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 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]