Assay Detail
Functional
CHEMBL1119826
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human OX2R 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 | 7.49 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1084949 | — | — | 1 | 7.75 |
| CHEMBL469146 | — | — | 1 | 7.57 |
| CHEMBL1083358 | — | — | 1 | 7.57 |
| CHEMBL1083657 | — | — | 1 | 7.55 |
| CHEMBL1083357 | — | — | 1 | 7.52 |
| CHEMBL1083041 | — | — | 1 | 7.50 |
| CHEMBL1083659 | SUVOREXANT | 4.0 | 1 | 7.25 |
| CHEMBL1083658 | — | — | 1 | 7.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1084949 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL469146 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1083358 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1083657 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL1083357 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1083041 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL1083659 | SUVOREXANT | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL1083658 | — | IC50 | = | 57.0 | nM | 7.24 |