Assay Detail
Binding
CHEMBL868699
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]8-hydroxy-2-(di-n-propylamino)tetralin from cloned human 5HT1A receptor expressed in HeLa cells
16
Total Activities
16
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Structure-activity relationships in 1,4-benzodioxan-related compounds. 8.(1) {2-[2-(4-chlorobenzyloxy)phenoxy]ethyl}-[2-(2,6-dimethoxyphenoxy)ethyl]amine (clopenphendioxan) as a tool to highlight the involvement of alpha1D- and alpha1B-adrenoreceptor subtypes in the regulation of human PC-3 prostate cancer cell apoptosis and proliferation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 7.82 | 8.32 |
| Log Ki | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL200839 | — | — | 1 | 8.32 |
| CHEMBL198860 | — | — | 1 | 8.18 |
| CHEMBL382972 | — | — | 1 | 7.95 |
| CHEMBL43116 | — | — | 1 | 7.93 |
| CHEMBL196817 | — | — | 1 | 7.93 |
| CHEMBL200446 | CLOPENPHENDIOXAN | — | 1 | 7.81 |
| CHEMBL200580 | — | — | 1 | 7.76 |
| CHEMBL199080 | — | — | 1 | 7.74 |
| CHEMBL197442 | — | — | 1 | 7.68 |
| CHEMBL200366 | — | — | 1 | 7.65 |
| CHEMBL198431 | — | — | 1 | 7.63 |
| CHEMBL200136 | — | — | 1 | 7.62 |
| CHEMBL427552 | — | — | 1 | 7.51 |
| CHEMBL707 | DOXAZOSIN | 4.0 | 1 | - |
| CHEMBL199077 | — | — | 1 | - |
| CHEMBL200777 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL200839 | — | Ki | = | 4.786 | nM | 8.32 |
| CHEMBL198860 | — | Ki | = | 6.607 | nM | 8.18 |
| CHEMBL382972 | — | Ki | = | 11.22 | nM | 7.95 |
| CHEMBL43116 | — | Ki | = | 11.75 | nM | 7.93 |
| CHEMBL196817 | — | Ki | = | 11.75 | nM | 7.93 |
| CHEMBL200446 | CLOPENPHENDIOXAN | Ki | = | 15.49 | nM | 7.81 |
| CHEMBL200580 | — | Ki | = | 17.38 | nM | 7.76 |
| CHEMBL199080 | — | Ki | = | 18.2 | nM | 7.74 |
| CHEMBL197442 | — | Ki | = | 20.89 | nM | 7.68 |
| CHEMBL200366 | — | Ki | = | 22.39 | nM | 7.65 |
| CHEMBL198431 | — | Ki | = | 23.44 | nM | 7.63 |
| CHEMBL200136 | — | Ki | = | 23.99 | nM | 7.62 |
| CHEMBL427552 | — | Ki | = | 30.9 | nM | 7.51 |
| CHEMBL707 | DOXAZOSIN | Log Ki | - | — | - | |
| CHEMBL199077 | — | Log Ki | - | — | - | |
| CHEMBL200777 | — | Log Ki | - | — | - |