compound 3 [PMID: 21105727] [Ligand Id: 6223] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1630806
  • mGlu2 receptor/Metabotropic glutamate receptor 2 in Human [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416]
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  • mGlu3 receptor/Metabotropic glutamate receptor 3 in Human [ChEMBL: CHEMBL2888] [GtoPdb: 291] [UniProtKB: Q14832]
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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]
GtoPdb - - 6.22 pKi 600 nM Ki J Med Chem (2010) 53: 8775-9 [PMID:21105727]
ChEMBL Binding affinity to GFP tagged human mGluR2 containing truncated N-terminal region expressed in HEK cells by FRET assay B 6.22 pKi 600 nM Ki J Med Chem (2010) 53: 8775-8779 [PMID:21105727]
GtoPdb - - 5.82 pIC50 1500 nM IC50 J Med Chem (2010) 53: 8775-9 [PMID:21105727]
ChEMBL Negative allosteric modulator activity at human mGluR2 expressed in HEK cells in presence of glutamate EC80 concentration by Ca2+ functional assay F 5.82 pIC50 1500 nM IC50 J Med Chem (2010) 53: 8775-8779 [PMID:21105727]
mGlu3 receptor/Metabotropic glutamate receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2888] [GtoPdb: 291] [UniProtKB: Q14832]
ChEMBL Positive allosteric modulator activity at human mGluR3 expressed in HEK cells in presence of glutamate EC10 concentration by Ca2+ functional assay F 5.05 pEC50 8900 nM EC50 J Med Chem (2010) 53: 8775-8779 [PMID:21105727]
GtoPdb - - 5.1 pEC50 8900 nM EC50 J Med Chem (2010) 53: 8775-9 [PMID:21105727]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]