Assay Detail
Binding
CHEMBL914893
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]CP-55940 from CB1 receptor in CD1 mouse brain
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Tricyclic pyrazoles. 3. Synthesis, biological evaluation, and molecular modeling of analogues of the cannabinoid antagonist 8-chloro-1-(2',4'-dichlorophenyl)-N-piperidin-1-yl-1,4,5,6-tetrahydrobenzo[6,7]cyclohepta[1,2-c]pyrazole-3-carboxamide.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 9.22 | 12.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL376700 | — | — | 1 | 12.46 |
| CHEMBL223278 | — | — | 1 | 12.00 |
| CHEMBL374933 | — | — | 1 | 11.40 |
| CHEMBL224609 | — | — | 1 | 11.28 |
| CHEMBL438782 | — | — | 1 | 11.10 |
| CHEMBL387112 | — | — | 1 | 10.89 |
| CHEMBL225415 | — | — | 1 | 9.96 |
| CHEMBL225622 | — | — | 1 | 9.52 |
| CHEMBL111 | RIMONABANT | 4.0 | 1 | 8.74 |
| CHEMBL224847 | — | — | 1 | 8.60 |
| CHEMBL225377 | — | — | 1 | 8.36 |
| CHEMBL224114 | — | — | 1 | 8.24 |
| CHEMBL541216 | — | — | 1 | 8.01 |
| CHEMBL389203 | — | — | 1 | 7.83 |
| CHEMBL389693 | — | — | 1 | 7.59 |
| CHEMBL224053 | — | — | 1 | 7.51 |
| CHEMBL389669 | — | — | 1 | 6.78 |
| CHEMBL218957 | — | — | 1 | 5.69 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL376700 | — | Ki | = | 0.00035 | nM | 12.46 |
| CHEMBL223278 | — | Ki | = | 0.001 | nM | 12.00 |
| CHEMBL374933 | — | Ki | = | 0.004 | nM | 11.40 |
| CHEMBL224609 | — | Ki | = | 0.0052 | nM | 11.28 |
| CHEMBL438782 | — | Ki | = | 0.008 | nM | 11.10 |
| CHEMBL387112 | — | Ki | = | 0.013 | nM | 10.89 |
| CHEMBL225415 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL225622 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL111 | RIMONABANT | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL224847 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL225377 | — | Ki | = | 4.35 | nM | 8.36 |
| CHEMBL224114 | — | Ki | = | 5.74 | nM | 8.24 |
| CHEMBL541216 | — | Ki | = | 9.84 | nM | 8.01 |
| CHEMBL389203 | — | Ki | = | 14.8 | nM | 7.83 |
| CHEMBL389693 | — | Ki | = | 25.83 | nM | 7.59 |
| CHEMBL224053 | — | Ki | = | 31.2 | nM | 7.51 |
| CHEMBL389669 | — | Ki | = | 168.0 | nM | 6.78 |
| CHEMBL218957 | — | Ki | = | 2050.0 | nM | 5.69 |