Assay Detail
Binding
CHEMBL3384633
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-Orexin A from human OX2R expressed in CHO cells after 30 mins by topcount analysis
27
Total Activities
26
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
Design, synthesis, and structure-activity relationships of a series of novel N-aryl-2-phenylcyclopropanecarboxamide that are potent and orally active orexin receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 6.92 | 8.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL455136 | ALMOREXANT | 3.0 | 1 | 8.33 |
| CHEMBL3343260 | — | — | 2 | 8.30 |
| CHEMBL3343242 | — | — | 1 | 8.14 |
| CHEMBL1272307 | SB-649868 | 2.0 | 1 | 8.07 |
| CHEMBL1083659 | SUVOREXANT | 4.0 | 1 | 7.93 |
| CHEMBL3343259 | — | — | 1 | 7.85 |
| CHEMBL3343255 | — | — | 1 | 7.85 |
| CHEMBL3343257 | — | — | 1 | 7.57 |
| CHEMBL3343256 | — | — | 1 | 7.55 |
| CHEMBL3343258 | — | — | 1 | 7.47 |
| CHEMBL3343254 | — | — | 1 | 7.46 |
| CHEMBL3343246 | — | — | 1 | 7.44 |
| CHEMBL3343252 | — | — | 1 | 7.29 |
| CHEMBL3343253 | — | — | 1 | 7.07 |
| CHEMBL3343248 | — | — | 1 | 6.89 |
| CHEMBL3343250 | — | — | 1 | 6.42 |
| CHEMBL3341773 | — | — | 1 | 6.23 |
| CHEMBL3343247 | — | — | 1 | 6.01 |
| CHEMBL3343249 | — | — | 1 | 5.88 |
| CHEMBL3343251 | — | — | 1 | 5.48 |
| CHEMBL3343241 | — | — | 1 | 5.37 |
| CHEMBL3343244 | — | — | 1 | 5.33 |
| CHEMBL3343243 | — | — | 1 | 5.11 |
| CHEMBL3343239 | — | — | 1 | 5.06 |
| CHEMBL3343240 | — | — | 1 | - |
| CHEMBL3343245 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL455136 | ALMOREXANT | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL3343260 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL3343242 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL1272307 | SB-649868 | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL1083659 | SUVOREXANT | Ki | = | 11.8 | nM | 7.93 |
| CHEMBL3343259 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL3343255 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL3343257 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL3343256 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL3343258 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL3343254 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL3343246 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL3343252 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL3343253 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL3343248 | — | Ki | = | 129.0 | nM | 6.89 |
| CHEMBL3343250 | — | Ki | = | 384.0 | nM | 6.42 |
| CHEMBL3341773 | — | Ki | = | 588.0 | nM | 6.23 |
| CHEMBL3343247 | — | Ki | = | 967.0 | nM | 6.01 |
| CHEMBL3343249 | — | Ki | = | 1330.0 | nM | 5.88 |
| CHEMBL3343251 | — | Ki | = | 3336.0 | nM | 5.48 |
| CHEMBL3343241 | — | Ki | = | 4226.0 | nM | 5.37 |
| CHEMBL3343244 | — | Ki | = | 4679.0 | nM | 5.33 |
| CHEMBL3343243 | — | Ki | = | 7846.0 | nM | 5.11 |
| CHEMBL3343239 | — | Ki | = | 8654.0 | nM | 5.06 |
| CHEMBL3343240 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3343245 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3343260 | — | Ki | > | 2000.0 | nM | - |