Target & Activity
| Target | Activity | Value |
|---|---|---|
| mGluR5 |
Cellular Effect
| Cell Line | Activity | Value | Description | Reference |
|---|---|---|---|---|
| HEK293 | IC50 | 2.6 nM | Negative allosteric modulation of rat recombinant mGluR5 expressed in HEK293 cells expressing GLAST assessed as inhibition of DHPG-induced intracellular Ca2+ level after 30 mins by FLIPR assay | [PMID: 23046966] |
| HEK293 | IC50 | 26 nM | Negative allosteric modulation of human recombinant mGluR5 expressed in HEK293 cells expressing GLAST assessed as inhibition of glutamate-stimulated IP accumulation incubated for 10 mins prior to glutamate challenge measured 30 mins post glutamate challen | [PMID: 23046966] |
| HEK293 | IC50 | 7.6 nM | Negative allosteric modulation of human recombinant mGluR5 expressed in HEK293 cells expressing GLAST assessed as inhibition of DHPG-induced intracellular Ca2+ level after 30 mins by FLIPR assay | [PMID: 23046966] |