Assay Detail
Functional
CHEMBL983968
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human CB1 receptor expressed in CHOK1 cells assessed as inhibition of CP-55940-induced response after 10 mins by GTPgamma[35S] binding assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 8.50 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL520345 | — | — | 1 | 9.15 |
| CHEMBL483543 | — | — | 1 | 9.10 |
| CHEMBL484929 | — | — | 1 | 9.09 |
| CHEMBL201602 | — | — | 1 | 9.00 |
| CHEMBL482742 | — | — | 1 | 8.82 |
| CHEMBL111 | RIMONABANT | 4.0 | 1 | 8.80 |
| CHEMBL485538 | — | — | 1 | 8.51 |
| CHEMBL482741 | — | — | 1 | 8.32 |
| CHEMBL485013 | — | — | 1 | 8.26 |
| CHEMBL482985 | — | — | 1 | 8.01 |
| CHEMBL518982 | — | — | 1 | 7.96 |
| CHEMBL519863 | — | — | 1 | 7.89 |
| CHEMBL484163 | — | — | 1 | 7.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL520345 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL483543 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL484929 | — | Ki | = | 0.82 | nM | 9.09 |
| CHEMBL201602 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL482742 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL111 | RIMONABANT | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL485538 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL482741 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL485013 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL482985 | — | Ki | = | 9.8 | nM | 8.01 |
| CHEMBL518982 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL519863 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL484163 | — | Ki | = | 25.0 | nM | 7.60 |