Assay Detail
Functional
CHEMBL1639554
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human mGluR2 receptor expressed in CHO cells assessed as inhibition of GIRK current
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and characterization of 1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: Part 4. In vivo active potent and selective non-competitive metabotropic glutamate receptor 2/3 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.69 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1629864 | — | — | 1 | 8.15 |
| CHEMBL1629863 | — | — | 1 | 8.00 |
| CHEMBL1629855 | — | — | 1 | 7.85 |
| CHEMBL1629866 | — | — | 1 | 7.82 |
| CHEMBL1629865 | — | — | 1 | 7.60 |
| CHEMBL1629862 | — | — | 1 | 7.42 |
| CHEMBL1631859 | — | — | 1 | 7.39 |
| CHEMBL1629861 | — | — | 1 | 7.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1629864 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1629863 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1629855 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1629866 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1629865 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1629862 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL1631859 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL1629861 | — | IC50 | = | 52.0 | nM | 7.28 |