Assay Detail
Binding
CHEMBL680165
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory activity for Group II Metabotropic glutamate receptor in rat forebrain membranes by using [3H]glutamate radioligand
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Forebrain |
| Subcellular | Membrane |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
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. 1. Effects of alkyl, arylalkyl, and diarylalkyl substitution.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 6.12 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL144151 | — | — | 1 | 8.00 |
| CHEMBL333311 | — | — | 1 | 7.72 |
| CHEMBL2112586 | — | — | 1 | 6.70 |
| CHEMBL325688 | — | — | 1 | 6.70 |
| CHEMBL2112581 | — | — | 1 | 6.68 |
| CHEMBL118141 | — | — | 1 | 6.64 |
| CHEMBL2112574 | — | — | 1 | 6.64 |
| CHEMBL2112583 | — | — | 1 | 6.62 |
| CHEMBL2311086 | — | — | 1 | 6.62 |
| CHEMBL2112580 | — | — | 1 | 6.55 |
| CHEMBL2112582 | — | — | 1 | 6.50 |
| CHEMBL119251 | — | — | 1 | 6.42 |
| CHEMBL119635 | — | — | 1 | 6.33 |
| CHEMBL332519 | — | — | 1 | 6.26 |
| CHEMBL333545 | — | — | 1 | 6.24 |
| CHEMBL2112584 | — | — | 1 | 6.20 |
| CHEMBL121574 | — | — | 1 | 6.20 |
| CHEMBL331753 | — | — | 1 | 6.16 |
| CHEMBL119619 | — | — | 1 | 6.07 |
| CHEMBL119447 | — | — | 1 | 5.96 |
| CHEMBL118541 | — | — | 1 | 5.85 |
| CHEMBL118837 | — | — | 1 | 5.85 |
| CHEMBL118623 | — | — | 1 | 5.77 |
| CHEMBL118913 | — | — | 1 | 5.75 |
| CHEMBL116825 | — | — | 1 | 5.68 |
| CHEMBL2112579 | — | — | 1 | 5.66 |
| CHEMBL2112585 | — | — | 1 | 5.64 |
| CHEMBL120565 | — | — | 1 | 5.55 |
| CHEMBL324264 | — | — | 1 | 5.21 |
| CHEMBL332822 | — | — | 1 | 5.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL144151 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL333311 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL325688 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2112586 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2112581 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL118141 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL2112574 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL2112583 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL2311086 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL2112580 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL2112582 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL119251 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL119635 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL332519 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL333545 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL2112584 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL121574 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL331753 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL119619 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL119447 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL118837 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL118541 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL118623 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL118913 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL116825 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL2112579 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL2112585 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL120565 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL324264 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL332822 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL333487 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL325498 | — | IC50 | = | 11200.0 | nM | 4.95 |
| CHEMBL332141 | — | IC50 | = | 29500.0 | nM | 4.53 |
| CHEMBL430697 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL325500 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL118993 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL323610 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL325497 | — | IC50 | > | 10000.0 | nM | - |