Assay Detail
Binding
CHEMBL717237
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Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.
7
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | RGT |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists for group II metabotropic glutamate receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 7.46 | 8.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL8839 | LY-389795 | — | 3 | 8.33 |
| CHEMBL275079 | LY-379268 | — | 3 | 8.24 |
| CHEMBL8759 | EGLUMETAD | 2.0 | 1 | 7.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL8839 | LY-389795 | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL275079 | LY-379268 | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL8839 | LY-389795 | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL275079 | LY-379268 | Ki | = | 14.3 | nM | 7.84 |
| CHEMBL8759 | EGLUMETAD | Ki | = | 93.3 | nM | 7.03 |
| CHEMBL8839 | LY-389795 | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL275079 | LY-379268 | Ki | = | 1040.0 | nM | 5.98 |