MGS0028 [Ligand Id: 1395] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL121053
  • 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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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 Agonist activity at mGLUR2 expressed in CHO cells F 9.24 pEC50 0.57 nM EC50 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 Tested for binding affinity against Metabotropic glutamate receptor 2 in CHO cells using [3H]-7 as radioligand B 8.48 pKi 3.3 nM Ki J Med Chem (2000) 43: 4893-4909 [PMID:11123999]
GtoPdb - - 9.2 pKi - - - J Med Chem (2000) 43: 4893-909 [PMID:11123999]
ChEMBL Antagonist activity against Metabotropic glutamate receptor 2 expressed in CHO cells was evaluated in presence of 30 uM glutamic acid F 4 pEC50 >100000 nM EC50 J Med Chem (2000) 43: 4893-4909 [PMID:11123999]
ChEMBL Agonist activity against Metabotropic glutamate receptor 2 expressed in CHO cells was evaluated by measuring forskolin-induced cyclic AMP formation F 7.02 pEC50 94.7 nM EC50 J Med Chem (2000) 43: 4893-4909 [PMID:11123999]
ChEMBL Agonist activity against Metabotropic glutamate receptor 2 expressed in CHO cells was evaluated by measuring forskolin-induced cyclic AMP formation F 8.9 pEC50 1.26 nM EC50 J Med Chem (2000) 43: 4893-4909 [PMID:11123999]
ChEMBL Agonist activity against Metabotropic glutamate receptor 2 expressed in CHO cells was evaluated by measuring forskolin-induced cyclic AMP formation F 9.24 pEC50 0.57 nM EC50 J Med Chem (2000) 43: 4893-4909 [PMID:11123999]
mGlu3 receptor/Metabotropic glutamate receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2888] [GtoPdb: 291] [UniProtKB: Q14832]
ChEMBL Agonist activity at mGLUR3 expressed in CHO cells F 8.68 pEC50 2.07 nM EC50 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 Tested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells using [3H]-7 as radioligand B 8.44 pKi 3.62 nM Ki J Med Chem (2000) 43: 4893-4909 [PMID:11123999]
ChEMBL Antagonist activity against Metabotropic glutamate receptor 3 expressed in CHO cells was evaluated in presence of 30 uM glutamic acid F 4 pEC50 >100000 nM EC50 J Med Chem (2000) 43: 4893-4909 [PMID:11123999]
ChEMBL Agonist potency against cloned Metabotropic glutamate receptor 3 F 8.68 pEC50 2.07 nM EC50 J Med Chem (2000) 43: 4893-4909 [PMID:11123999]

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]