Assay Detail
Binding
CHEMBL4353358
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Displacement of [3H]8-OH-DPAT from human cloned 5HT-1AR transfected in HeLa cells incubated for 30 mins by liquid scintillation counter
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
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 | 8.30 | 9.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL31354 | WAY-100,635 | — | 1 | 9.48 |
| CHEMBL4458714 | — | — | 1 | 9.30 |
| CHEMBL286003 | — | — | 1 | 9.22 |
| CHEMBL4467585 | — | — | 1 | 9.11 |
| CHEMBL4462600 | — | — | 1 | 8.87 |
| CHEMBL4439658 | — | — | 1 | 8.81 |
| CHEMBL4588223 | — | — | 1 | 8.79 |
| CHEMBL4582160 | — | — | 1 | 8.73 |
| CHEMBL4570387 | — | — | 1 | 8.70 |
| CHEMBL4526865 | — | — | 1 | 8.50 |
| CHEMBL37883 | — | — | 1 | 8.45 |
| CHEMBL4558985 | — | — | 1 | 8.34 |
| CHEMBL4457585 | — | — | 1 | 8.28 |
| CHEMBL4468507 | — | — | 1 | 8.14 |
| CHEMBL4462768 | — | — | 1 | 7.94 |
| CHEMBL4551941 | — | — | 1 | 7.81 |
| CHEMBL4544457 | — | — | 1 | 7.63 |
| CHEMBL4579802 | — | — | 1 | 7.59 |
| CHEMBL4580335 | — | — | 1 | 7.24 |
| CHEMBL4473623 | — | — | 1 | 7.22 |
| CHEMBL4520390 | — | — | 1 | 6.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL31354 | WAY-100,635 | Ki | = | 0.3311 | nM | 9.48 |
| CHEMBL4458714 | — | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL286003 | — | Ki | = | 0.6026 | nM | 9.22 |
| CHEMBL4467585 | — | Ki | = | 0.7762 | nM | 9.11 |
| CHEMBL4462600 | — | Ki | = | 1.349 | nM | 8.87 |
| CHEMBL4439658 | — | Ki | = | 1.549 | nM | 8.81 |
| CHEMBL4588223 | — | Ki | = | 1.622 | nM | 8.79 |
| CHEMBL4582160 | — | Ki | = | 1.862 | nM | 8.73 |
| CHEMBL4570387 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL4526865 | — | Ki | = | 3.162 | nM | 8.50 |
| CHEMBL37883 | — | Ki | = | 3.548 | nM | 8.45 |
| CHEMBL4558985 | — | Ki | = | 4.571 | nM | 8.34 |
| CHEMBL4457585 | — | Ki | = | 5.248 | nM | 8.28 |
| CHEMBL4468507 | — | Ki | = | 7.244 | nM | 8.14 |
| CHEMBL4462768 | — | Ki | = | 11.48 | nM | 7.94 |
| CHEMBL4551941 | — | Ki | = | 15.49 | nM | 7.81 |
| CHEMBL4544457 | — | Ki | = | 23.44 | nM | 7.63 |
| CHEMBL4579802 | — | Ki | = | 25.7 | nM | 7.59 |
| CHEMBL4580335 | — | Ki | = | 57.54 | nM | 7.24 |
| CHEMBL4473623 | — | Ki | = | 60.26 | nM | 7.22 |
| CHEMBL4520390 | — | Ki | = | 724.44 | nM | 6.14 |