Assay Detail
Binding
CHEMBL940411
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHOK1 cells by liquid scintillation spectrometry
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| 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 | 39 | 5.95 | 6.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL487384 | — | — | 1 | 6.62 |
| CHEMBL519214 | — | — | 1 | 6.43 |
| CHEMBL520729 | — | — | 1 | 6.42 |
| CHEMBL487380 | — | — | 1 | 6.39 |
| CHEMBL487178 | — | — | 1 | 6.29 |
| CHEMBL487172 | — | — | 1 | 6.27 |
| CHEMBL509751 | — | — | 1 | 6.24 |
| CHEMBL487586 | — | — | 1 | 6.17 |
| CHEMBL487582 | — | — | 1 | 6.13 |
| CHEMBL520551 | — | — | 1 | 6.09 |
| CHEMBL486562 | — | — | 1 | 6.03 |
| CHEMBL487381 | — | — | 1 | 6.02 |
| CHEMBL488786 | — | — | 1 | 6.02 |
| CHEMBL521382 | — | — | 1 | 6.01 |
| CHEMBL521216 | — | — | 1 | 5.98 |
| CHEMBL501851 | — | — | 1 | 5.98 |
| CHEMBL485753 | — | — | 1 | 5.95 |
| CHEMBL487585 | — | — | 1 | 5.95 |
| CHEMBL488787 | — | — | 1 | 5.95 |
| CHEMBL220360 | TARANABANT | 3.0 | 1 | 5.93 |
| CHEMBL468425 | — | — | 1 | 5.91 |
| CHEMBL487170 | — | — | 1 | 5.89 |
| CHEMBL487158 | — | — | 1 | 5.85 |
| CHEMBL487171 | — | — | 1 | 5.83 |
| CHEMBL505814 | — | — | 1 | 5.83 |
| CHEMBL485754 | — | — | 1 | 5.78 |
| CHEMBL519875 | — | — | 1 | 5.78 |
| CHEMBL486154 | — | — | 1 | 5.76 |
| CHEMBL530339 | — | — | 1 | 5.76 |
| CHEMBL111 | RIMONABANT | 4.0 | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL487384 | — | IC50 | = | 242.0 | nM | 6.62 |
| CHEMBL519214 | — | IC50 | = | 375.0 | nM | 6.43 |
| CHEMBL520729 | — | IC50 | = | 376.0 | nM | 6.42 |
| CHEMBL487380 | — | IC50 | = | 407.0 | nM | 6.39 |
| CHEMBL487178 | — | IC50 | = | 513.0 | nM | 6.29 |
| CHEMBL487172 | — | IC50 | = | 539.0 | nM | 6.27 |
| CHEMBL509751 | — | IC50 | = | 579.0 | nM | 6.24 |
| CHEMBL487586 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL487582 | — | IC50 | = | 736.0 | nM | 6.13 |
| CHEMBL520551 | — | IC50 | = | 804.0 | nM | 6.09 |
| CHEMBL486562 | — | IC50 | = | 924.0 | nM | 6.03 |
| CHEMBL487381 | — | IC50 | = | 948.0 | nM | 6.02 |
| CHEMBL488786 | — | IC50 | = | 954.0 | nM | 6.02 |
| CHEMBL521382 | — | IC50 | = | 979.0 | nM | 6.01 |
| CHEMBL501851 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL521216 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL485753 | — | IC50 | = | 1120.0 | nM | 5.95 |
| CHEMBL487585 | — | IC50 | = | 1120.0 | nM | 5.95 |
| CHEMBL488787 | — | IC50 | = | 1130.0 | nM | 5.95 |
| CHEMBL220360 | TARANABANT | IC50 | = | 1170.0 | nM | 5.93 |
| CHEMBL468425 | — | IC50 | = | 1240.0 | nM | 5.91 |
| CHEMBL487170 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL487158 | — | IC50 | = | 1410.0 | nM | 5.85 |
| CHEMBL487171 | — | IC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL505814 | — | IC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL485754 | — | IC50 | = | 1670.0 | nM | 5.78 |
| CHEMBL519875 | — | IC50 | = | 1670.0 | nM | 5.78 |
| CHEMBL486154 | — | IC50 | = | 1730.0 | nM | 5.76 |
| CHEMBL530339 | — | IC50 | = | 1750.0 | nM | 5.76 |
| CHEMBL111 | RIMONABANT | IC50 | = | 1760.0 | nM | 5.75 |
| CHEMBL486548 | — | IC50 | = | 1810.0 | nM | 5.74 |
| CHEMBL487161 | — | IC50 | = | 1890.0 | nM | 5.72 |
| CHEMBL519731 | — | IC50 | = | 2040.0 | nM | 5.69 |
| CHEMBL486756 | — | IC50 | = | 2330.0 | nM | 5.63 |
| CHEMBL487163 | — | IC50 | = | 2820.0 | nM | 5.55 |
| CHEMBL521042 | — | IC50 | = | 3320.0 | nM | 5.48 |
| CHEMBL487377 | — | IC50 | = | 5910.0 | nM | 5.23 |
| CHEMBL487162 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL520542 | — | IC50 | > | 10000.0 | nM | - |