Assay Detail
Binding
CHEMBL3395398
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human OX2R by radioligand displacement assay
25
Total Activities
25
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
Discovery of piperidine ethers as selective orexin receptor antagonists (SORAs) inspired by filorexant.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 25 | 8.18 | 9.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3394847 | — | — | 1 | 9.62 |
| CHEMBL2107822 | FILOREXANT | 2.0 | 1 | 9.52 |
| CHEMBL3394829 | — | — | 1 | 9.52 |
| CHEMBL3394842 | — | — | 1 | 9.22 |
| CHEMBL3394845 | — | — | 1 | 9.10 |
| CHEMBL3394840 | — | — | 1 | 9.05 |
| CHEMBL3394828 | — | — | 1 | 9.00 |
| CHEMBL3394844 | — | — | 1 | 8.96 |
| CHEMBL3394841 | — | — | 1 | 8.89 |
| CHEMBL3394839 | — | — | 1 | 8.59 |
| CHEMBL3394833 | — | — | 1 | 8.29 |
| CHEMBL3394838 | — | — | 1 | 8.28 |
| CHEMBL3394832 | — | — | 1 | 8.17 |
| CHEMBL3394830 | — | — | 1 | 8.12 |
| CHEMBL3394825 | — | — | 1 | 8.05 |
| CHEMBL3394831 | — | — | 1 | 8.03 |
| CHEMBL3394834 | — | — | 1 | 8.01 |
| CHEMBL3394827 | — | — | 1 | 7.75 |
| CHEMBL3394835 | — | — | 1 | 7.54 |
| CHEMBL3394826 | — | — | 1 | 7.26 |
| CHEMBL3394843 | — | — | 1 | 7.20 |
| CHEMBL3394836 | — | — | 1 | 6.83 |
| CHEMBL3394837 | — | — | 1 | 6.75 |
| CHEMBL3394846 | — | — | 1 | 6.43 |
| CHEMBL3394848 | — | — | 1 | 6.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3394847 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL2107822 | FILOREXANT | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3394829 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3394842 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL3394845 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL3394840 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL3394828 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3394844 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3394841 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL3394839 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL3394833 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL3394838 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL3394832 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL3394830 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL3394825 | — | Ki | = | 8.9 | nM | 8.05 |
| CHEMBL3394831 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL3394834 | — | Ki | = | 9.8 | nM | 8.01 |
| CHEMBL3394827 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL3394835 | — | Ki | = | 28.9 | nM | 7.54 |
| CHEMBL3394826 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL3394843 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL3394836 | — | Ki | = | 149.0 | nM | 6.83 |
| CHEMBL3394837 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL3394846 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL3394848 | — | Ki | = | 521.0 | nM | 6.28 |