L-glutamic acid [Ligand Id: 1369] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL575060 (E 620, E-620, E620, FEMA NO. 3285, Glutamic acid, Glutamic acid, l-, Glutamidex, INS-620, INS NO.620, L-2-amino-pentanedioic acid, L-alpha-aminoglutaric acid, L-glutamate, L-glutamic acid, NSC-143503)
  • Excitatory amino acid transporter 1 in Human [ChEMBL: CHEMBL3085] [GtoPdb: 868] [UniProtKB: P43003]
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  • Excitatory amino acid transporter 2 in Human [ChEMBL: CHEMBL4973] [GtoPdb: 869] [UniProtKB: P43004]
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  • Excitatory amino acid transporter 3 in Human [ChEMBL: CHEMBL2721] [GtoPdb: 870] [UniProtKB: P43005]
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  • Excitatory amino acid transporter 4 in Rat [ChEMBL: CHEMBL3700] [GtoPdb: 871] [UniProtKB: O35921]
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  • Glutamate racemase in Lactobacillus fermentum [ChEMBL: CHEMBL3353] [UniProtKB: Q03469]
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  • GluA1/Glutamate receptor ionotropic, AMPA 1 in Human [ChEMBL: CHEMBL2009] [GtoPdb: 444] [UniProtKB: P42261]
  • GluA1/Glutamate receptor ionotropic, AMPA 1 in Rat [ChEMBL: CHEMBL3753] [GtoPdb: 444] [UniProtKB: P19490]
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  • GluA2/Glutamate receptor ionotropic, AMPA 2 in Human [ChEMBL: CHEMBL4016] [GtoPdb: 445] [UniProtKB: P42262]
  • GluA2/Glutamate receptor ionotropic, AMPA 2 in Rat [ChEMBL: CHEMBL3503] [GtoPdb: 445] [UniProtKB: P19491]
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  • GluA3/Glutamate receptor ionotropic, AMPA 3 in Human [ChEMBL: CHEMBL3595] [GtoPdb: 446] [UniProtKB: P42263]
  • GluA3/Glutamate receptor ionotropic, AMPA 3 in Rat [ChEMBL: CHEMBL3504] [GtoPdb: 446] [UniProtKB: P19492]
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  • GluA4/Glutamate receptor ionotropic, AMPA 4 in Human [ChEMBL: CHEMBL3190] [GtoPdb: 447] [UniProtKB: P48058]
  • GluA4/Glutamate receptor ionotropic, AMPA 4 in Rat [ChEMBL: CHEMBL3505] [GtoPdb: 447] [UniProtKB: P19493]
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  • GluK1/Glutamate receptor ionotropic kainate 1 in Human [ChEMBL: CHEMBL1918] [GtoPdb: 450] [UniProtKB: P39086]
  • 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 Human [ChEMBL: CHEMBL3683] [GtoPdb: 451] [UniProtKB: Q13002]
  • 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 Human [ChEMBL: CHEMBL3684] [GtoPdb: 452] [UniProtKB: Q13003]
  • GluK3/Glutamate receptor ionotropic kainate 3 in Rat [ChEMBL: CHEMBL3744] [GtoPdb: 452] [UniProtKB: P42264]
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  • GluK5/Glutamate receptor ionotropic kainate 5 in Human [ChEMBL: CHEMBL2675] [GtoPdb: 454] [UniProtKB: Q16478]
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  • glutathione-disulfide reductase/Glutathione reductase in Human [ChEMBL: CHEMBL2755] [GtoPdb: 2613] [UniProtKB: P00390]
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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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  • 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/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 Human [ChEMBL: CHEMBL2736] [GtoPdb: 292] [UniProtKB: Q14833]
  • 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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  • mGlu6 receptor/Metabotropic glutamate receptor 6 in Human [ChEMBL: CHEMBL4573] [GtoPdb: 294] [UniProtKB: O15303]
  • mGlu6 receptor/Metabotropic glutamate receptor 6 in Rat [ChEMBL: CHEMBL3842] [GtoPdb: 294] [UniProtKB: P35349]
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  • mGlu7 receptor/Metabotropic glutamate receptor 7 in Human [ChEMBL: CHEMBL3777] [GtoPdb: 295] [UniProtKB: Q14831]
  • mGlu7 receptor/Metabotropic glutamate receptor 7 in Rat [ChEMBL: CHEMBL3879] [GtoPdb: 295] [UniProtKB: P35400]
