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 34:

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]