Assay Detail
Functional
CHEMBL937486
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at rat mGluR2 assessed as blockade of (1S,3R)-ACPD-induced inhibition of forskolin-stimulated cAMP production
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Metabotropic glutamate receptor 2 (CHEMBL2851) ↗| 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 | 31 | 7.45 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL261050 | — | — | 1 | 8.00 |
| CHEMBL411440 | — | — | 1 | 7.96 |
| CHEMBL260642 | — | — | 1 | 7.85 |
| CHEMBL261051 | — | — | 1 | 7.82 |
| CHEMBL437835 | — | — | 1 | 7.77 |
| CHEMBL261081 | — | — | 1 | 7.75 |
| CHEMBL411095 | — | — | 1 | 7.72 |
| CHEMBL259054 | — | — | 1 | 7.62 |
| CHEMBL260636 | — | — | 1 | 7.57 |
| CHEMBL408455 | — | — | 1 | 7.47 |
| CHEMBL409638 | — | — | 1 | 7.44 |
| CHEMBL261288 | — | — | 1 | 7.43 |
| CHEMBL408229 | — | — | 1 | 7.41 |
| CHEMBL259269 | — | — | 1 | 7.33 |
| CHEMBL263649 | — | — | 1 | 7.28 |
| CHEMBL261263 | — | — | 1 | 7.14 |
| CHEMBL259340 | — | — | 1 | 7.13 |
| CHEMBL259053 | — | — | 1 | 6.94 |
| CHEMBL259924 | — | — | 1 | 6.74 |
| CHEMBL260643 | — | — | 1 | 6.57 |
| CHEMBL263906 | — | — | 1 | - |
| CHEMBL260343 | — | — | 1 | - |
| CHEMBL260415 | — | — | 1 | - |
| CHEMBL405895 | — | — | 1 | - |
| CHEMBL261251 | — | — | 1 | - |
| CHEMBL437646 | — | — | 1 | - |
| CHEMBL406061 | — | — | 1 | - |
| CHEMBL430231 | — | — | 1 | - |
| CHEMBL260455 | — | — | 1 | - |
| CHEMBL261128 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL261050 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL411440 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL260642 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL261051 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL437835 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL261081 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL411095 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL259054 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL260636 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL408455 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL409638 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL261288 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL408229 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL259269 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL263649 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL261263 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL259340 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL259053 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL259924 | — | IC50 | = | 184.0 | nM | 6.74 |
| CHEMBL260643 | — | IC50 | = | 268.0 | nM | 6.57 |
| CHEMBL263906 | — | IC50 | - | — | - | |
| CHEMBL260343 | — | IC50 | - | — | - | |
| CHEMBL260415 | — | IC50 | - | — | - | |
| CHEMBL405895 | — | IC50 | - | — | - | |
| CHEMBL261251 | — | IC50 | - | — | - | |
| CHEMBL437646 | — | IC50 | - | — | - | |
| CHEMBL406061 | — | IC50 | - | — | - | |
| CHEMBL430231 | — | IC50 | - | — | - | |
| CHEMBL260455 | — | IC50 | - | — | - | |
| CHEMBL261128 | — | IC50 | - | — | - | |
| CHEMBL430053 | — | IC50 | - | — | - |