Assay Detail
Functional
CHEMBL937488
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at rat mGluR3 expressed in CHO cells assessed as inhibition of glutamate-induced GIRK current
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Metabotropic glutamate receptor 3 (CHEMBL3067) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and characterization of 1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: Part 3. New potent non-competitive metabotropic glutamate receptor 2/3 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.39 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL259054 | — | — | 1 | 7.77 |
| CHEMBL260636 | — | — | 1 | 7.48 |
| CHEMBL261288 | — | — | 1 | 7.38 |
| CHEMBL405895 | — | — | 1 | 6.91 |
| CHEMBL411440 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL259054 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL260636 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL261288 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL405895 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL411440 | — | IC50 | - | — | - |