Assay Detail
Functional
CHEMBL3619271
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human recombinant mGlu2 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
16
Total Activities
16
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
Synthesis and Pharmacological Characterization of C4-(Thiotriazolyl)-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1R,2S,4R,5R,6R)-2-Amino-4-(1H-1,2,4-triazol-3-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2812223), a Highly Potent, Functionally Selective mGlu2 Receptor Agonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 16 | 7.97 | 9.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3616857 | — | — | 1 | 9.24 |
| CHEMBL3616856 | — | — | 1 | 9.19 |
| CHEMBL3616851 | — | — | 1 | 8.35 |
| CHEMBL3616860 | — | — | 1 | 8.28 |
| CHEMBL3616847 | — | — | 1 | 8.25 |
| CHEMBL3616858 | — | — | 1 | 8.19 |
| CHEMBL8759 | EGLUMETAD | 2.0 | 1 | 8.15 |
| CHEMBL3616848 | — | — | 1 | 7.98 |
| CHEMBL3616854 | — | — | 1 | 7.95 |
| CHEMBL3616850 | — | — | 1 | 7.93 |
| CHEMBL3616853 | — | — | 1 | 7.91 |
| CHEMBL3616849 | — | — | 1 | 7.86 |
| CHEMBL3616852 | — | — | 1 | 7.78 |
| CHEMBL3616855 | — | — | 1 | 7.35 |
| CHEMBL3616859 | — | — | 1 | 7.13 |
| CHEMBL2381651 | — | — | 1 | 5.93 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3616857 | — | EC50 | = | 0.58 | nM | 9.24 |
| CHEMBL3616856 | — | EC50 | = | 0.65 | nM | 9.19 |
| CHEMBL3616851 | — | EC50 | = | 4.5 | nM | 8.35 |
| CHEMBL3616860 | — | EC50 | = | 5.2 | nM | 8.28 |
| CHEMBL3616847 | — | EC50 | = | 5.6 | nM | 8.25 |
| CHEMBL3616858 | — | EC50 | = | 6.4 | nM | 8.19 |
| CHEMBL8759 | EGLUMETAD | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3616848 | — | EC50 | = | 10.4 | nM | 7.98 |
| CHEMBL3616854 | — | EC50 | = | 11.2 | nM | 7.95 |
| CHEMBL3616850 | — | EC50 | = | 11.8 | nM | 7.93 |
| CHEMBL3616853 | — | EC50 | = | 12.4 | nM | 7.91 |
| CHEMBL3616849 | — | EC50 | = | 13.9 | nM | 7.86 |
| CHEMBL3616852 | — | EC50 | = | 16.5 | nM | 7.78 |
| CHEMBL3616855 | — | EC50 | = | 44.3 | nM | 7.35 |
| CHEMBL3616859 | — | EC50 | = | 74.0 | nM | 7.13 |
| CHEMBL2381651 | — | EC50 | = | 1170.0 | nM | 5.93 |