Assay Detail
Binding
CHEMBL2184422
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Positive allosteric modulation activity at rat mGlu2R expressed in HEK293 cells co-expressing GIRK channels by thallium flux assay
30
Total Activities
30
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Metabotropic glutamate receptor 2 (CHEMBL2851) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Orally active metabotropic glutamate subtype 2 receptor positive allosteric modulators: structure-activity relationships and assessment in a rat model of nicotine dependence.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 25 | 6.71 | 7.70 |
| EC90 | 5 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2179632 | — | — | 1 | 7.70 |
| CHEMBL2179646 | — | — | 1 | 7.70 |
| CHEMBL1651208 | — | — | 1 | 7.30 |
| CHEMBL2179631 | — | — | 1 | 7.10 |
| CHEMBL2179633 | — | — | 1 | 7.10 |
| CHEMBL2179634 | — | — | 1 | 7.05 |
| CHEMBL2179635 | — | — | 1 | 6.96 |
| CHEMBL2179636 | — | — | 1 | 6.96 |
| CHEMBL2179629 | — | — | 1 | 6.89 |
| CHEMBL2179637 | — | — | 1 | 6.89 |
| CHEMBL1651219 | — | — | 1 | 6.77 |
| CHEMBL2179638 | — | — | 1 | 6.77 |
| CHEMBL2179643 | — | — | 1 | 6.70 |
| CHEMBL2179644 | — | — | 1 | 6.62 |
| CHEMBL593013 | — | — | 1 | 6.42 |
| CHEMBL2179628 | — | — | 1 | 6.33 |
| CHEMBL2179627 | — | — | 1 | 6.24 |
| CHEMBL2179630 | — | — | 1 | 6.19 |
| CHEMBL2179625 | — | — | 1 | 6.19 |
| CHEMBL2179642 | — | — | 1 | 6.13 |
| CHEMBL2179645 | — | — | 1 | 6.01 |
| CHEMBL2179626 | — | — | 1 | 5.61 |
| CHEMBL2179639 | — | — | 1 | - |
| CHEMBL2179640 | — | — | 1 | - |
| CHEMBL2179641 | — | — | 1 | - |
| CHEMBL2179624 | — | — | 1 | - |
| CHEMBL2179623 | — | — | 1 | - |
| CHEMBL2179622 | — | — | 1 | - |
| CHEMBL2179621 | — | — | 1 | - |
| CHEMBL2179620 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2179632 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2179646 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1651208 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2179631 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2179633 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2179634 | — | EC50 | = | 90.0 | nM | 7.05 |
| CHEMBL2179635 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL2179636 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL2179629 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL2179637 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1651219 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL2179638 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL2179643 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2179644 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL593013 | — | EC50 | = | 380.0 | nM | 6.42 |
| CHEMBL2179628 | — | EC50 | = | 470.0 | nM | 6.33 |
| CHEMBL2179627 | — | EC50 | = | 580.0 | nM | 6.24 |
| CHEMBL2179630 | — | EC50 | = | 650.0 | nM | 6.19 |
| CHEMBL2179625 | — | EC50 | = | 640.0 | nM | 6.19 |
| CHEMBL2179642 | — | EC50 | = | 740.0 | nM | 6.13 |
| CHEMBL2179645 | — | EC50 | = | 980.0 | nM | 6.01 |
| CHEMBL2179626 | — | EC50 | = | 2480.0 | nM | 5.61 |
| CHEMBL2179639 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL2179640 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL2179641 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL2179624 | — | EC90 | = | 0.237 | uM | - |
| CHEMBL2179623 | — | EC90 | = | 0.664 | uM | - |
| CHEMBL2179622 | — | EC90 | = | 0.248 | uM | - |
| CHEMBL2179621 | — | EC90 | = | 0.102 | uM | - |
| CHEMBL2179620 | — | EC90 | - | — | - |