Assay Detail
Functional
CHEMBL3625146
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Antagonist activity at human orexin 2 receptor expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium level after 60 mins by FLIPR assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of diazepane amide DORAs and 2-SORAs enabled by exploration of isosteric quinazoline replacements.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.19 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1083659 | SUVOREXANT | 4.0 | 1 | 9.40 |
| CHEMBL3622325 | — | — | 1 | 7.58 |
| CHEMBL1083358 | — | — | 1 | 7.57 |
| CHEMBL3622332 | — | — | 1 | 7.57 |
| CHEMBL3622326 | — | — | 1 | 7.52 |
| CHEMBL3622327 | — | — | 1 | 7.42 |
| CHEMBL3622331 | — | — | 1 | 7.37 |
| CHEMBL3622333 | — | — | 1 | 7.36 |
| CHEMBL3622330 | — | — | 1 | 7.28 |
| CHEMBL3622329 | — | — | 1 | 7.00 |
| CHEMBL3622328 | — | — | 1 | 6.92 |
| CHEMBL3622337 | — | — | 1 | 6.61 |
| CHEMBL3622336 | — | — | 1 | 5.58 |
| CHEMBL3622323 | — | — | 1 | 5.50 |
| CHEMBL3622335 | — | — | 1 | - |
| CHEMBL3622334 | — | — | 1 | - |
| CHEMBL3622322 | — | — | 1 | - |
| CHEMBL3622324 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1083659 | SUVOREXANT | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3622325 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1083358 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3622332 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3622326 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3622327 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3622331 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3622333 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL3622330 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL3622329 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL3622328 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3622337 | — | IC50 | = | 245.0 | nM | 6.61 |
| CHEMBL3622336 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL3622323 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL3622335 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3622334 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3622322 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3622324 | — | IC50 | > | 10000.0 | nM | - |