Assay Detail
Functional
CHEMBL5629576
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human Ox1R overexpressed in rat Chem-1 cells assessed as inhibition of orexin A induced calcium flux preincubated for 15 mins followed by orexin A addition by FLIPR analysis
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | Chem-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and first-time disclosure of CVN766, an exquisitely selective orexin 1 receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.52 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3941690 | — | — | 1 | 8.22 |
| CHEMBL3958101 | CVN-766 | 1.0 | 1 | 8.10 |
| CHEMBL5633370 | — | — | 1 | 7.80 |
| CHEMBL3932722 | — | — | 1 | 7.80 |
| CHEMBL5631363 | — | — | 1 | 7.77 |
| CHEMBL3954899 | — | — | 1 | 7.68 |
| CHEMBL3963632 | — | — | 1 | 7.50 |
| CHEMBL3927726 | — | — | 1 | 7.47 |
| CHEMBL3957941 | — | — | 1 | 7.28 |
| CHEMBL3922313 | — | — | 1 | 7.17 |
| CHEMBL5632556 | — | — | 1 | 5.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3941690 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3958101 | CVN-766 | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5633370 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3932722 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5631363 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3954899 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3963632 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3927726 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3957941 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3922313 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL5632556 | — | IC50 | = | 1230.0 | nM | 5.91 |