Assay Detail
Functional
CHEMBL2215923
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Agonist activity at human mGLuR2 expressed in CHO cell membrane assessed as [32S]GTPgammaS after 30 mins by scintillation counting
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis, evaluation, and radiolabeling of new potent positive allosteric modulators of the metabotropic glutamate receptor 2 as potential tracers for positron emission tomography imaging.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 14 | 7.83 | 8.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2206449 | — | — | 1 | 8.39 |
| CHEMBL2206442 | — | — | 1 | 8.22 |
| CHEMBL2206447 | — | — | 1 | 8.16 |
| CHEMBL2206445 | — | — | 1 | 8.12 |
| CHEMBL2206441 | — | — | 1 | 8.09 |
| CHEMBL2206446 | — | — | 1 | 8.03 |
| CHEMBL2206439 | — | — | 1 | 7.98 |
| CHEMBL2206448 | — | — | 1 | 7.96 |
| CHEMBL2206440 | — | — | 1 | 7.70 |
| CHEMBL2206444 | — | — | 1 | 7.58 |
| CHEMBL2206438 | — | — | 1 | 7.51 |
| CHEMBL2206443 | — | — | 1 | 7.43 |
| CHEMBL2179333 | — | — | 1 | 7.25 |
| CHEMBL2206437 | — | — | 1 | 7.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2206449 | — | EC50 | = | 4.1 | nM | 8.39 |
| CHEMBL2206442 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2206447 | — | EC50 | = | 6.9 | nM | 8.16 |
| CHEMBL2206445 | — | EC50 | = | 7.5 | nM | 8.12 |
| CHEMBL2206441 | — | EC50 | = | 8.2 | nM | 8.09 |
| CHEMBL2206446 | — | EC50 | = | 9.3 | nM | 8.03 |
| CHEMBL2206439 | — | EC50 | = | 10.5 | nM | 7.98 |
| CHEMBL2206448 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2206440 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2206444 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2206438 | — | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL2206443 | — | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL2179333 | — | EC50 | = | 56.23 | nM | 7.25 |
| CHEMBL2206437 | — | EC50 | = | 61.66 | nM | 7.21 |