Assay Detail
Binding
CHEMBL3857710
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-CP55,940 from human CB2 receptor transfected in CHO cell membranes after 60 mins by liquid scintillation spectrometry
16
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
A critical review of both the synthesis approach and the receptor profile of the 8-chloro-1-(2',4'-dichlorophenyl)-N-piperidin-1-yl-1,4,5,6-tetrahydrobenzo[6,7]cyclohepta[1,2-c]pyrazole-3-carboxamide and analogue derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 7.37 | 8.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3984538 | — | — | 1 | 8.02 |
| CHEMBL559612 | CP-55940 | — | 1 | 8.01 |
| CHEMBL3889602 | — | — | 1 | 7.88 |
| CHEMBL3914728 | — | — | 1 | 7.87 |
| CHEMBL225622 | — | — | 1 | 7.75 |
| CHEMBL3978981 | — | — | 1 | 7.71 |
| CHEMBL3927357 | — | — | 1 | 7.62 |
| CHEMBL223278 | — | — | 1 | 7.55 |
| CHEMBL3917142 | — | — | 1 | 7.50 |
| CHEMBL3924830 | — | — | 1 | 7.29 |
| CHEMBL3949933 | — | — | 1 | 7.28 |
| CHEMBL376700 | — | — | 2 | 7.25 |
| CHEMBL374933 | — | — | 1 | 6.74 |
| CHEMBL3895744 | — | — | 1 | 6.49 |
| CHEMBL111 | RIMONABANT | 4.0 | 1 | 5.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3984538 | — | Ki | = | 9.5 | nM | 8.02 |
| CHEMBL559612 | CP-55940 | Ki | = | 9.73 | nM | 8.01 |
| CHEMBL3889602 | — | Ki | = | 13.3 | nM | 7.88 |
| CHEMBL3914728 | — | Ki | = | 13.6 | nM | 7.87 |
| CHEMBL225622 | — | Ki | = | 17.9 | nM | 7.75 |
| CHEMBL3978981 | — | Ki | = | 19.5 | nM | 7.71 |
| CHEMBL3927357 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL223278 | — | Ki | = | 28.1 | nM | 7.55 |
| CHEMBL3917142 | — | Ki | = | 31.8 | nM | 7.50 |
| CHEMBL3924830 | — | Ki | = | 51.1 | nM | 7.29 |
| CHEMBL3949933 | — | Ki | = | 52.1 | nM | 7.28 |
| CHEMBL376700 | — | Ki | = | 55.7 | nM | 7.25 |
| CHEMBL376700 | — | Ki | = | 85.2 | nM | 7.07 |
| CHEMBL374933 | — | Ki | = | 182.0 | nM | 6.74 |
| CHEMBL3895744 | — | Ki | = | 325.0 | nM | 6.49 |
| CHEMBL111 | RIMONABANT | Ki | = | 1400.0 | nM | 5.85 |