Assay Detail
Binding
CHEMBL3771845
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Antagonist activity at OX2R (unknown origin)
12
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.07 | 7.85 |
| pKb | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3597953 | — | — | 1 | 7.85 |
| CHEMBL3770745 | — | — | 1 | 7.75 |
| CHEMBL469146 | — | — | 1 | 7.57 |
| CHEMBL1083358 | — | — | 1 | 7.57 |
| CHEMBL1083659 | SUVOREXANT | 4.0 | 1 | 7.25 |
| CHEMBL490082 | — | — | 1 | 7.10 |
| CHEMBL3586412 | — | — | 1 | 7.01 |
| CHEMBL493427 | — | — | 1 | 7.00 |
| CHEMBL489485 | — | — | 1 | 6.55 |
| CHEMBL490489 | — | — | 1 | 5.09 |
| CHEMBL359632 | — | — | 1 | - |
| CHEMBL3771066 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3597953 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3770745 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL469146 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1083358 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1083659 | SUVOREXANT | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL490082 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3586412 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL493427 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL489485 | — | IC50 | = | 281.0 | nM | 6.55 |
| CHEMBL490489 | — | IC50 | = | 8152.0 | nM | 5.09 |
| CHEMBL359632 | — | pKb | = | 8.3 | — | - |
| CHEMBL3771066 | — | IC50 | > | 10000.0 | nM | - |