Assay Detail
Functional
CHEMBL718223
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Agonist activity against Metabotropic glutamate receptor 2 expressed in CHO cells was evaluated by measuring forskolin-induced cyclic AMP formation
15
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Metabotropic glutamate receptor 2 (CHEMBL2851) ↗| 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 |
|---|---|---|---|
| EC50 | 15 | 7.29 | 9.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL121053 | — | — | 3 | 9.24 |
| CHEMBL333519 | — | — | 3 | 7.78 |
| CHEMBL8759 | EGLUMETAD | 2.0 | 1 | 7.74 |
| CHEMBL144747 | — | — | 1 | 7.68 |
| CHEMBL334014 | — | — | 3 | 7.53 |
| CHEMBL144678 | — | — | 1 | 5.35 |
| CHEMBL356502 | — | — | 1 | - |
| CHEMBL341888 | — | — | 1 | - |
| CHEMBL144201 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL121053 | — | EC50 | = | 0.57 | nM | 9.24 |
| CHEMBL121053 | — | EC50 | = | 1.26 | nM | 8.90 |
| CHEMBL333519 | — | EC50 | = | 16.6 | nM | 7.78 |
| CHEMBL8759 | EGLUMETAD | EC50 | = | 18.3 | nM | 7.74 |
| CHEMBL144747 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL334014 | — | EC50 | = | 29.4 | nM | 7.53 |
| CHEMBL333519 | — | EC50 | = | 34.2 | nM | 7.47 |
| CHEMBL334014 | — | EC50 | = | 64.7 | nM | 7.19 |
| CHEMBL121053 | — | EC50 | = | 94.7 | nM | 7.02 |
| CHEMBL333519 | — | EC50 | = | 1120.0 | nM | 5.95 |
| CHEMBL334014 | — | EC50 | = | 2640.0 | nM | 5.58 |
| CHEMBL144678 | — | EC50 | = | 4490.0 | nM | 5.35 |
| CHEMBL356502 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL341888 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL144201 | — | EC50 | > | 100000.0 | nM | - |