Assay Detail
Binding
CHEMBL820029
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Inhibition of 10 uM 1S, 3R-ACPD stimulated GTP gamma 35S binding to rat mGluR2 expressed in CHO cells
12
Total Activities
12
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 of heterocyclic enol ethers and their use as group 2 metabotropic glutamate receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 5.73 | 6.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL305406 | — | — | 1 | 6.96 |
| CHEMBL69461 | — | — | 1 | 6.33 |
| CHEMBL303193 | — | — | 1 | 6.24 |
| CHEMBL69970 | — | — | 1 | 5.98 |
| CHEMBL68739 | — | — | 1 | 5.92 |
| CHEMBL70026 | — | — | 1 | 5.86 |
| CHEMBL70025 | — | — | 1 | 5.70 |
| CHEMBL305799 | — | — | 1 | 5.59 |
| CHEMBL69204 | — | — | 1 | 5.57 |
| CHEMBL66701 | — | — | 1 | 5.50 |
| CHEMBL304285 | — | — | 1 | 4.94 |
| CHEMBL69869 | — | — | 1 | 4.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL305406 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL69461 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL303193 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL69970 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL68739 | — | IC50 | = | 1210.0 | nM | 5.92 |
| CHEMBL70026 | — | IC50 | = | 1380.0 | nM | 5.86 |
| CHEMBL70025 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL305799 | — | IC50 | = | 2550.0 | nM | 5.59 |
| CHEMBL69204 | — | IC50 | = | 2680.0 | nM | 5.57 |
| CHEMBL66701 | — | IC50 | = | 3160.0 | nM | 5.50 |
| CHEMBL304285 | — | IC50 | = | 11500.0 | nM | 4.94 |
| CHEMBL69869 | — | IC50 | = | 75000.0 | nM | 4.12 |