compound 4 [PMID: 21105727] [Ligand Id: 6224] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1630807
  • mGlu2 receptor/Metabotropic glutamate receptor 2 in Human [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416]
Created with Highcharts 10.3.3ValuesChart context menuMetabotropic glutamate receptor 2pKd HumanpKi HumanpIC50 HumanpEC50 Human01234567Highcharts.com
  • mGlu3 receptor/Metabotropic glutamate receptor 3 in Human [ChEMBL: CHEMBL2888] [GtoPdb: 291] [UniProtKB: Q14832]
Created with Highcharts 10.3.3ValuesChart context menuMetabotropic glutamate receptor 3pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
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 Binding affinity to GFP tagged human mGluR2 containing truncated N-terminal region expressed in HEK cells by FRET assay B 6.1 pKi 800 nM Ki J Med Chem (2010) 53: 8775-8779 [PMID:21105727]
GtoPdb - - 6.1 pKi 800 nM Ki J Med Chem (2010) 53: 8775-9 [PMID:21105727]
GtoPdb - - 6 pIC50 1000 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 6 pIC50 1000 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]
GtoPdb - - 4.98 pEC50 10400 nM EC50 J Med Chem (2010) 53: 8775-9 [PMID:21105727]
ChEMBL Positive allosteric modulator activity at human mGluR3 expressed in HEK cells in presence of glutamate EC10 concentration by Ca2+ functional assay F 4.98 pEC50 10400 nM EC50 J Med Chem (2010) 53: 8775-8779 [PMID:21105727]

ChEMBL data shown on this page come from version 35:

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]