ChEMBL ligand: CHEMBL108939
mGlu2 receptor/Metabotropic glutamate receptor 2 in Human [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
mGlu2 receptor/Metabotropic glutamate receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416]
ChEMBL	Ability to displace [3H]LY-341,495 at glutamate-site on Metabotropic glutamate receptor 2; No significant displacement	B	4	pIC50	>100000	nM	IC50	J Med Chem (2003) 46: 3189-3192 [PMID:12852748]
GtoPdb	-	-	5.8	pIC50	-	-	-	J Med Chem (2003) 46: 3189-92 [PMID:12852748]; Mol Pharmacol (2003) 64: 798-810 [PMID:14500736]; Psychopharmacology (Berl.) (2005) 179: 271-83 [PMID:15717213]; Bioorg Med Chem Lett (2004) 14: 3099-102 [PMID:15149652]
ChEMBL	Binding affinity towards human metabotropic glutamate receptor 2 determined by [35S]GTP gamma S binding assay	F	5.77	pEC50	1700	nM	EC50	Bioorg Med Chem Lett (2004) 14: 5867-5872 [PMID:15501058]
ChEMBL	Effective concentration for binding to human metabotropic glutamate receptor 2 as determined by GTPgammaS assay	B	5.77	pEC50	1700	nM	EC50	Bioorg Med Chem Lett (2004) 14: 5329-5332 [PMID:15454221]
ChEMBL	Effective concentration against Metabotropic glutamate receptor 2	B	6.57	pEC50	270	nM	EC50	J Med Chem (2003) 46: 3189-3192 [PMID:12852748]
ChEMBL	In Vitro Activity Test for mGluR2: Experimental materials: HEK/mGluR2 cell line (human GluR2 transfected HEK cell line), DMEM (FBS) medium, positive control LY487379 (purchased from sigma; CAS: to 352317-17-1)Experimental instrument: FLIPR Tetra real-time fluorescence imaging analysis systemExperimental method: HDB Fluo-8 calcium fluorescence detection methodExperimental principle: HDB Fluo-8 calcium ion fluorescence detection method is a fast, simple and reliable fluorescence detection method of intracellular calcium concentration changes. The Fluo 8-AM fluorescent dye is an acetyl methyl ester derivative of Fluo 8 which can easily penetrate into the cell membrane by culture. The fluorescent dye in the cell will be hydrolyzed by intracellular esterase, the resulting Fluo 8 as a polar molecule, cannot easily pass through the lipid bimolecular membrane, and will be retained in the cell, and combine with calcium (Ca2+) to produce fluoresces.Cells expressing GPCR receptor protein (mGluR2) were first calibrated with a calcium ion sensitive fluorescent probe and then stimulated with the compound. After stimulation, the receptor activates the calcium ion mobilization, and the fluorescent probe captures the calcium ion to induce the fluorescence signal. The signal can be read by a fluoroscopy plate. The fluorescent plate reader contains a sample addition for compound addition, thus enabling the change of the fluorescence value of the compound be read in real time. If the selected compound activates mGluR2, the calcium flow reaction can be greatly increased; conversely, if the selected compound is able to antagonize mGluR2, the calcium flow reaction can be greatly reduced. Experimental results indicate that the EC50 for mGluR2 of the compounds 1 to 106 of the present invention are between 0.02 μM-10 μM, preferably between 0.02 μM-1 μm. Further, the experimental results show that the activities of the fluorine-containing triazolopyridine compound 1-106 according to the present invention to mGluR2 is about 8-15 times higher than that of the fluorine-free triazolopyridine compound corresponding to each compound.	B	6.64	pEC50	230	nM	EC50	US-10800776-B2. Fluorine-containing triazolopyridine, and manufacturing method, pharmaceutical composition, and application thereof (2020)

ChEMBL data shown on this page come from version 36:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]