Assay Detail
Binding
CHEMBL4724926
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Inverse agonist activity at cannabinoid CB2 receptor in human U2OS cells assessed as induction of beta-arrestin recruitment using CCF4/AM as substrate preincubated for 5 hrs followed by substrate addition and measured after 2 hrs by Tango assay
12
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U2OS |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and biological evaluation of a ring analogs of the selective CB2 inverse agonist SMM-189.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 11 | 5.61 | 6.81 |
| pEC50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL460545 | — | — | 1 | 6.81 |
| CHEMBL381791 | — | — | 1 | 5.93 |
| CHEMBL4793741 | — | — | 1 | 5.89 |
| CHEMBL4777102 | — | — | 1 | 5.85 |
| CHEMBL4749825 | — | — | 1 | 5.46 |
| CHEMBL4756251 | — | — | 1 | 5.22 |
| CHEMBL4759054 | — | — | 1 | 5.21 |
| CHEMBL4796513 | — | — | 1 | 5.07 |
| CHEMBL4764314 | — | — | 1 | 5.05 |
| CHEMBL4776518 | — | — | 1 | - |
| CHEMBL4752997 | — | — | 1 | - |
| CHEMBL3907723 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL460545 | — | EC50 | = | 154.88 | nM | 6.81 |
| CHEMBL381791 | — | EC50 | = | 1174.9 | nM | 5.93 |
| CHEMBL4793741 | — | EC50 | = | 1288.25 | nM | 5.89 |
| CHEMBL4777102 | — | EC50 | = | 1412.54 | nM | 5.85 |
| CHEMBL4749825 | — | EC50 | = | 3467.37 | nM | 5.46 |
| CHEMBL4756251 | — | EC50 | = | 6025.6 | nM | 5.22 |
| CHEMBL4759054 | — | EC50 | = | 6165.95 | nM | 5.21 |
| CHEMBL4796513 | — | EC50 | = | 8511.38 | nM | 5.07 |
| CHEMBL4764314 | — | EC50 | = | 8912.51 | nM | 5.05 |
| CHEMBL4776518 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4752997 | — | pEC50 | - | — | - | |
| CHEMBL3907723 | — | EC50 | > | 10000.0 | nM | - |