Assay Detail
Binding
CHEMBL910519
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]LY341495 from human recombinant mGluR2 in RGT cells
6
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 |
|---|---|---|---|
| Ki | 6 | 7.31 | 8.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL218710 | — | — | 2 | 8.36 |
| CHEMBL275079 | LY-379268 | — | 1 | 7.85 |
| CHEMBL8839 | LY-389795 | — | 1 | 7.39 |
| CHEMBL8759 | EGLUMETAD | 2.0 | 1 | 7.13 |
| CHEMBL375611 | LY404039 | 1.0 | 1 | 6.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL218710 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL275079 | LY-379268 | Ki | = | 14.1 | nM | 7.85 |
| CHEMBL8839 | LY-389795 | Ki | = | 40.6 | nM | 7.39 |
| CHEMBL8759 | EGLUMETAD | Ki | = | 74.9 | nM | 7.13 |
| CHEMBL375611 | LY404039 | Ki | = | 149.0 | nM | 6.83 |
| CHEMBL218710 | — | Ki | = | 508.0 | nM | 6.29 |