Assay Detail
Binding
CHEMBL1639368
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Partial displacement of [3H]LY354740 from recombinant rat mGluR2
54
Total Activities
54
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 4. In vivo active potent and selective non-competitive metabotropic glutamate receptor 2/3 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 54 | 7.86 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1631876 | — | — | 1 | 8.70 |
| CHEMBL1629857 | — | — | 1 | 8.70 |
| CHEMBL1629856 | — | — | 1 | 8.70 |
| CHEMBL1629855 | — | — | 1 | 8.70 |
| CHEMBL1629864 | — | — | 1 | 8.40 |
| CHEMBL1629862 | — | — | 1 | 8.40 |
| CHEMBL1631864 | — | — | 1 | 8.40 |
| CHEMBL1631859 | — | — | 1 | 8.40 |
| CHEMBL1631858 | — | — | 1 | 8.40 |
| CHEMBL1631757 | — | — | 1 | 8.30 |
| CHEMBL1629844 | — | — | 1 | 8.30 |
| CHEMBL1629846 | — | — | 1 | 8.22 |
| CHEMBL1629852 | — | — | 1 | 8.22 |
| CHEMBL1629866 | — | — | 1 | 8.22 |
| CHEMBL1629860 | — | — | 1 | 8.15 |
| CHEMBL1631854 | — | — | 1 | 8.10 |
| CHEMBL1629863 | — | — | 1 | 8.10 |
| CHEMBL1629859 | — | — | 1 | 8.10 |
| CHEMBL1631860 | — | — | 1 | 8.10 |
| CHEMBL408229 | — | — | 1 | 8.05 |
| CHEMBL1629715 | — | — | 1 | 8.05 |
| CHEMBL1631863 | — | — | 1 | 8.00 |
| CHEMBL1631865 | — | — | 1 | 8.00 |
| CHEMBL1629847 | — | — | 1 | 8.00 |
| CHEMBL1629861 | — | — | 1 | 8.00 |
| CHEMBL1631861 | — | — | 1 | 7.92 |
| CHEMBL261288 | — | — | 1 | 7.92 |
| CHEMBL411095 | — | — | 1 | 7.92 |
| CHEMBL1631868 | — | — | 1 | 7.89 |
| CHEMBL1631869 | — | — | 1 | 7.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1631876 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1629857 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1629856 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1629855 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1631858 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1631859 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1631864 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1629862 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1629864 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1631757 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1629844 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1629866 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1629852 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1629846 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1629860 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1631854 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1631860 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1629859 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1629863 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL408229 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1629715 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1631863 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1631865 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1629847 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1629861 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1631861 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL411095 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL261288 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1631868 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1631869 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1631872 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1629845 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1629848 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1629858 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1631867 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1629850 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1629865 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1629854 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1629853 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1631875 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL411440 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1631874 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL401446 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL1631856 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL1631870 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL1631873 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL1631862 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL1629849 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL1631866 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL1631857 | — | IC50 | = | 120.0 | nM | 6.92 |