Assay Detail
Functional
CHEMBL1108616
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Inverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins
4
Total Activities
3
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of benzhydrylpiperazine derivatives as CB1 receptor inverse agonists via privileged structure-based approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 2 | 9.51 | 9.96 |
| Activity | 1 | - | - |
| IC50 | 1 | 9.89 | 9.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL111 | RIMONABANT | 4.0 | 1 | 9.96 |
| CHEMBL559612 | CP-55940 | — | 1 | 9.89 |
| CHEMBL1093735 | — | — | 2 | 9.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL111 | RIMONABANT | EC50 | = | 0.11 | nM | 9.96 |
| CHEMBL559612 | CP-55940 | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL1093735 | — | EC50 | = | 0.87 | nM | 9.06 |
| CHEMBL1093735 | — | Activity | - | — | - |