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  • mGlu8 receptor/Metabotropic glutamate receptor 8 in Human [ChEMBL: CHEMBL3228] [GtoPdb: 296] [UniProtKB: O00222]
  • mGlu8 receptor/Metabotropic glutamate receptor 8 in Mouse [ChEMBL: CHEMBL4626] [GtoPdb: 296] [UniProtKB: P47743]
  • mGlu8 receptor/Metabotropic glutamate receptor 8 in Rat [ChEMBL: CHEMBL2718] [GtoPdb: 296] [UniProtKB: P70579]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Excitatory amino acid transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3085] [GtoPdb: 868] [UniProtKB: P43003]
ChEMBL Inhibition of [3H]D-Asp uptake at EAAT1 in HEK293 cells B 4.46 pKi 35000 nM Ki J Med Chem (2008) 51: 4085-4092 [PMID:18578477]
ChEMBL Inhibition of [3H]D-Asp uptake at EAAT1 in HEK293 cells B 4.5 pKi 31622.78 nM Ki J Med Chem (2008) 51: 4085-4092 [PMID:18578477]
ChEMBL Inhibition of human EAAT1 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method B 4.94 pIC50 11481.54 nM IC50 J Med Chem (2018) 61: 7741-7753 [PMID:30011368]
ChEMBL Inhibition of human EAAT1 transfected in HEK293 cells assessed as inhibition of [3H]-D-aspartate uptake incubated for 4 mins by TopCount scintillation counting analysis B 4.95 pIC50 11220.18 nM IC50 ACS Med Chem Lett (2020) 11: 2212-2220 [PMID:33214831]
ChEMBL Inhibition of human EAAT1 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method B 4.96 pIC50 11000 nM IC50 J Med Chem (2018) 61: 7741-7753 [PMID:30011368]
ChEMBL Inhibition of human EAAT1 transfected in HEK293 cells assessed as inhibition of [3H]-D-aspartate uptake incubated for 4 mins by TopCount scintillation counting analysis B 4.96 pIC50 11000 nM IC50 ACS Med Chem Lett (2020) 11: 2212-2220 [PMID:33214831]
ChEMBL Substrate uptake by the Excitatory Amino Acid Transporter 1 (EAAT1, SLC1A3) as assessed by the fluorescent FLIPR membrane potential dye in HEK-293 JumpIN-SLC1A3 cells (PubChem AID: 1745864) F 4.8 pEC50 16000 nM EC50 Membrane potential based transport assay for SLC1A3 using HEK293 JumpIn SLC1A3 OE cells
Excitatory amino acid transporter 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4973] [GtoPdb: 869] [UniProtKB: P43004]
ChEMBL Inhibition of [3H]D-Asp uptake at human EAAT2 in HEK293 cells B 4.2 pKi 63095.73 nM Ki J Med Chem (2008) 51: 4085-4092 [PMID:18578477]
ChEMBL Inhibition of [3H]D-Asp uptake at human EAAT2 in HEK293 cells B 4.21 pKi 62000 nM Ki J Med Chem (2008) 51: 4085-4092 [PMID:18578477]
ChEMBL Inhibition of human EAAT2 transfected in HEK293 cells assessed as inhibition of [3H]-D-aspartate uptake incubated for 4 mins by TopCount scintillation counting analysis B 4.1 pIC50 80000 nM IC50 ACS Med Chem Lett (2020) 11: 2212-2220 [PMID:33214831]
ChEMBL Inhibition of human EAAT2 transfected in HEK293 cells assessed as inhibition of [3H]-D-aspartate uptake incubated for 4 mins by TopCount scintillation counting analysis B 4.1 pIC50 79432.82 nM IC50 ACS Med Chem Lett (2020) 11: 2212-2220 [PMID:33214831]
ChEMBL Inhibition of human EAAT2 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method B 4.28 pIC50 52480.75 nM IC50 J Med Chem (2018) 61: 7741-7753 [PMID:30011368]
ChEMBL Inhibition of human EAAT2 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method B 4.28 pIC50 52000 nM IC50 J Med Chem (2018) 61: 7741-7753 [PMID:30011368]
Excitatory amino acid transporter 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2721] [GtoPdb: 870] [UniProtKB: P43005]
ChEMBL Inhibition of [3H]D-Asp uptake at human EAAT3 in HEK293 cells B 4.3 pKi 50118.72 nM Ki J Med Chem (2008) 51: 4085-4092 [PMID:18578477]
ChEMBL Inhibition of [3H]D-Asp uptake at human EAAT3 in HEK293 cells B 7.29 pKi 51 nM Ki J Med Chem (2008) 51: 4085-4092 [PMID:18578477]
ChEMBL Inhibition of human EAAT3 transfected in HEK293 cells assessed as inhibition of [3H]-D-aspartate uptake incubated for 4 mins by TopCount scintillation counting analysis B 4.3 pIC50 50118.72 nM IC50 ACS Med Chem Lett (2020) 11: 2212-2220 [PMID:33214831]
