Assay Detail
Binding
CHEMBL832679
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Concentration required to inhibit metabotropic glutamate receptor 2 activity of rat expressed in CHO cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Metabotropic glutamate receptor 2 (CHEMBL2851) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis, in vitro pharmacology, structure-activity relationships, and pharmacokinetics of 3-alkoxy-2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent and selective group II metabotropic glutamate receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.26 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL186453 | — | — | 1 | 7.70 |
| CHEMBL185210 | — | — | 1 | 7.64 |
| CHEMBL432038 | — | — | 1 | 7.63 |
| CHEMBL434536 | — | — | 1 | 7.61 |
| CHEMBL189814 | — | — | 1 | 7.54 |
| CHEMBL186630 | — | — | 1 | 7.39 |
| CHEMBL186214 | — | — | 1 | 6.88 |
| CHEMBL183956 | — | — | 1 | 6.64 |
| CHEMBL185822 | — | — | 1 | 6.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL186453 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL185210 | — | IC50 | = | 22.7 | nM | 7.64 |
| CHEMBL432038 | — | IC50 | = | 23.2 | nM | 7.63 |
| CHEMBL434536 | — | IC50 | = | 24.4 | nM | 7.61 |
| CHEMBL189814 | — | IC50 | = | 29.1 | nM | 7.54 |
| CHEMBL186630 | — | IC50 | = | 40.8 | nM | 7.39 |
| CHEMBL186214 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL183956 | — | IC50 | = | 229.0 | nM | 6.64 |
| CHEMBL185822 | — | IC50 | = | 476.0 | nM | 6.32 |