Assay Detail
Functional
CHEMBL3868337
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at rat OX1 receptor assessed as inhibition of Ala-6,12 orexin-A-induced calcium increase preincubated for 5 mins prior to Ala-6,12 orexin-A addition measured at 1 sec intervals for 1 min by Fluo-4AM dye-based FLIPR assay
3
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Orexin/Hypocretin receptor type 1 (CHEMBL1075232) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Discovery of highly potent and selective orexin 1 receptor antagonists (1-SORAs) suitable for in vivo interrogation of orexin 1 receptor pharmacology.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 7.88 | 7.96 |
| Ki | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3394848 | — | — | 1 | 7.96 |
| CHEMBL3973097 | — | — | 1 | 7.80 |
| CHEMBL3955752 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3394848 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3973097 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3955752 | — | Ki | > | 6800.0 | nM | - |