Assay Detail
Binding
CHEMBL3101094
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Displacement of [3H]SB-674042 from human orexin-1 receptor after 60 mins by scintillation counting analysis
16
Total Activities
16
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 2,5-diarylnicotinamides as selective orexin-2 receptor antagonists (2-SORAs).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 5.84 | 7.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3099899 | — | — | 1 | 7.03 |
| CHEMBL3099892 | — | — | 1 | 6.63 |
| CHEMBL3099886 | — | — | 1 | 6.56 |
| CHEMBL3099893 | — | — | 1 | 6.33 |
| CHEMBL3099897 | — | — | 1 | 6.13 |
| CHEMBL3099889 | — | — | 1 | 6.08 |
| CHEMBL3099894 | — | — | 1 | 5.97 |
| CHEMBL3099898 | — | — | 1 | 5.96 |
| CHEMBL3099891 | — | — | 1 | 5.96 |
| CHEMBL3099885 | — | — | 1 | 5.72 |
| CHEMBL3099888 | — | — | 1 | 5.53 |
| CHEMBL3099890 | — | — | 1 | 5.47 |
| CHEMBL3099884 | — | — | 1 | 5.45 |
| CHEMBL3099895 | — | — | 1 | 5.29 |
| CHEMBL3099887 | — | — | 1 | 5.14 |
| CHEMBL3099896 | — | — | 1 | 4.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3099899 | — | Ki | = | 94.5 | nM | 7.03 |
| CHEMBL3099892 | — | Ki | = | 236.0 | nM | 6.63 |
| CHEMBL3099886 | — | Ki | = | 273.0 | nM | 6.56 |
| CHEMBL3099893 | — | Ki | = | 462.0 | nM | 6.33 |
| CHEMBL3099897 | — | Ki | = | 747.0 | nM | 6.13 |
| CHEMBL3099889 | — | Ki | = | 833.0 | nM | 6.08 |
| CHEMBL3099894 | — | Ki | = | 1073.0 | nM | 5.97 |
| CHEMBL3099898 | — | Ki | = | 1087.0 | nM | 5.96 |
| CHEMBL3099891 | — | Ki | = | 1105.0 | nM | 5.96 |
| CHEMBL3099885 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL3099888 | — | Ki | = | 2975.0 | nM | 5.53 |
| CHEMBL3099890 | — | Ki | = | 3350.0 | nM | 5.47 |
| CHEMBL3099884 | — | Ki | = | 3550.0 | nM | 5.45 |
| CHEMBL3099895 | — | Ki | = | 5150.0 | nM | 5.29 |
| CHEMBL3099887 | — | Ki | = | 7250.0 | nM | 5.14 |
| CHEMBL3099896 | — | Ki | = | 65000.0 | nM | 4.19 |