Assay Detail
Binding
CHEMBL1034998
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]prazosin from human cloned alpha1A 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 | 6.85 | 9.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL25554 | — | — | 1 | 9.37 |
| CHEMBL493486 | — | — | 1 | 7.56 |
| CHEMBL493283 | — | — | 1 | 7.13 |
| CHEMBL493041 | — | — | 1 | 7.06 |
| CHEMBL493284 | — | — | 1 | 7.05 |
| CHEMBL494908 | — | — | 1 | 6.80 |
| CHEMBL493285 | — | — | 1 | 6.77 |
| CHEMBL452437 | — | — | 1 | 6.70 |
| CHEMBL495289 | — | — | 1 | 6.65 |
| CHEMBL493697 | — | — | 1 | 6.47 |
| CHEMBL13647 | BMY-7378 | — | 1 | 6.42 |
| CHEMBL492785 | — | — | 1 | 6.39 |
| CHEMBL521665 | — | — | 1 | 6.36 |
| CHEMBL493043 | — | — | 1 | 6.33 |
| CHEMBL493661 | — | — | 1 | 6.29 |
| CHEMBL521694 | — | — | 1 | 6.27 |
| CHEMBL449057 | — | — | 1 | - |
| CHEMBL492834 | — | — | 1 | - |
| CHEMBL492835 | — | — | 1 | - |
| CHEMBL493042 | — | — | 1 | - |
| CHEMBL56 | 8-OH-DPAT | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL25554 | — | Ki | = | 0.4266 | nM | 9.37 |
| CHEMBL493486 | — | Ki | = | 27.54 | nM | 7.56 |
| CHEMBL493283 | — | Ki | = | 74.13 | nM | 7.13 |
| CHEMBL493041 | — | Ki | = | 87.1 | nM | 7.06 |
| CHEMBL493284 | — | Ki | = | 89.13 | nM | 7.05 |
| CHEMBL494908 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL493285 | — | Ki | = | 169.82 | nM | 6.77 |
| CHEMBL452437 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL495289 | — | Ki | = | 223.87 | nM | 6.65 |
| CHEMBL493697 | — | Ki | = | 338.84 | nM | 6.47 |
| CHEMBL13647 | BMY-7378 | Ki | = | 380.19 | nM | 6.42 |
| CHEMBL492785 | — | Ki | = | 407.38 | nM | 6.39 |
| CHEMBL521665 | — | Ki | = | 436.52 | nM | 6.36 |
| CHEMBL493043 | — | Ki | = | 467.74 | nM | 6.33 |
| CHEMBL493661 | — | Ki | = | 512.86 | nM | 6.29 |
| CHEMBL521694 | — | Ki | = | 537.03 | nM | 6.27 |
| CHEMBL449057 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL492834 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL492835 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL493042 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL56 | 8-OH-DPAT | Ki | > | 1000.0 | nM | - |