Assay Detail
Functional
CHEMBL947083
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Antagonist activity at rat mGluR2 assessed as effect on (1S,3R)-ACPD-induced inhibition of forskolin-stimulated cAMP production
19
Total Activities
19
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 8-ethynyl-1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: part 2. New potent non-competitive metabotropic glutamate receptor 2/3 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.89 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL256011 | — | — | 1 | 8.05 |
| CHEMBL402886 | — | — | 1 | 8.00 |
| CHEMBL411440 | — | — | 1 | 7.96 |
| CHEMBL256812 | — | — | 1 | 7.92 |
| CHEMBL270616 | — | — | 1 | 7.89 |
| CHEMBL404463 | — | — | 1 | 7.82 |
| CHEMBL404080 | — | — | 1 | 7.80 |
| CHEMBL401446 | — | — | 1 | 7.77 |
| CHEMBL404886 | — | — | 1 | 7.77 |
| CHEMBL256008 | — | — | 1 | - |
| CHEMBL428066 | — | — | 1 | - |
| CHEMBL271319 | — | — | 1 | - |
| CHEMBL258113 | — | — | 1 | - |
| CHEMBL255356 | — | — | 1 | - |
| CHEMBL270402 | — | — | 1 | - |
| CHEMBL430408 | — | — | 1 | - |
| CHEMBL255151 | — | — | 1 | - |
| CHEMBL402963 | — | — | 1 | - |
| CHEMBL256424 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL256011 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL402886 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL411440 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL256812 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL270616 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL404463 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL404080 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL401446 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL404886 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL256008 | — | IC50 | - | — | - | |
| CHEMBL428066 | — | IC50 | - | — | - | |
| CHEMBL271319 | — | IC50 | - | — | - | |
| CHEMBL258113 | — | IC50 | - | — | - | |
| CHEMBL255356 | — | IC50 | - | — | - | |
| CHEMBL270402 | — | IC50 | - | — | - | |
| CHEMBL430408 | — | IC50 | - | — | - | |
| CHEMBL255151 | — | IC50 | - | — | - | |
| CHEMBL402963 | — | IC50 | - | — | - | |
| CHEMBL256424 | — | IC50 | - | — | - |