| CHEMBL493043 | — | — | 1 | - |
| CHEMBL56 | 8-OH-DPAT | — | 1 | - |
| CHEMBL521694 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL25554 | — | Ki | = | 0.5129 | nM | 9.29 |
| CHEMBL493486 | — | Ki | = | 1.148 | nM | 8.94 |
| CHEMBL13647 | BMY-7378 | Ki | = | 1.288 | nM | 8.89 |
| CHEMBL493285 | — | Ki | = | 3.631 | nM | 8.44 |
| CHEMBL521665 | — | Ki | = | 16.22 | nM | 7.79 |
| CHEMBL493041 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL452437 | — | Ki | = | 43.65 | nM | 7.36 |
| CHEMBL493697 | — | Ki | = | 66.07 | nM | 7.18 |
| CHEMBL492835 | — | Ki | = | 72.44 | nM | 7.14 |
| CHEMBL494908 | — | Ki | = | 97.72 | nM | 7.01 |
| CHEMBL493283 | — | Ki | = | 102.33 | nM | 6.99 |
| CHEMBL495289 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL492785 | — | Ki | = | 154.88 | nM | 6.81 |
| CHEMBL493284 | — | Ki | = | 169.82 | nM | 6.77 |
| CHEMBL449057 | — | Ki | = | 354.81 | nM | 6.45 |
| CHEMBL493661 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL492834 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL493042 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL493043 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL56 | 8-OH-DPAT | Ki | > | 1000.0 | nM | - |
| CHEMBL521694 | — | Ki | > | 1000.0 | nM | - |