Assay Detail
Functional
CHEMBL966989
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human CB1 receptor by [35S]GTPgammaS binding assay
10
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and labeling of high-affinity 3,4-diarylpyrazolines as candidate radioligands for in vivo imaging of cannabinoid subtype-1 (CB1) receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.98 | 8.72 |
| Ki | 5 | 8.75 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL460796 | — | — | 2 | 9.52 |
| CHEMBL111 | RIMONABANT | 4.0 | 2 | 9.40 |
| CHEMBL459730 | — | — | 2 | 9.30 |
| CHEMBL461855 | — | — | 2 | 7.77 |
| CHEMBL460797 | — | — | 2 | 7.76 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL460796 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL111 | RIMONABANT | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL459730 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL460796 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL111 | RIMONABANT | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL459730 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL461855 | — | Ki | = | 16.9 | nM | 7.77 |
| CHEMBL460797 | — | Ki | = | 17.4 | nM | 7.76 |
| CHEMBL461855 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL460797 | — | IC50 | = | 103.5 | nM | 6.99 |