Assay Detail
Functional
CHEMBL717203
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 2
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | RGT |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
2-substituted (2SR)-2-amino-2-((1SR,2SR)-2-carboxycycloprop-1-yl)glycines as potent and selective antagonists of group II metabotropic glutamate receptors. 2. Effects of aromatic substitution, pharmacological characterization, and bioavailability.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.47 | 7.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL432038 | — | — | 1 | 7.64 |
| CHEMBL333771 | — | — | 1 | 6.75 |
| CHEMBL124501 | — | — | 1 | 6.75 |
| CHEMBL338282 | — | — | 1 | 6.75 |
| CHEMBL2111822 | — | — | 1 | 6.72 |
| CHEMBL124078 | — | — | 1 | 6.66 |
| CHEMBL123847 | — | — | 1 | 6.66 |
| CHEMBL341457 | — | — | 1 | 6.37 |
| CHEMBL2112582 | — | — | 1 | 6.07 |
| CHEMBL124483 | — | — | 1 | 6.00 |
| CHEMBL2112634 | — | — | 1 | 5.75 |
| CHEMBL123842 | — | — | 1 | 5.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL432038 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL333771 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL124501 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL338282 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL2111822 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL124078 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL123847 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL341457 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL2112582 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL124483 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2112634 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL123842 | — | IC50 | = | 3100.0 | nM | 5.51 |