Assay Detail
Functional
CHEMBL910533
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Agonist activity at human mGluR2 assessed as effect on cAMP production in RGT cells
6
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | RGT |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Synthesis and metabotropic glutamate receptor activity of S-oxidized variants of (-)-4-amino-2-thiabicyclo-[3.1.0]hexane-4,6-dicarboxylate: identification of potent, selective, and orally bioavailable agonists for mGlu2/3 receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 6 | 8.39 | 10.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL218710 | — | — | 2 | 10.05 |
| CHEMBL275079 | LY-379268 | — | 1 | 8.57 |
| CHEMBL8839 | LY-389795 | — | 1 | 8.41 |
| CHEMBL8759 | EGLUMETAD | 2.0 | 1 | 7.96 |
| CHEMBL375611 | LY404039 | 1.0 | 1 | 7.63 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL218710 | — | EC50 | = | 0.089 | nM | 10.05 |
| CHEMBL275079 | LY-379268 | EC50 | = | 2.7 | nM | 8.57 |
| CHEMBL8839 | LY-389795 | EC50 | = | 3.9 | nM | 8.41 |
| CHEMBL8759 | EGLUMETAD | EC50 | = | 11.1 | nM | 7.96 |
| CHEMBL218710 | — | EC50 | = | 18.1 | nM | 7.74 |
| CHEMBL375611 | LY404039 | EC50 | = | 23.4 | nM | 7.63 |