Assay Detail
Functional
CHEMBL2438192
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at mouse OX1 receptor expressed in CHO cells assessed as inhibition of orexin A-induced Ca2+ accumulation after 1 hr by Fluo-4-AM staining-based FLIPR assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Orexin/Hypocretin receptor type 1 (CHEMBL2434819) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Identification of a novel series of orexin receptor antagonists with a distinct effect on sleep architecture for the treatment of insomnia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 2 | 7.56 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1083659 | SUVOREXANT | 4.0 | 1 | 8.77 |
| CHEMBL2435402 | — | — | 1 | 6.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1083659 | SUVOREXANT | Ki | = | 1.698 | nM | 8.77 |
| CHEMBL2435402 | — | Ki | = | 457.09 | nM | 6.34 |