quisqualate [Ligand Id: 1372] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL279956 (Quisqualate, quisqualic acid) |
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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] | ||||||||
| GtoPdb | - | - | 5.3 | pIC50 | 5000 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 2680-3 [PMID:20303751] |
| 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: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: P35439, Q00959, Q00960, Q00961, Q62645, Q8VHN2, Q9R1M7] | ||||||||
| 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: 444, 445, 447, 446] [UniProtKB: P23818, P23819, Q9Z2W8, Q9Z2W9] | ||||||||
| 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: 444, 445, 446, 447] [UniProtKB: P19490, P19491, P19492, P19493] | ||||||||
| 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: 450, 451, 452, 453, 454] [UniProtKB: P22756, P42260, P42264, Q01812, Q63273] | ||||||||
| 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 | - | - | 8 | pKi | - | - | - |
Mol Pharmacol (2003) 63: 1082-93 [PMID:12695537]; J Neurochem (2000) 75: 2590-601 [PMID:11080213] |
| 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] | ||||||||
| GtoPdb | - | - | 7.5 | pIC50 | - | - | - | J Neurochem (2000) 75: 2590-601 [PMID:11080213] |
| 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 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]
