Assay Detail
Binding
CHEMBL983967
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to CB2 receptor
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
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 | 5.63 | 6.79 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL519863 | — | — | 1 | 6.79 |
| CHEMBL111 | RIMONABANT | 4.0 | 1 | 5.80 |
| CHEMBL482985 | — | — | 1 | 5.75 |
| CHEMBL518982 | — | — | 1 | 5.17 |
| CHEMBL484163 | — | — | 1 | 4.63 |
| CHEMBL201602 | — | — | 1 | - |
| CHEMBL485013 | — | — | 1 | - |
| CHEMBL485538 | — | — | 1 | - |
| CHEMBL483543 | — | — | 1 | - |
| CHEMBL482741 | — | — | 1 | - |
| CHEMBL482742 | — | — | 1 | - |
| CHEMBL484929 | — | — | 1 | - |
| CHEMBL520345 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL519863 | — | Ki | = | 162.0 | nM | 6.79 |
| CHEMBL111 | RIMONABANT | Ki | = | 1569.0 | nM | 5.80 |
| CHEMBL482985 | — | Ki | = | 1780.0 | nM | 5.75 |
| CHEMBL518982 | — | Ki | = | 6810.0 | nM | 5.17 |
| CHEMBL484163 | — | Ki | = | 23440.0 | nM | 4.63 |
| CHEMBL201602 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL485013 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL485538 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL483543 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL482741 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL482742 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL484929 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL520345 | — | Ki | > | 10000.0 | nM | - |