MGS0039 [Ligand Id: 1397] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL186453
  • mGlu1 receptor/Metabotropic glutamate receptor 1 in Rat [ChEMBL: CHEMBL4477] [GtoPdb: 289] [UniProtKB: P23385]
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  • mGlu2 receptor/Metabotropic glutamate receptor 2 in Human [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416]
  • mGlu2 receptor/Metabotropic glutamate receptor 2 in Rat [ChEMBL: CHEMBL2851] [GtoPdb: 290] [UniProtKB: P31421]
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  • mGlu3 receptor/Metabotropic glutamate receptor 3 in Human [ChEMBL: CHEMBL2888] [GtoPdb: 291] [UniProtKB: Q14832]
  • mGlu3 receptor/Metabotropic glutamate receptor 3 in Rat [ChEMBL: CHEMBL3067] [GtoPdb: 291] [UniProtKB: P31422]
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  • mGlu4 receptor/Metabotropic glutamate receptor 4 in Rat [ChEMBL: CHEMBL2787] [GtoPdb: 292] [UniProtKB: P31423]
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  • mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424]
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  • mGlu6 receptor/Metabotropic glutamate receptor 6 in Rat [ChEMBL: CHEMBL3842] [GtoPdb: 294] [UniProtKB: P35349]
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  • mGlu7 receptor/Metabotropic glutamate receptor 7 in Rat [ChEMBL: CHEMBL3879] [GtoPdb: 295] [UniProtKB: P35400]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
mGlu1 receptor/Metabotropic glutamate receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4477] [GtoPdb: 289] [UniProtKB: P23385]
ChEMBL Concentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cells B 4.03 pIC50 93300 nM IC50 J. Med. Chem. (2004) 47: 4570-4587 [PMID:15317467]
ChEMBL Effective concentration for agonistic activity towards metabotropic glutamate receptor 1 of rat expressed in CHO cells F 4 pEC50 >100000 nM EC50 J. Med. Chem. (2004) 47: 4570-4587 [PMID:15317467]
mGlu2 receptor/Metabotropic glutamate receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416]
ChEMBL Binding affinity to mGLUR2 B 8.66 pKi 2.2 nM Ki Bioorg. Med. Chem. Lett. (2012) 22: 1958-1962 [PMID:22318160]
ChEMBL Antagonist activity at mGLUR2 expressed in CHO cells assessed as inhibition of glutamate-induced inhibition of forskolin-stimulated cAMP production F 7.7 pIC50 20 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 1958-1962 [PMID:22318160]
mGlu2 receptor/Metabotropic glutamate receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2851] [GtoPdb: 290] [UniProtKB: P31421]
ChEMBL Binding affinity towards metabotropic glutamate receptor 2 of rat expressed in CHO cells was determined by using [3H]MGS-0008 B 8.62 pKi 2.38 nM Ki J. Med. Chem. (2004) 47: 4570-4587 [PMID:15317467]
GtoPdb - - 8.7 pKi - - - Neuropharmacology (2004) 46: 457-67 [PMID:14975669];
J. Med. Chem. (2004) 47: 4570-87 [PMID:15317467]
ChEMBL Concentration required to inhibit metabotropic glutamate receptor 2 activity of rat expressed in CHO cells B 7.7 pIC50 20 nM IC50 J. Med. Chem. (2004) 47: 4570-4587 [PMID:15317467]
ChEMBL Effective concentration for agonistic activity towards metabotropic glutamate receptor 2 of rat expressed in CHO cells F 4 pEC50 >100000 nM EC50 J. Med. Chem. (2004) 47: 4570-4587 [PMID:15317467]
mGlu3 receptor/Metabotropic glutamate receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2888] [GtoPdb: 291] [UniProtKB: Q14832]
ChEMBL Binding affinity to mGLUR3 B 8.35 pKi 4.5 nM Ki Bioorg. Med. Chem. Lett. (2012) 22: 1958-1962 [PMID:22318160]
ChEMBL Antagonist activity at mGLUR3 expressed in CHO cells assessed as inhibition of glutamate-induced inhibition of forskolin-stimulated cAMP production F 7.62 pIC50 24 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 1958-1962 [PMID:22318160]
mGlu3 receptor/Metabotropic glutamate receptor 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3067] [GtoPdb: 291] [UniProtKB: P31422]
ChEMBL Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008 B 8.35 pKi 4.46 nM Ki J. Med. Chem. (2004) 47: 4570-4587 [PMID:15317467]
GtoPdb - - 8.4 pKi - - - Neuropharmacology (2004) 46: 457-67 [PMID:14975669];
J. Med. Chem. (2004) 47: 4570-87 [PMID:15317467]
ChEMBL Concentration required to inhibit metabotropic glutamate receptor 3 activity of rat expressed in CHO cells B 7.62 pIC50 24 nM IC50 J. Med. Chem. (2004) 47: 4570-4587 [PMID:15317467]
ChEMBL Effective concentration for agonistic activity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells F 4 pEC50 >100000 nM EC50 J. Med. Chem. (2004) 47: 4570-4587 [PMID:15317467]
mGlu4 receptor/Metabotropic glutamate receptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2787] [GtoPdb: 292] [UniProtKB: P31423]
ChEMBL Concentration required to inhibit metabotropic glutamate receptor 4 activity of rat expressed in CHO cells B 5.76 pIC50 1740 nM IC50 J. Med. Chem. (2004) 47: 4570-4587 [PMID:15317467]
mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424]
ChEMBL Concentration required to inhibit metabotropic glutamate receptor 5 activity of rat expressed in CHO cells B 4.93 pIC50 11700 nM IC50 J. Med. Chem. (2004) 47: 4570-4587 [PMID:15317467]
ChEMBL Effective concentration for agonistic activity towards metabotropic glutamate receptor 5 of rat expressed in CHO cells F 4 pEC50 >100000 nM EC50 J. Med. Chem. (2004) 47: 4570-4587 [PMID:15317467]
mGlu6 receptor/Metabotropic glutamate receptor 6 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3842] [GtoPdb: 294] [UniProtKB: P35349]
ChEMBL Concentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cells B 5.69 pIC50 2060 nM IC50 J. Med. Chem. (2004) 47: 4570-4587 [PMID:15317467]
ChEMBL Effective concentration for agonistic activity towards metabotropic glutamate receptor 6 of rat expressed in CHO cells F 4 pEC50 >100000 nM EC50 J. Med. Chem. (2004) 47: 4570-4587 [PMID:15317467]
mGlu7 receptor/Metabotropic glutamate receptor 7 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3879] [GtoPdb: 295] [UniProtKB: P35400]
ChEMBL Binding affinity towards metabotropic glutamate receptor 7 of rat expressed in CHO cells was determined by using [3H]MGS-0008 B 6.18 pKi 664 nM Ki J. Med. Chem. (2004) 47: 4570-4587 [PMID:15317467]

ChEMBL data shown on this page come from version 26:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]