Assay Detail
Functional
CHEMBL1119825
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Antagonist activity at human OX1R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium mobilization after 5 mins by FLIPR assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.54 | 7.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1083657 | — | — | 1 | 7.62 |
| CHEMBL1083658 | — | — | 1 | 7.62 |
| CHEMBL1084949 | — | — | 1 | 7.58 |
| CHEMBL1083358 | — | — | 1 | 7.57 |
| CHEMBL1083041 | — | — | 1 | 7.55 |
| CHEMBL469146 | — | — | 1 | 7.54 |
| CHEMBL1083357 | — | — | 1 | 7.52 |
| CHEMBL1083659 | SUVOREXANT | 4.0 | 1 | 7.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1083657 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL1083658 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL1084949 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1083358 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1083041 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL469146 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL1083357 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1083659 | SUVOREXANT | IC50 | = | 50.0 | nM | 7.30 |