[3H]quisqualate [Ligand Id: 1370] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL279956 (Quisqualate, quisqualic acid)
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  • Folate hydrolase (prostate-specific membrane antigen) 1/Glutamate carboxypeptidase II in Human [ChEMBL: CHEMBL1892] [GtoPdb: 1606] [UniProtKB: Q04609]
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  • GluK1/Glutamate receptor ionotropic kainate 1 in Rat [ChEMBL: CHEMBL2919] [GtoPdb: 450] [UniProtKB: P22756]
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  • GluK2/Glutamate receptor ionotropic kainate 2 in Rat [ChEMBL: CHEMBL3607] [GtoPdb: 451] [UniProtKB: P42260]
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  • GluK3/Glutamate receptor ionotropic kainate 3 in Rat [ChEMBL: CHEMBL3744] [GtoPdb: 452] [UniProtKB: P42264]
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  • mGlu1 receptor/Metabotropic glutamate receptor 1 in Human [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255]
  • mGlu1 receptor/Metabotropic glutamate receptor 1 in Rat [ChEMBL: CHEMBL4477] [GtoPdb: 289] [UniProtKB: P23385]
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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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  • mGlu4 receptor/Metabotropic glutamate receptor 4 in Rat [ChEMBL: CHEMBL2787] [GtoPdb: 292] [UniProtKB: P31423]
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  • mGlu5 receptor/Metabotropic glutamate receptor 5 in Human [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
  • mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424]
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  • mGlu8 receptor/Metabotropic glutamate receptor 8 in Mouse [ChEMBL: CHEMBL4626] [GtoPdb: 296] [UniProtKB: P47743]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Cystine/glutamate transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075149] [GtoPdb: 902] [UniProtKB: Q9UPY5]
ChEMBL Inhibition of amino acid transport system xc- B 5.3 pIC50 5000 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 2680-2683 [PMID:20303751]
Folate hydrolase (prostate-specific membrane antigen) 1/Glutamate carboxypeptidase II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1892] [GtoPdb: 1606] [UniProtKB: Q04609]
ChEMBL Inhibition of human recombinant glutamate carboxypeptidase 2 by radioenzymatic assay B 5.02 pIC50 9500 nM IC50 J. Med. Chem. (2007) 50: 3267-3273 [PMID:17567119]
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455456457458459461460] [UniProtKB: P35439Q00959Q00960Q00961Q62645Q8VHN2Q9R1M7]
ChEMBL Inhibition of [3H]CPP binding to rat N-methyl-D-aspartate glutamate receptor B 4 pIC50 >100000 nM IC50 J. Med. Chem. (1992) 35: 4720-4726 [PMID:1361582]
GluA1/GluA2/GluA4/GluA3/Glutamate receptor ionotropic, AMPA in Mouse (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2096617] [GtoPdb: 444445447446] [UniProtKB: P23818P23819Q9Z2W8Q9Z2W9]
ChEMBL Compound was tested for in vitro binding affinity against Ionotropic glutamate receptor AMPA using [3H]AMPA ligand B 7.1 pIC50 80 nM IC50 J. Med. Chem. (1998) 41: 930-939 [PMID:9526567]
GluA1/GluA2/GluA3/GluA4/Glutamate receptor ionotropic, AMPA in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2093871] [GtoPdb: 444445446447] [UniProtKB: P19490P19491P19492P19493]
ChEMBL Inhibition of Ionotropic glutamate receptor AMPA mediated depolarization by the compound at a concentration of 16 uM after 4 minutes B 5.15 pIC50 7000 nM IC50 J. Med. Chem. (1999) 42: 1639-1647 [PMID:10229632]
ChEMBL The compound was tested for its affinity against AMPA receptor in rats B 5.89 pIC50 1300 nM IC50 J. Med. Chem. (1992) 35: 4720-4726 [PMID:1361582]
GluK1/GluK2/GluK3/GluK4/GluK5/Glutamate receptor ionotropic, kainate in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094119] [GtoPdb: 450451452453454] [UniProtKB: P22756P42260P42264Q01812Q63273]
ChEMBL Compound was tested or its affinity against ionotropic glutamate receptor ionotropic kainate in rats B 6.82 pIC50 150 nM IC50 J. Med. Chem. (1992) 35: 4720-4726 [PMID:1361582]
GluK1/Glutamate receptor ionotropic kainate 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2919] [GtoPdb: 450] [UniProtKB: P22756]
ChEMBL Displacement of [3H]SYM2081 from rat recombinant iGluR5 B 6.77 pKi 171 nM Ki J. Med. Chem. (2008) 51: 4093-4103 [PMID:18578478]
ChEMBL Displacement of [3H]SYM2081 from rat recombinant iGluR5 B 6.77 pKi 169.82 nM Ki J. Med. Chem. (2008) 51: 4093-4103 [PMID:18578478]
GluK2/Glutamate receptor ionotropic kainate 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3607] [GtoPdb: 451] [UniProtKB: P42260]
ChEMBL Displacement of [3H]SYM2081 from rat recombinant iGluR6 B 6.87 pKi 134 nM Ki J. Med. Chem. (2008) 51: 4093-4103 [PMID:18578478]
