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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
