Assay Detail
Binding
CHEMBL3240641
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Binding affinity to human OX1 receptor in cell membrane by in vitro radioligand binding assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and evaluation of carbon-linked analogs of dual orexin receptor antagonist filorexant.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 7.42 | 9.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3235265 | — | — | 1 | 9.25 |
| CHEMBL3235249 | — | — | 1 | 9.00 |
| CHEMBL3235253 | — | — | 1 | 8.96 |
| CHEMBL3235251 | — | — | 1 | 7.77 |
| CHEMBL3235260 | — | — | 1 | 7.75 |
| CHEMBL3235257 | — | — | 1 | 7.62 |
| CHEMBL3235256 | — | — | 1 | 7.58 |
| CHEMBL3235254 | — | — | 1 | 7.57 |
| CHEMBL3235261 | — | — | 1 | 7.12 |
| CHEMBL3235264 | — | — | 1 | 7.12 |
| CHEMBL3235255 | — | — | 1 | 6.97 |
| CHEMBL3235263 | — | — | 1 | 6.97 |
| CHEMBL3235252 | — | — | 1 | 6.87 |
| CHEMBL3235259 | — | — | 1 | 6.68 |
| CHEMBL3235262 | — | — | 1 | 6.47 |
| CHEMBL3235250 | — | — | 1 | 6.33 |
| CHEMBL3235258 | — | — | 1 | 6.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3235265 | — | Ki | = | 0.56 | nM | 9.25 |
| CHEMBL3235249 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3235253 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3235251 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL3235260 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL3235257 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL3235256 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL3235254 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL3235261 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL3235264 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL3235255 | — | Ki | = | 107.0 | nM | 6.97 |
| CHEMBL3235263 | — | Ki | = | 108.0 | nM | 6.97 |
| CHEMBL3235252 | — | Ki | = | 135.0 | nM | 6.87 |
| CHEMBL3235259 | — | Ki | = | 211.0 | nM | 6.68 |
| CHEMBL3235262 | — | Ki | = | 339.0 | nM | 6.47 |
| CHEMBL3235250 | — | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL3235258 | — | Ki | = | 866.0 | nM | 6.06 |