Assay Detail
Functional
CHEMBL4724914
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inverse agonist activity at human recombinant cannabinoid CB2 receptor expressed in HEK cells transfected with CNG assessed as increase in cAMP level measured up to 1 hr by ACTOne membrane potential dye based assay
21
Total Activities
21
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK |
| 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 | 13 | 6.26 | 7.41 |
| pEC50 | 7 | - | - |
| Emax | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4796513 | — | — | 1 | 7.41 |
| CHEMBL4776518 | — | — | 1 | 6.85 |
| CHEMBL460545 | — | — | 1 | 6.81 |
| CHEMBL4759054 | — | — | 1 | 6.70 |
| CHEMBL4749825 | — | — | 1 | 6.62 |
| CHEMBL4756251 | — | — | 1 | 6.44 |
| CHEMBL4777102 | — | — | 1 | 6.43 |
| CHEMBL4793741 | — | — | 1 | 6.17 |
| CHEMBL3907723 | — | — | 1 | 5.78 |
| CHEMBL4764314 | — | — | 1 | 5.77 |
| CHEMBL4741155 | — | — | 1 | 5.56 |
| CHEMBL4752997 | — | — | 1 | 5.55 |
| CHEMBL4747418 | — | — | 1 | 5.31 |
| CHEMBL4752097 | — | — | 1 | - |
| CHEMBL4785051 | — | — | 1 | - |
| CHEMBL4792566 | — | — | 1 | - |
| CHEMBL4750515 | — | — | 1 | - |
| CHEMBL4740459 | — | — | 1 | - |
| CHEMBL4755496 | — | — | 1 | - |
| CHEMBL4741108 | — | — | 1 | - |
| CHEMBL4786835 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4796513 | — | EC50 | = | 38.9 | nM | 7.41 |
| CHEMBL4776518 | — | EC50 | = | 141.25 | nM | 6.85 |
| CHEMBL460545 | — | EC50 | = | 154.88 | nM | 6.81 |
| CHEMBL4759054 | — | EC50 | = | 199.53 | nM | 6.70 |
| CHEMBL4749825 | — | EC50 | = | 239.88 | nM | 6.62 |
| CHEMBL4756251 | — | EC50 | = | 363.08 | nM | 6.44 |
| CHEMBL4777102 | — | EC50 | = | 371.54 | nM | 6.43 |
| CHEMBL4793741 | — | EC50 | = | 676.08 | nM | 6.17 |
| CHEMBL3907723 | — | EC50 | = | 1659.59 | nM | 5.78 |
| CHEMBL4764314 | — | EC50 | = | 1698.24 | nM | 5.77 |
| CHEMBL4741155 | — | EC50 | = | 2754.23 | nM | 5.56 |
| CHEMBL4752997 | — | EC50 | = | 2818.38 | nM | 5.55 |
| CHEMBL4747418 | — | EC50 | = | 4897.79 | nM | 5.31 |
| CHEMBL4752097 | — | pEC50 | - | — | - | |
| CHEMBL4785051 | — | Emax | - | — | - | |
| CHEMBL4792566 | — | pEC50 | - | — | - | |
| CHEMBL4750515 | — | pEC50 | - | — | - | |
| CHEMBL4740459 | — | pEC50 | - | — | - | |
| CHEMBL4755496 | — | pEC50 | - | — | - | |
| CHEMBL4741108 | — | pEC50 | - | — | - | |
| CHEMBL4786835 | — | pEC50 | - | — | - |