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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL284193
  • mGlu1 receptor/Metabotropic glutamate receptor 1 in Rat [ChEMBL: CHEMBL4477] [GtoPdb: 289] [UniProtKB: P23385]
Created with Highcharts 10.3.3ValuesChart context menuMetabotropic glutamate receptor 1pKd RatpKi RatpIC50 RatpEC50 Rat012345Highcharts.com
  • 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]
Created with Highcharts 10.3.3ValuesChart context menuMetabotropic glutamate receptor 2pKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd RatpKi RatpIC50 RatpEC50 Rat02468Highcharts.com
  • mGlu3 receptor in Human [GtoPdb: 291] [UniProtKB: Q14832]
  • mGlu3 receptor/Metabotropic glutamate receptor 3 in Rat [ChEMBL: CHEMBL3067] [GtoPdb: 291] [UniProtKB: P31422]
Created with Highcharts 10.3.3ValuesChart context menumGlu3 receptorpKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd RatpKi RatpIC50 RatpEC50 Rat02468Highcharts.com
  • mGlu4 receptor/Metabotropic glutamate receptor 4 in Rat [ChEMBL: CHEMBL2787] [GtoPdb: 292] [UniProtKB: P31423]
Created with Highcharts 10.3.3ValuesChart context menuMetabotropic glutamate receptor 4pKd RatpKi RatpIC50 RatpEC50 Rat012345Highcharts.com
  • mGlu6 receptor/Metabotropic glutamate receptor 6 in Rat [ChEMBL: CHEMBL3842] [GtoPdb: 294] [UniProtKB: P35349]
Created with Highcharts 10.3.3ValuesChart context menuMetabotropic glutamate receptor 6pKd RatpKi RatpIC50 RatpEC50 Rat0123456Highcharts.com
  • mGlu7 receptor in Human [GtoPdb: 295] [UniProtKB: Q14831]
  • mGlu7 receptor/Metabotropic glutamate receptor 7 in Rat [ChEMBL: CHEMBL3879] [GtoPdb: 295] [UniProtKB: P35400]
Created with Highcharts 10.3.3ValuesChart context menumGlu7 receptorpKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd RatpKi RatpIC50 RatpEC50 Rat012345Highcharts.com
  • mGlu8 receptor in Human [GtoPdb: 296] [UniProtKB: O00222]
  • mGlu8 receptor/Metabotropic glutamate receptor 8 in Rat [ChEMBL: CHEMBL2718] [GtoPdb: 296] [UniProtKB: P70579]
Created with Highcharts 10.3.3ValuesChart context menumGlu8 receptorpKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd RatpKi RatpIC50 RatpEC50 Rat0123456Highcharts.com
  • mGlu5 receptor in Rat [GtoPdb: 293] [UniProtKB: P31424]
Created with Highcharts 10.3.3ValuesChart context menumGlu5 receptorpKd RatpKi RatpIC50 RatpEC50 Rat012345Highcharts.com
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 35:

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]