Assay Detail
Functional
CHEMBL4719942
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | AV12 |
| 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 |
|---|---|---|---|
| IC50 | 18 | 6.92 | 8.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4751065 | — | — | 1 | 8.21 |
| CHEMBL432038 | — | — | 1 | 8.11 |
| CHEMBL4746125 | — | — | 1 | 7.91 |
| CHEMBL4759992 | — | — | 1 | 7.79 |
| CHEMBL4780402 | — | — | 1 | 7.57 |
| CHEMBL4776989 | — | — | 1 | 7.38 |
| CHEMBL4748699 | — | — | 1 | 7.25 |
| CHEMBL4760856 | — | — | 1 | 7.21 |
| CHEMBL4757159 | — | — | 1 | 7.21 |
| CHEMBL3956934 | — | — | 1 | 6.96 |
| CHEMBL4756556 | — | — | 1 | 6.79 |
| CHEMBL4759209 | — | — | 1 | 6.70 |
| CHEMBL4784701 | — | — | 1 | 6.57 |
| CHEMBL4781638 | — | — | 1 | 6.26 |
| CHEMBL4755204 | — | — | 1 | 6.01 |
| CHEMBL4779554 | — | — | 1 | 5.67 |
| CHEMBL4778355 | — | — | 1 | 5.62 |
| CHEMBL4749728 | — | — | 1 | 5.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4751065 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL432038 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL4746125 | — | IC50 | = | 12.4 | nM | 7.91 |
| CHEMBL4759992 | — | IC50 | = | 16.1 | nM | 7.79 |
| CHEMBL4780402 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4776989 | — | IC50 | = | 41.9 | nM | 7.38 |
| CHEMBL4748699 | — | IC50 | = | 56.5 | nM | 7.25 |
| CHEMBL4760856 | — | IC50 | = | 62.3 | nM | 7.21 |
| CHEMBL4757159 | — | IC50 | = | 61.1 | nM | 7.21 |
| CHEMBL3956934 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4756556 | — | IC50 | = | 163.0 | nM | 6.79 |
| CHEMBL4759209 | — | IC50 | = | 202.0 | nM | 6.70 |
| CHEMBL4784701 | — | IC50 | = | 272.0 | nM | 6.57 |
| CHEMBL4781638 | — | IC50 | = | 547.0 | nM | 6.26 |
| CHEMBL4755204 | — | IC50 | = | 967.0 | nM | 6.01 |
| CHEMBL4779554 | — | IC50 | = | 2160.0 | nM | 5.67 |
| CHEMBL4778355 | — | IC50 | = | 2410.0 | nM | 5.62 |
| CHEMBL4749728 | — | IC50 | = | 4560.0 | nM | 5.34 |