Assay Detail
Binding
CHEMBL983966
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to CB1 receptor
17
Total Activities
17
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 | 17 | 8.39 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL201602 | — | — | 1 | 9.22 |
| CHEMBL483543 | — | — | 1 | 9.15 |
| CHEMBL484929 | — | — | 1 | 9.00 |
| CHEMBL482741 | — | — | 1 | 8.89 |
| CHEMBL520345 | — | — | 1 | 8.85 |
| CHEMBL485538 | — | — | 1 | 8.77 |
| CHEMBL111 | RIMONABANT | 4.0 | 1 | 8.74 |
| CHEMBL482742 | — | — | 1 | 8.72 |
| CHEMBL482985 | — | — | 1 | 8.60 |
| CHEMBL485013 | — | — | 1 | 8.60 |
| CHEMBL518982 | — | — | 1 | 8.33 |
| CHEMBL484163 | — | — | 1 | 8.33 |
| CHEMBL519863 | — | — | 1 | 7.96 |
| CHEMBL482986 | — | — | 1 | 7.62 |
| CHEMBL483544 | — | — | 1 | 7.52 |
| CHEMBL521173 | — | — | 1 | 7.21 |
| CHEMBL520315 | — | — | 1 | 7.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL201602 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL483543 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL484929 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL482741 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL520345 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL485538 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL111 | RIMONABANT | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL482742 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL482985 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL485013 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL518982 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL484163 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL519863 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL482986 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL483544 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL521173 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL520315 | — | Ki | = | 83.0 | nM | 7.08 |