Assay Detail
Functional
CHEMBL3137095
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Non-competitive antagonist activity at human recombinant mGluR2 expressed in Chem-1 cell membrane assessed as inhibition of L-glutamate-induced [35S]GTPgammaS binding after 30 mins by liquid scintillation counting analysis
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | Chem-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and biological evaluation of novel 2,3-dihydro-1H-1,5-benzodiazepin-2-ones; potential imaging agents of the metabotropic glutamate 2 receptor
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 6.88 | 7.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3133882 | — | — | 1 | 7.05 |
| CHEMBL3133887 | — | — | 1 | 7.05 |
| CHEMBL3133885 | — | — | 1 | 7.04 |
| CHEMBL3133886 | — | — | 1 | 7.00 |
| CHEMBL3133883 | — | — | 1 | 6.88 |
| CHEMBL3133884 | — | — | 1 | 6.88 |
| CHEMBL305406 | — | — | 1 | 6.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3133882 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL3133887 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL3133885 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL3133886 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3133883 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL3133884 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL305406 | — | IC50 | = | 533.0 | nM | 6.27 |