Assay Detail
Binding
CHEMBL947082
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]LY354740 from rat recombinant mGluR2 expressed in CHO cells
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | CHO |
| 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 | 7.33 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL256812 | — | — | 1 | 8.22 |
| CHEMBL256011 | — | — | 1 | 8.05 |
| CHEMBL402886 | — | — | 1 | 7.89 |
| CHEMBL270616 | — | — | 1 | 7.75 |
| CHEMBL404886 | — | — | 1 | 7.70 |
| CHEMBL404080 | — | — | 1 | 7.70 |
| CHEMBL404463 | — | — | 1 | 7.64 |
| CHEMBL411440 | — | — | 1 | 7.58 |
| CHEMBL401446 | — | — | 1 | 7.47 |
| CHEMBL270402 | — | — | 1 | 7.44 |
| CHEMBL402963 | — | — | 1 | 7.34 |
| CHEMBL255151 | — | — | 1 | 7.19 |
| CHEMBL430408 | — | — | 1 | 7.14 |
| CHEMBL255356 | — | — | 1 | 7.01 |
| CHEMBL428066 | — | — | 1 | 7.01 |
| CHEMBL256424 | — | — | 1 | 6.85 |
| CHEMBL271319 | — | — | 1 | 6.77 |
| CHEMBL256008 | — | — | 1 | 6.42 |
| CHEMBL258113 | — | — | 1 | 6.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL256812 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL256011 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL402886 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL270616 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL404886 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL404080 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL404463 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL411440 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL401446 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL270402 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL402963 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL255151 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL430408 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL255356 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL428066 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL256424 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL271319 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL256008 | — | IC50 | = | 378.0 | nM | 6.42 |
| CHEMBL258113 | — | IC50 | = | 730.0 | nM | 6.14 |