Assay Detail
Binding
CHEMBL713034
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Tested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells using [3H]-7 as radioligand
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Metabotropic glutamate receptor 3 (CHEMBL3067) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 7.73 | 8.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL121053 | — | — | 1 | 8.44 |
| CHEMBL144151 | — | — | 1 | 8.39 |
| CHEMBL333519 | — | — | 1 | 7.38 |
| CHEMBL8759 | EGLUMETAD | 2.0 | 1 | 7.27 |
| CHEMBL334014 | — | — | 1 | 7.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL121053 | — | Ki | = | 3.62 | nM | 8.44 |
| CHEMBL144151 | — | Ki | = | 4.11 | nM | 8.39 |
| CHEMBL333519 | — | Ki | = | 41.7 | nM | 7.38 |
| CHEMBL8759 | EGLUMETAD | Ki | = | 53.5 | nM | 7.27 |
| CHEMBL334014 | — | Ki | = | 65.9 | nM | 7.18 |