Assay Detail
Binding
CHEMBL1035001
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Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor expressed in human HeLa cells
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| 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 | 7.85 | 9.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL13647 | BMY-7378 | — | 1 | 9.43 |
| CHEMBL493285 | — | — | 1 | 9.23 |
| CHEMBL493486 | — | — | 1 | 9.18 |
| CHEMBL493697 | — | — | 1 | 8.85 |
| CHEMBL25554 | — | — | 1 | 8.68 |
| CHEMBL56 | 8-OH-DPAT | — | 1 | 8.47 |
| CHEMBL521665 | — | — | 1 | 8.46 |
| CHEMBL452437 | — | — | 1 | 8.38 |
| CHEMBL493041 | — | — | 1 | 8.22 |
| CHEMBL493283 | — | — | 1 | 8.12 |
| CHEMBL449057 | — | — | 1 | 7.59 |
| CHEMBL495289 | — | — | 1 | 7.43 |
| CHEMBL494908 | — | — | 1 | 7.41 |
| CHEMBL492785 | — | — | 1 | 7.28 |
| CHEMBL492835 | — | — | 1 | 7.27 |
| CHEMBL521694 | — | — | 1 | 6.83 |
| CHEMBL493284 | — | — | 1 | 6.64 |
| CHEMBL493661 | — | — | 1 | 6.63 |
| CHEMBL492834 | — | — | 1 | 6.59 |
| CHEMBL493042 | — | — | 1 | 6.38 |
| CHEMBL493043 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL13647 | BMY-7378 | Ki | = | 0.3715 | nM | 9.43 |
| CHEMBL493285 | — | Ki | = | 0.5888 | nM | 9.23 |
| CHEMBL493486 | — | Ki | = | 0.6607 | nM | 9.18 |
| CHEMBL493697 | — | Ki | = | 1.413 | nM | 8.85 |
| CHEMBL25554 | — | Ki | = | 2.089 | nM | 8.68 |
| CHEMBL56 | 8-OH-DPAT | Ki | = | 3.388 | nM | 8.47 |
| CHEMBL521665 | — | Ki | = | 3.467 | nM | 8.46 |
| CHEMBL452437 | — | Ki | = | 4.169 | nM | 8.38 |
| CHEMBL493041 | — | Ki | = | 6.026 | nM | 8.22 |
| CHEMBL493283 | — | Ki | = | 7.586 | nM | 8.12 |
| CHEMBL449057 | — | Ki | = | 25.7 | nM | 7.59 |
| CHEMBL495289 | — | Ki | = | 37.15 | nM | 7.43 |
| CHEMBL494908 | — | Ki | = | 38.9 | nM | 7.41 |
| CHEMBL492785 | — | Ki | = | 52.48 | nM | 7.28 |
| CHEMBL492835 | — | Ki | = | 53.7 | nM | 7.27 |
| CHEMBL521694 | — | Ki | = | 147.91 | nM | 6.83 |
| CHEMBL493284 | — | Ki | = | 229.09 | nM | 6.64 |
| CHEMBL493661 | — | Ki | = | 234.42 | nM | 6.63 |
| CHEMBL492834 | — | Ki | = | 257.04 | nM | 6.59 |
| CHEMBL493042 | — | Ki | = | 416.87 | nM | 6.38 |
| CHEMBL493043 | — | Ki | > | 1000.0 | nM | - |