Assay Detail
Binding
CHEMBL3868341
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Antagonist activity at human OX1 receptor Ile408-Val mutant expressed on CHO cell membrane 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
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
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 | 3 | 7.27 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3955752 | — | — | 1 | 7.52 |
| CHEMBL3973097 | — | — | 1 | 7.24 |
| CHEMBL3394848 | — | — | 1 | 7.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3955752 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3973097 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL3394848 | — | IC50 | = | 89.0 | nM | 7.05 |