Assay Detail
Binding
CHEMBL4719947
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-LY459477 from recombinant human mGlu2 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | AV12 |
| Subcellular | Cell membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of (1S,2R,3S,4S,5R,6R)-2-Amino-3-[(3,4-difluorophenyl)sulfanylmethyl]-4-hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid Hydrochloride (LY3020371·HCl): A Potent, Metabotropic Glutamate 2/3 Receptor Antagonist with Antidepressant-Like Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 7.53 | 8.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL432038 | — | — | 1 | 8.37 |
| CHEMBL4759992 | — | — | 1 | 8.28 |
| CHEMBL4751065 | — | — | 1 | 8.28 |
| CHEMBL4748699 | — | — | 1 | 8.08 |
| CHEMBL4780402 | — | — | 1 | 8.05 |
| CHEMBL4746125 | — | — | 1 | 8.04 |
| CHEMBL4776989 | — | — | 1 | 7.98 |
| CHEMBL4757159 | — | — | 1 | 7.85 |
| CHEMBL4760856 | — | — | 1 | 7.69 |
| CHEMBL4759209 | — | — | 1 | 7.67 |
| CHEMBL4756556 | — | — | 1 | 7.62 |
| CHEMBL4781638 | — | — | 1 | 7.51 |
| CHEMBL4784701 | — | — | 1 | 7.36 |
| CHEMBL4778355 | — | — | 1 | 6.57 |
| CHEMBL4779554 | — | — | 1 | 6.57 |
| CHEMBL4755204 | — | — | 1 | 6.14 |
| CHEMBL4749728 | — | — | 1 | 5.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL432038 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL4759992 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL4751065 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL4748699 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL4780402 | — | Ki | = | 8.9 | nM | 8.05 |
| CHEMBL4746125 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL4776989 | — | Ki | = | 10.4 | nM | 7.98 |
| CHEMBL4757159 | — | Ki | = | 14.2 | nM | 7.85 |
| CHEMBL4760856 | — | Ki | = | 20.5 | nM | 7.69 |
| CHEMBL4759209 | — | Ki | = | 21.4 | nM | 7.67 |
| CHEMBL4756556 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL4781638 | — | Ki | = | 30.9 | nM | 7.51 |
| CHEMBL4784701 | — | Ki | = | 43.7 | nM | 7.36 |
| CHEMBL4778355 | — | Ki | = | 268.0 | nM | 6.57 |
| CHEMBL4779554 | — | Ki | = | 271.0 | nM | 6.57 |
| CHEMBL4755204 | — | Ki | = | 728.0 | nM | 6.14 |
| CHEMBL4749728 | — | Ki | = | 1200.0 | nM | 5.92 |