Assay Detail
Binding
CHEMBL940410
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]CP-55940 from CB1 receptor in Sprague-Dawley rat cerebellum by liquid scintillation spectrometry
78
Total Activities
78
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebellum |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Biarylpyrazolyl oxadiazole as potent, selective, orally bioavailable cannabinoid-1 receptor antagonists for the treatment of obesity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 78 | 7.79 | 9.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL501851 | — | — | 1 | 9.24 |
| CHEMBL220360 | TARANABANT | 3.0 | 1 | 9.07 |
| CHEMBL487381 | — | — | 1 | 9.03 |
| CHEMBL487384 | — | — | 1 | 9.02 |
| CHEMBL468425 | — | — | 1 | 8.96 |
| CHEMBL509751 | — | — | 1 | 8.87 |
| CHEMBL530339 | — | — | 1 | 8.82 |
| CHEMBL488786 | — | — | 1 | 8.70 |
| CHEMBL505814 | — | — | 1 | 8.66 |
| CHEMBL520551 | — | — | 1 | 8.63 |
| CHEMBL487178 | — | — | 1 | 8.56 |
| CHEMBL487380 | — | — | 1 | 8.55 |
| CHEMBL487586 | — | — | 1 | 8.47 |
| CHEMBL111 | RIMONABANT | 4.0 | 1 | 8.34 |
| CHEMBL521513 | — | — | 1 | 8.32 |
| CHEMBL486154 | — | — | 1 | 8.32 |
| CHEMBL487172 | — | — | 1 | 8.21 |
| CHEMBL486756 | — | — | 1 | 8.18 |
| CHEMBL487158 | — | — | 1 | 8.12 |
| CHEMBL487582 | — | — | 1 | 8.12 |
| CHEMBL487773 | — | — | 1 | 8.07 |
| CHEMBL485732 | — | — | 1 | 8.07 |
| CHEMBL485744 | — | — | 1 | 8.06 |
| CHEMBL487162 | — | — | 1 | 8.05 |
| CHEMBL487161 | — | — | 1 | 8.00 |
| CHEMBL520401 | — | — | 1 | 7.98 |
| CHEMBL487974 | — | — | 1 | 7.98 |
| CHEMBL486956 | — | — | 1 | 7.96 |
| CHEMBL486549 | — | — | 1 | 7.96 |
| CHEMBL485733 | — | — | 1 | 7.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL501851 | — | IC50 | = | 0.57 | nM | 9.24 |
| CHEMBL220360 | TARANABANT | IC50 | = | 0.86 | nM | 9.07 |
| CHEMBL487381 | — | IC50 | = | 0.93 | nM | 9.03 |
| CHEMBL487384 | — | IC50 | = | 0.96 | nM | 9.02 |
| CHEMBL468425 | — | IC50 | = | 1.09 | nM | 8.96 |
| CHEMBL509751 | — | IC50 | = | 1.34 | nM | 8.87 |
| CHEMBL530339 | — | IC50 | = | 1.51 | nM | 8.82 |
| CHEMBL488786 | — | IC50 | = | 1.98 | nM | 8.70 |
| CHEMBL505814 | — | IC50 | = | 2.21 | nM | 8.66 |
| CHEMBL520551 | — | IC50 | = | 2.36 | nM | 8.63 |
| CHEMBL487178 | — | IC50 | = | 2.75 | nM | 8.56 |
| CHEMBL487380 | — | IC50 | = | 2.81 | nM | 8.55 |
| CHEMBL487586 | — | IC50 | = | 3.37 | nM | 8.47 |
| CHEMBL111 | RIMONABANT | IC50 | = | 4.53 | nM | 8.34 |
| CHEMBL486154 | — | IC50 | = | 4.83 | nM | 8.32 |
| CHEMBL521513 | — | IC50 | = | 4.78 | nM | 8.32 |
| CHEMBL487172 | — | IC50 | = | 6.12 | nM | 8.21 |
| CHEMBL486756 | — | IC50 | = | 6.57 | nM | 8.18 |
| CHEMBL487158 | — | IC50 | = | 7.59 | nM | 8.12 |
| CHEMBL487582 | — | IC50 | = | 7.64 | nM | 8.12 |
| CHEMBL487773 | — | IC50 | = | 8.53 | nM | 8.07 |
| CHEMBL485732 | — | IC50 | = | 8.42 | nM | 8.07 |
| CHEMBL485744 | — | IC50 | = | 8.61 | nM | 8.06 |
| CHEMBL487162 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL487161 | — | IC50 | = | 10.1 | nM | 8.00 |
| CHEMBL520401 | — | IC50 | = | 10.4 | nM | 7.98 |
| CHEMBL487974 | — | IC50 | = | 10.4 | nM | 7.98 |
| CHEMBL486956 | — | IC50 | = | 10.9 | nM | 7.96 |
| CHEMBL486549 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL485733 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL487585 | — | IC50 | = | 12.8 | nM | 7.89 |
| CHEMBL520884 | — | IC50 | = | 13.1 | nM | 7.88 |
| CHEMBL486562 | — | IC50 | = | 14.1 | nM | 7.85 |
| CHEMBL486548 | — | IC50 | = | 14.6 | nM | 7.84 |
| CHEMBL485753 | — | IC50 | = | 14.7 | nM | 7.83 |
| CHEMBL487772 | — | IC50 | = | 14.7 | nM | 7.83 |
| CHEMBL486957 | — | IC50 | = | 15.1 | nM | 7.82 |
| CHEMBL485754 | — | IC50 | = | 15.6 | nM | 7.81 |
| CHEMBL519214 | — | IC50 | = | 15.4 | nM | 7.81 |
| CHEMBL521216 | — | IC50 | = | 16.9 | nM | 7.77 |
| CHEMBL487163 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL520729 | — | IC50 | = | 18.7 | nM | 7.73 |
| CHEMBL519400 | — | IC50 | = | 19.2 | nM | 7.72 |
| CHEMBL521382 | — | IC50 | = | 20.5 | nM | 7.69 |
| CHEMBL487171 | — | IC50 | = | 20.7 | nM | 7.68 |
| CHEMBL487170 | — | IC50 | = | 22.4 | nM | 7.65 |
| CHEMBL519875 | — | IC50 | = | 22.6 | nM | 7.65 |
| CHEMBL485735 | — | IC50 | = | 22.7 | nM | 7.64 |
| CHEMBL519731 | — | IC50 | = | 24.4 | nM | 7.61 |
| CHEMBL488595 | — | IC50 | = | 25.0 | nM | 7.60 |