Assay Detail
Binding
CHEMBL4353355
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting
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
1,3-Dioxane as a scaffold for potent and selective 5-HT1AR agonist with in-vivo anxiolytic, anti-depressant and anti-nociceptive activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 7.21 | 8.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4458714 | — | — | 1 | 8.14 |
| CHEMBL4462600 | — | — | 1 | 7.77 |
| CHEMBL31354 | WAY-100,635 | — | 1 | 7.73 |
| CHEMBL286003 | — | — | 1 | 7.71 |
| CHEMBL4467585 | — | — | 1 | 7.61 |
| CHEMBL4570387 | — | — | 1 | 7.51 |
| CHEMBL4588223 | — | — | 1 | 7.47 |
| CHEMBL37883 | — | — | 1 | 7.43 |
| CHEMBL4582160 | — | — | 1 | 7.41 |
| CHEMBL4468507 | — | — | 1 | 7.35 |
| CHEMBL4579802 | — | — | 1 | 7.30 |
| CHEMBL4520390 | — | — | 1 | 7.23 |
| CHEMBL4551941 | — | — | 1 | 7.22 |
| CHEMBL4439658 | — | — | 1 | 7.08 |
| CHEMBL4580335 | — | — | 1 | 7.05 |
| CHEMBL4457585 | — | — | 1 | 6.92 |
| CHEMBL4558985 | — | — | 1 | 6.85 |
| CHEMBL4473623 | — | — | 1 | 6.77 |
| CHEMBL4544457 | — | — | 1 | 6.54 |
| CHEMBL4462768 | — | — | 1 | 6.37 |
| CHEMBL4526865 | — | — | 1 | 6.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4458714 | — | Ki | = | 7.244 | nM | 8.14 |
| CHEMBL4462600 | — | Ki | = | 16.98 | nM | 7.77 |
| CHEMBL31354 | WAY-100,635 | Ki | = | 18.62 | nM | 7.73 |
| CHEMBL286003 | — | Ki | = | 19.5 | nM | 7.71 |
| CHEMBL4467585 | — | Ki | = | 24.55 | nM | 7.61 |
| CHEMBL4570387 | — | Ki | = | 30.9 | nM | 7.51 |
| CHEMBL4588223 | — | Ki | = | 33.88 | nM | 7.47 |
| CHEMBL37883 | — | Ki | = | 37.15 | nM | 7.43 |
| CHEMBL4582160 | — | Ki | = | 38.9 | nM | 7.41 |
| CHEMBL4468507 | — | Ki | = | 44.67 | nM | 7.35 |
| CHEMBL4579802 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL4520390 | — | Ki | = | 58.88 | nM | 7.23 |
| CHEMBL4551941 | — | Ki | = | 60.26 | nM | 7.22 |
| CHEMBL4439658 | — | Ki | = | 83.18 | nM | 7.08 |
| CHEMBL4580335 | — | Ki | = | 89.13 | nM | 7.05 |
| CHEMBL4457585 | — | Ki | = | 120.23 | nM | 6.92 |
| CHEMBL4558985 | — | Ki | = | 141.25 | nM | 6.85 |
| CHEMBL4473623 | — | Ki | = | 169.82 | nM | 6.77 |
| CHEMBL4544457 | — | Ki | = | 288.4 | nM | 6.54 |
| CHEMBL4462768 | — | Ki | = | 426.58 | nM | 6.37 |
| CHEMBL4526865 | — | Ki | = | 977.24 | nM | 6.01 |