DCG-IV [Ligand Id: 1377] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL284193
  • 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 in Human [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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  • mGlu6 receptor/Metabotropic glutamate receptor 6 in Rat [ChEMBL: CHEMBL3842] [GtoPdb: 294] [UniProtKB: P35349]
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  • mGlu7 receptor in Human [GtoPdb: 295] [UniProtKB: Q14831]
  • mGlu7 receptor/Metabotropic glutamate receptor 7 in Rat [ChEMBL: CHEMBL3879] [GtoPdb: 295] [UniProtKB: P35400]
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  • mGlu8 receptor in Human [GtoPdb: 296] [UniProtKB: O00222]
  • mGlu8 receptor/Metabotropic glutamate receptor 8 in Rat [ChEMBL: CHEMBL2718] [GtoPdb: 296] [UniProtKB: P70579]
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  • mGlu5 receptor in Rat [GtoPdb: 293] [UniProtKB: P31424]
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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]
GtoPdb - - 4.1 pKi - - - J Neurochem (2000) 75: 2590-601 [PMID:11080213]
ChEMBL Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells B 4.11 pKi 77000 nM Ki J. Med. Chem. (2002) 45: 3171-3183 [PMID:12109902]
ChEMBL Metabotropic glutamate receptor 1 agonist activity as basal [3H]- IP formation in rat F 4 pEC50 >100000 nM EC50 J. Med. Chem. (2004) 47: 456-466 [PMID:14711315]
mGlu2 receptor/Metabotropic glutamate receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416]
GtoPdb - - 6.5 pKi - - - Neuropharmacology (1999) 38: 1519-29 [PMID:10530814]
ChEMBL Binding affinity at Metabotropic glutamate receptor 2 B 6.96 pKi 110 nM Ki J. Med. Chem. (2002) 45: 3171-3183 [PMID:12109902]
mGlu2 receptor/Metabotropic glutamate receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2851] [GtoPdb: 290] [UniProtKB: P31421]
GtoPdb - - 7 pKi - - - Br J Pharmacol (1998) 123: 497-504 [PMID:9504391];
Neuropharmacology (2000) 39: 1700-6 [PMID:10884552]
ChEMBL Agonist activity at rat mGlu2 receptor by FRET based mGlu sensor assay B 6.46 pEC50 350 nM EC50 J. Med. Chem. (2016) 59: 914-924 [PMID:26814576]
ChEMBL Concentration for half maximal activation of metabotropic glutamate mGluR2 in rat B 6.52 pEC50 300 nM EC50 J. Med. Chem. (1995) 38: 1417-1426 [PMID:7738999]
ChEMBL Metabotropic glutamate receptor 2 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells F 6.52 pEC50 300 nM EC50 J. Med. Chem. (2004) 47: 456-466 [PMID:14711315]
ChEMBL Agonist activity at rat mGlu2 receptor expressed in HEK293 cells assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader F 7.35 pEC50 45 nM EC50 J. Med. Chem. (2010) 53: 2797-2813 [PMID:20218620]
mGlu3 receptor in Human [GtoPdb: 291] [UniProtKB: Q14832]
GtoPdb - - 7.2 pKi - - - Neuropharmacology (1999) 38: 1519-29 [PMID:10530814]
mGlu3 receptor/Metabotropic glutamate receptor 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3067] [GtoPdb: 291] [UniProtKB: P31422]
GtoPdb - - 6.8 pKi - - - Neuropharmacology (2000) 39: 1700-6 [PMID:10884552]
ChEMBL Concentration for half maximal activation of metabotropic glutamate mGluR3 in rat B 6.52 pEC50 300 nM EC50 J. Med. Chem. (1995) 38: 1417-1426 [PMID:7738999]
ChEMBL Metabotropic glutamate receptor 3 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells F 6.7 pEC50 200 nM EC50 J. Med. Chem. (2004) 47: 456-466 [PMID:14711315]
ChEMBL Agonist activity at rat mGlu3 receptor by FRET based mGlu sensor assay B 7.1 pEC50 80 nM EC50 J. Med. Chem. (2016) 59: 914-924 [PMID:26814576]
mGlu4 receptor/Metabotropic glutamate receptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2787] [GtoPdb: 292] [UniProtKB: P31423]
ChEMBL Metabotropic glutamate receptor 4 antagonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells F 4.64 pEC50 23000 nM EC50 J. Med. Chem. (2004) 47: 456-466 [PMID:14711315]
mGlu6 receptor/Metabotropic glutamate receptor 6 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3842] [GtoPdb: 294] [UniProtKB: P35349]
ChEMBL Metabotropic glutamate receptor 6 antagonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells F 4.4 pEC50 40000 nM EC50 J. Med. Chem. (2004) 47: 456-466 [PMID:14711315]
GtoPdb - - 5.6 pEC50 - - - Neuropharmacology (1998) 37: 1043-51 [PMID:9833633]
mGlu7 receptor in Human [GtoPdb: 295] [UniProtKB: Q14831]
GtoPdb - - 4.7 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2000) 362: 546-54 [PMID:11138847]
mGlu7 receptor/Metabotropic glutamate receptor 7 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3879] [GtoPdb: 295] [UniProtKB: P35400]
ChEMBL Metabotropic glutamate receptor 7 antagonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells F 4.4 pEC50 40000 nM EC50 J. Med. Chem. (2004) 47: 456-466 [PMID:14711315]
mGlu8 receptor in Human [GtoPdb: 296] [UniProtKB: O00222]
GtoPdb - - 5.5 pIC50 - - - Brain Res Mol Brain Res (1999) 67: 201-10 [PMID:10216218]
mGlu8 receptor/Metabotropic glutamate receptor 8 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2718] [GtoPdb: 296] [UniProtKB: P70579]
ChEMBL Metabotropic glutamate receptor 8 antagonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells F 4.49 pEC50 32000 nM EC50 J. Med. Chem. (2004) 47: 456-466 [PMID:14711315]
mGlu5 receptor in Rat [GtoPdb: 293] [UniProtKB: P31424]
GtoPdb - - 4.7 pIC50 - - - J Neurochem (2000) 75: 2590-601 [PMID:11080213]

ChEMBL data shown on this page come from version 31:

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]