ChEMBL Displacement of [3H]SYM2081 from rat recombinant iGluR6 B 6.88 pKi 131.83 nM Ki J. Med. Chem. (2008) 51: 4093-4103 [PMID:18578478]
GluK3/Glutamate receptor ionotropic kainate 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3744] [GtoPdb: 452] [UniProtKB: P42264]
ChEMBL Displacement of [3H]SYM2081 from rat recombinant iGluR7 B 5.78 pKi 1670 nM Ki J. Med. Chem. (2008) 51: 4093-4103 [PMID:18578478]
ChEMBL Displacement of [3H]SYM2081 from rat recombinant iGluR7 B 5.86 pKi 1380.38 nM Ki J. Med. Chem. (2008) 51: 4093-4103 [PMID:18578478]
mGlu1 receptor/Metabotropic glutamate receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255]
ChEMBL Agonist potency against cloned human metabotropic glutamate receptor 1 F 5.96 pKi 1100 nM Ki J. Med. Chem. (2000) 43: 2609-2645 [PMID:10893301]
ChEMBL Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a) B 6.7 pEC50 200 nM EC50 J. Med. Chem. (1996) 39: 3998-4006 [PMID:8831765]
mGlu1 receptor/Metabotropic glutamate receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4477] [GtoPdb: 289] [UniProtKB: P23385]
GtoPdb - - 7.7 pKd - - - Mol Pharmacol (2003) 63: 1082-93 [PMID:12695537];
J Biol Chem (2003) 278: 8340-7 [PMID:12509432]
ChEMBL Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells B 8 pKi 10 nM Ki J. Med. Chem. (2002) 45: 3171-3183 [PMID:12109902]
ChEMBL Concentration for half maximal activation of metabotropic glutamate mGluR1b in human B 4.79 pEC50 16400 nM EC50 J. Med. Chem. (1995) 38: 1417-1426 [PMID:7738999]
ChEMBL Concentration for half maximal activation of metabotropic glutamate mGluR1b in rat B 5.6 pEC50 2500 nM EC50 J. Med. Chem. (1995) 38: 1417-1426 [PMID:7738999]
ChEMBL Concentration for half maximal activation of metabotropic glutamate mGluR1c in rat B 6.12 pEC50 750 nM EC50 J. Med. Chem. (1995) 38: 1417-1426 [PMID:7738999]
ChEMBL Concentration for half maximal activation of metabotropic glutamate mGluR1a in rat B 6.15 pEC50 700 nM EC50 J. Med. Chem. (1995) 38: 1417-1426 [PMID:7738999]
ChEMBL Concentration for half maximal activation of metabotropic glutamate mGluR1a in rat B 6.7 pEC50 200 nM EC50 J. Med. Chem. (1995) 38: 1417-1426 [PMID:7738999]
mGlu3 receptor/Metabotropic glutamate receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2888] [GtoPdb: 291] [UniProtKB: Q14832]
ChEMBL Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3). F 4.4 pKi 40000 nM Ki J. Med. Chem. (2000) 43: 2609-2645 [PMID:10893301]
mGlu3 receptor/Metabotropic glutamate receptor 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3067] [GtoPdb: 291] [UniProtKB: P31422]
ChEMBL Concentration for half maximal activation of metabotropic glutamate mGluR3 in rat B 4.4 pEC50 40000 nM EC50 J. Med. Chem. (1995) 38: 1417-1426 [PMID:7738999]
mGlu4 receptor/Metabotropic glutamate receptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2787] [GtoPdb: 292] [UniProtKB: P31423]
ChEMBL Concentration for half maximal activation of metabotropic glutamate mGluR4a in rat B 4 pEC50 >100000 nM EC50 J. Med. Chem. (1995) 38: 1417-1426 [PMID:7738999]
mGlu5 receptor/Metabotropic glutamate receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
ChEMBL Agonist potency against cloned metabotropic glutamate receptor 5 F 7.26 pKi 55 nM Ki J. Med. Chem. (2000) 43: 2609-2645 [PMID:10893301]
ChEMBL Agonist activity at mGlu5 receptor (unknown origin) expressed in CHO cells assessed as increase in Gq-mediated PI hydrolysis after 45 mins by yttrium scintillation proximity assay B 6.2 pEC50 630 nM EC50 J Med Chem (2018) 61: 9841-9878 [PMID:29939744]
ChEMBL Concentration for half maximal activation of metabotropic glutamate mGluR5a in human B 6.82 pEC50 150 nM EC50 J. Med. Chem. (1995) 38: 1417-1426 [PMID:7738999]
mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424]
ChEMBL Concentration for half maximal activation of metabotropic glutamate mGluR5a in rat B 6.52 pEC50 300 nM EC50 J. Med. Chem. (1995) 38: 1417-1426 [PMID:7738999]
ChEMBL Concentration for half maximal activation of metabotropic glutamate mGluR5a in rat B 6.7 pEC50 200 nM EC50 J. Med. Chem. (1995) 38: 1417-1426 [PMID:7738999]
ChEMBL Concentration for half maximal activation of metabotropic glutamate mGluR5b in rat B 6.7 pEC50 200 nM EC50 J. Med. Chem. (1995) 38: 1417-1426 [PMID:7738999]
mGlu8 receptor/Metabotropic glutamate receptor 8 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4626] [GtoPdb: 296] [UniProtKB: P47743]
ChEMBL Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouse B 4 pEC50 >100000 nM EC50 J. Med. Chem. (1995) 38: 1417-1426 [PMID:7738999]

ChEMBL data shown on this page come from version 28:

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]