Assay Detail
Functional
CHEMBL2400169
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human OX1R expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
23
Total Activities
23
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
Structure-activity relationship studies and sleep-promoting activity of novel 1-chloro-5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine derivatives as dual orexin receptor antagonists. Part 2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.13 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL455136 | ALMOREXANT | 3.0 | 1 | 7.89 |
| CHEMBL2396838 | — | — | 1 | 7.80 |
| CHEMBL2396835 | — | — | 1 | 7.80 |
| CHEMBL2396833 | — | — | 1 | 7.77 |
| CHEMBL2396867 | — | — | 1 | 7.75 |
| CHEMBL2396869 | — | — | 1 | 7.70 |
| CHEMBL2347607 | — | — | 1 | 7.52 |
| CHEMBL2396836 | — | — | 1 | 7.52 |
| CHEMBL2396834 | — | — | 1 | 7.50 |
| CHEMBL2347482 | — | — | 1 | 7.40 |
| CHEMBL2396870 | — | — | 1 | 7.35 |
| CHEMBL2396840 | — | — | 1 | 7.28 |
| CHEMBL2396861 | — | — | 1 | 7.14 |
| CHEMBL2396865 | — | — | 1 | 7.13 |
| CHEMBL2396839 | — | — | 1 | 7.04 |
| CHEMBL2396841 | — | — | 1 | 7.03 |
| CHEMBL2396842 | — | — | 1 | 6.77 |
| CHEMBL2396866 | — | — | 1 | 6.69 |
| CHEMBL2396863 | — | — | 1 | 6.51 |
| CHEMBL2396837 | — | — | 1 | 6.42 |
| CHEMBL2396862 | — | — | 1 | 6.37 |
| CHEMBL2396868 | — | — | 1 | 6.26 |
| CHEMBL2396864 | — | — | 1 | 5.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL455136 | ALMOREXANT | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2396838 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2396835 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2396833 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL2396867 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2396869 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2347607 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2396836 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2396834 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL2347482 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2396870 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL2396840 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL2396861 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL2396865 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL2396839 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL2396841 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL2396842 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL2396866 | — | IC50 | = | 203.0 | nM | 6.69 |
| CHEMBL2396863 | — | IC50 | = | 312.0 | nM | 6.51 |
| CHEMBL2396837 | — | IC50 | = | 378.0 | nM | 6.42 |
| CHEMBL2396862 | — | IC50 | = | 431.0 | nM | 6.37 |
| CHEMBL2396868 | — | IC50 | = | 547.0 | nM | 6.26 |
| CHEMBL2396864 | — | IC50 | = | 3902.0 | nM | 5.41 |