Assay Detail
Binding
CHEMBL3267683
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Antagonist activity at human orexin-1 receptor expressed in CHO cells assessed as inhibition of Ala-6, 12-induced responses by FLIPR assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of dual orexin receptor antagonists with rat sleep efficacy enabled by expansion of the acetonitrile-assisted/diphosgene-mediated 2,4-dichloropyrimidine synthesis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.25 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3260832 | — | — | 1 | 7.82 |
| CHEMBL3260831 | — | — | 1 | 7.58 |
| CHEMBL1083358 | — | — | 1 | 7.57 |
| CHEMBL3260836 | — | — | 1 | 7.55 |
| CHEMBL3260834 | — | — | 1 | 7.51 |
| CHEMBL3260828 | — | — | 1 | 7.43 |
| CHEMBL3260826 | — | — | 1 | 7.35 |
| CHEMBL3260833 | — | — | 1 | 7.33 |
| CHEMBL1083659 | SUVOREXANT | 4.0 | 1 | 7.30 |
| CHEMBL3260835 | — | — | 1 | 7.28 |
| CHEMBL3260827 | — | — | 1 | 7.17 |
| CHEMBL3260823 | — | — | 1 | 7.04 |
| CHEMBL3260824 | — | — | 1 | 6.92 |
| CHEMBL3260829 | — | — | 1 | 6.71 |
| CHEMBL3260830 | — | — | 1 | 6.71 |
| CHEMBL3260825 | — | — | 1 | 6.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3260832 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3260831 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1083358 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3260836 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3260834 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3260828 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3260826 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3260833 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL1083659 | SUVOREXANT | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3260835 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3260827 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL3260823 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL3260824 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL3260829 | — | IC50 | = | 195.0 | nM | 6.71 |
| CHEMBL3260830 | — | IC50 | = | 195.0 | nM | 6.71 |
| CHEMBL3260825 | — | IC50 | = | 200.0 | nM | 6.70 |