Assay Detail
Binding
CHEMBL937485
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Displacement of [3H]LY354740 from rat mGluR2
33
Total Activities
33
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 3. New potent non-competitive metabotropic glutamate receptor 2/3 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 7.45 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL261050 | — | — | 1 | 8.40 |
| CHEMBL408455 | — | — | 1 | 8.15 |
| CHEMBL437835 | — | — | 1 | 8.15 |
| CHEMBL408229 | — | — | 1 | 8.05 |
| CHEMBL263649 | — | — | 1 | 8.05 |
| CHEMBL260642 | — | — | 1 | 7.96 |
| CHEMBL411095 | — | — | 1 | 7.92 |
| CHEMBL260636 | — | — | 1 | 7.92 |
| CHEMBL261288 | — | — | 1 | 7.80 |
| CHEMBL259054 | — | — | 1 | 7.77 |
| CHEMBL261051 | — | — | 1 | 7.77 |
| CHEMBL261081 | — | — | 1 | 7.77 |
| CHEMBL261263 | — | — | 1 | 7.72 |
| CHEMBL405895 | — | — | 1 | 7.66 |
| CHEMBL260415 | — | — | 1 | 7.60 |
| CHEMBL411440 | — | — | 1 | 7.58 |
| CHEMBL259053 | — | — | 1 | 7.57 |
| CHEMBL259340 | — | — | 1 | 7.54 |
| CHEMBL409638 | — | — | 1 | 7.51 |
| CHEMBL401446 | — | — | 1 | 7.47 |
| CHEMBL259924 | — | — | 1 | 7.42 |
| CHEMBL259269 | — | — | 1 | 7.41 |
| CHEMBL260643 | — | — | 1 | 7.38 |
| CHEMBL263906 | — | — | 1 | 7.37 |
| CHEMBL406061 | — | — | 1 | 7.22 |
| CHEMBL430231 | — | — | 1 | 7.16 |
| CHEMBL437646 | — | — | 1 | 7.14 |
| CHEMBL261128 | — | — | 1 | 7.04 |
| CHEMBL260343 | — | — | 1 | 6.89 |
| CHEMBL261251 | — | — | 1 | 6.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL261050 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL408455 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL437835 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL408229 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL263649 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL260642 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL411095 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL260636 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL261288 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL259054 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL261051 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL261081 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL261263 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL405895 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL260415 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL411440 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL259053 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL259340 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL409638 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL401446 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL259924 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL259269 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL260643 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL263906 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL406061 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL430231 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL437646 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL261128 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL260343 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL261251 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL430053 | — | IC50 | = | 466.0 | nM | 6.33 |
| CHEMBL260455 | — | IC50 | = | 608.0 | nM | 6.22 |
| CHEMBL394287 | — | IC50 | = | 6400.0 | nM | 5.19 |