ChEMBL Inhibition of human EAAT3 transfected in HEK293 cells assessed as inhibition of [3H]-D-aspartate uptake incubated for 4 mins by TopCount scintillation counting analysis B 4.3 pIC50 50000 nM IC50 ACS Med Chem Lett (2020) 11: 2212-2220 [PMID:33214831]
ChEMBL Inhibition of human EAAT3 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method B 4.49 pIC50 32359.37 nM IC50 J Med Chem (2018) 61: 7741-7753 [PMID:30011368]
ChEMBL Inhibition of human EAAT3 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method B 4.49 pIC50 32000 nM IC50 J Med Chem (2018) 61: 7741-7753 [PMID:30011368]
Excitatory amino acid transporter 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3700] [GtoPdb: 871] [UniProtKB: O35921]
ChEMBL Inhibition of rat EAAT4 expressed in tsA201 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method B 4.88 pIC50 13182.57 nM IC50 J Med Chem (2018) 61: 7741-7753 [PMID:30011368]
ChEMBL Inhibition of rat EAAT4 expressed in tsA201 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method B 4.89 pIC50 13000 nM IC50 J Med Chem (2018) 61: 7741-7753 [PMID:30011368]
ChEMBL Inhibition of rat EAAT4 transfected in human tsA201 cells assessed as inhibition of [3H]-D-aspartate uptake incubated for 4 mins by TopCount scintillation counting analysis B 4.9 pIC50 12589.25 nM IC50 ACS Med Chem Lett (2020) 11: 2212-2220 [PMID:33214831]
ChEMBL Inhibition of rat EAAT4 transfected in human tsA201 cells assessed as inhibition of [3H]-D-aspartate uptake incubated for 4 mins by TopCount scintillation counting analysis B 4.92 pIC50 12000 nM IC50 ACS Med Chem Lett (2020) 11: 2212-2220 [PMID:33214831]
GluN2D/GluN3B/GluN1/GluN2A/GluN2B/GluN2C/GluN3A/Glutamate [NMDA] receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094124] [GtoPdb: 459, 461, 455, 456, 457, 458, 460] [UniProtKB: O15399, O60391, Q05586, Q12879, Q13224, Q14957, Q8TCU5]
ChEMBL Antagonist activity at NMDA receptor (unknwon origin) F 7.15 pIC50 70 nM IC50 J Med Chem (2011) 54: 2529-2591 [PMID:21413808]
ChEMBL Binding affinity to NMDA receptor (unknown origin) B 7.15 pIC50 70 nM IC50 Eur J Med Chem (2021) 209: 112872-112872 [PMID:33035923]
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 Displacement of L-[3H]glutamate from N-methyl-D-aspartate glutamate receptor in rat brain synaptic membranes B 6.06 pKi 870 nM Ki Bioorg Med Chem Lett (2005) 15: 2279-2283 [PMID:15837309]
ChEMBL Displacement of [3H]CGP 39653 from NMDA receptor agonist binding site in Wistar rat cerebral cortex after 20 mins B 6.43 pKi 370 nM Ki Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL Displacement of [3H]CGP39653 from NMDA receptor in rat brain membranes B 6.54 pKi 290 nM Ki Bioorg Med Chem (2009) 17: 242-250 [PMID:19042134]
ChEMBL Displacement of [3H]CGP39653 from NMDA receptor in Sprague-Dawley rat brain membranes B 6.7 pKi 200 nM Ki J Med Chem (2010) 53: 4110-4118 [PMID:20408529]
ChEMBL Displacement of [3H]CGP39653 from NMDA receptor in rat brain cortex after 60 mins by Packard TopCount microplate scintillator counting B 6.7 pKi 200 nM Ki J Med Chem (2013) 56: 1614-1628 [PMID:23414088]
ChEMBL Displacement of [3H]CGP-39653 from NMDA receptor in rat brain cortical membranes B 6.7 pKi 200 nM Ki Medchemcomm (2011) 2: 1120-1124
ChEMBL Displacement of [3H]CGP39653 from NMDA receptor in rat cortical synaptosomes B 6.7 pKi 200 nM Ki Medchemcomm (2015) 6: 1285-1292
ChEMBL Binding affinity towards NMDA receptor by displacement of [3H]CGP-39653 radioligand. B 6.7 pKi 200 nM Ki J Med Chem (2001) 44: 2507-2510 [PMID:11472204]
ChEMBL Displacement of [3H]CGP39653 from NMDA receptor in rat brain synaptic cortical membranes after 60 mins by scintillation counting method B 6.7 pKi 200 nM Ki J Med Chem (2019) 62: 4467-4482 [PMID:30943028]
ChEMBL Displacement of [3H]CGP-39653 from rat NMDA receptor expressed in BHK cells B 6.7