Assay Detail
Functional
CHEMBL1833030
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at recombinant human OX2R expressed in CHO cells by FLIPR calcium based functional assay
14
Total Activities
14
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 process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 7.68 | 9.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1830963 | — | — | 1 | 9.60 |
| CHEMBL1272307 | SB-649868 | 2.0 | 1 | 9.40 |
| CHEMBL1830961 | — | — | 1 | 9.10 |
| CHEMBL1830968 | — | — | 1 | 8.30 |
| CHEMBL1830967 | — | — | 1 | 7.70 |
| CHEMBL1830962 | — | — | 1 | 7.70 |
| CHEMBL1830959 | — | — | 1 | 7.70 |
| CHEMBL1830966 | — | — | 1 | 7.50 |
| CHEMBL1830964 | — | — | 1 | 7.50 |
| CHEMBL1830960 | — | — | 1 | 6.90 |
| CHEMBL1830956 | — | — | 1 | 6.30 |
| CHEMBL1830957 | — | — | 1 | 6.20 |
| CHEMBL1830965 | — | — | 1 | 5.90 |
| CHEMBL1830958 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1830963 | — | Ki | = | 0.2512 | nM | 9.60 |
| CHEMBL1272307 | SB-649868 | Ki | = | 0.3981 | nM | 9.40 |
| CHEMBL1830961 | — | Ki | = | 0.7943 | nM | 9.10 |
| CHEMBL1830968 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL1830967 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL1830962 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL1830959 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL1830966 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL1830964 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL1830960 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL1830956 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL1830957 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL1830965 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL1830958 | — | Ki | > | 3162.28 | nM | - |