DL-TBOA [Ligand Id: 4631] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL79140 (L-Threo-Benzyloxy Aspartate)
  • 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 Human [GtoPdb: 871] [UniProtKB: P48664]
  • Excitatory amino acid transporter 4 in Rat [ChEMBL: CHEMBL3700] [GtoPdb: 871] [UniProtKB: O35921]
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  • Excitatory amino acid transporter 5 in Human [GtoPdb: 872] [UniProtKB: O00341]
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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 Concentration required for blocking [14C]glutamate uptake in COS-1 cells expressing human Excitatory amino acid transporter 1 B 4.64 pIC50 23000 nM IC50 Bioorg. Med. Chem. Lett. (2000) 10: 2407-2410 [PMID:11078189]
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 5.68 pIC50 2100 nM IC50 J Med Chem (2018) 61: 7741-7753 [PMID:30011368]
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 5.68 pIC50 2089.3 nM IC50 J Med Chem (2018) 61: 7741-7753 [PMID:30011368]
ChEMBL Inhibition of [3H]-D-Asp uptake at human EAAT1 expressed in HEK293 cells measured after 3 mins by TopCount method B 5.79 pIC50 1621.81 nM IC50 J Med Chem (2016) 59: 8771-8786 [PMID:27636002]
ChEMBL Inhibition of [3H]-D-Asp uptake at human EAAT1 expressed in HEK293 cells measured after 3 mins by TopCount method B 5.8 pIC50 1600 nM IC50 J Med Chem (2016) 59: 8771-8786 [PMID:27636002]
Excitatory amino acid transporter 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4973] [GtoPdb: 869] [UniProtKB: P43004]
ChEMBL Concentration required for blocking [14C]glutamate uptake in COS-1 cells expressing human Excitatory amino acid transporter 2 B 4.19 pIC50 64000 nM IC50 Bioorg. Med. Chem. Lett. (2000) 10: 2407-2410 [PMID:11078189]
ChEMBL Concentration required for blocking [14C]glutamate uptake in COS-1 cells expressing human Excitatory amino acid transporter 2 B 5.42 pIC50 3800 nM IC50 Bioorg. Med. Chem. Lett. (2000) 10: 2407-2410 [PMID:11078189]
ChEMBL Inhibition of human GLT1 expressed in Xenopus laevis Oocytes assessed as reduction of [3H]-glutamate uptake after 10 mins by scintillation counting B 5.42 pIC50 3800 nM IC50 J. Med. Chem. (2010) 53: 7236-7250 [PMID:20812729]
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 5.72 pIC50 1905.46 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 5.72 pIC50 1900 nM IC50 J Med Chem (2018) 61: 7741-7753 [PMID:30011368]
ChEMBL Inhibition of [3H]-D-Asp uptake at human EAAT2 expressed in HEK293 cells measured after 3 mins by TopCount method B 6.02 pIC50 960 nM IC50 J Med Chem (2016) 59: 8771-8786 [PMID:27636002]
ChEMBL Inhibition of [3H]-D-Asp uptake at human EAAT2 expressed in HEK293 cells measured after 3 mins by TopCount method B 6.02 pIC50 954.99 nM IC50 J Med Chem (2016) 59: 8771-8786 [PMID:27636002]
Excitatory amino acid transporter 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2721] [GtoPdb: 870] [UniProtKB: P43005]
ChEMBL Concentration required for blocking [14C]glutamate uptake in COS-1 cells expressing human Excitatory amino acid transporter 3 B 4.68 pIC50 21000 nM IC50 Bioorg. Med. Chem. Lett. (2000) 10: 2407-2410 [PMID:11078189]
GtoPdb - - 5.1 pIC50 8000 nM IC50 Bioorg. Med. Chem. Lett. (2000) 10: 2407-10 [PMID:11078189]
ChEMBL Concentration required for blocking [14C]glutamate uptake in COS-1 cells expressing human Excitatory amino acid transporter 3 B 5.15 pIC50 7000 nM IC50 Bioorg. Med. Chem. Lett. (2000) 10: 2407-2410 [PMID:11078189]
ChEMBL Inhibition of [14C]glutamate uptake at human EAAT3 expressed in african green monkey COS1 cells B 5.15 pIC50 7000 nM IC50 Bioorg. Med. Chem. (2008) 16: 7740-7748 [PMID:18650095]
ChEMBL Inhibition of human EAAC1 expressed in Xenopus laevis Oocytes assessed as reduction of [3H]-glutamate uptake after 10 mins by scintillation counting B 5.15 pIC50 7000 nM IC50 J. Med. Chem. (2010) 53: 7236-7250 [PMID:20812729]
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 5.42 pIC50 3801.89 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 5.42 pIC50 3800 nM IC50 J Med Chem (2018) 61: 7741-7753 [PMID:30011368]
ChEMBL Inhibition of [3H]-D-Asp uptake at human EAAT3 expressed in HEK293 cells measured after 3 mins by TopCount method B 5.43 pIC50 3715.35 nM IC50 J Med Chem (2016) 59: 8771-8786 [PMID:27636002]
ChEMBL Inhibition of [3H]-D-Asp uptake at human EAAT3 expressed in HEK293 cells measured after 3 mins by TopCount method B 5.43 pIC50 3700 nM IC50 J Med Chem (2016) 59: 8771-8786 [PMID:27636002]
Excitatory amino acid transporter 4 in Human [GtoPdb: 871] [UniProtKB: P48664]
GtoPdb - - 5.4 pKi 4400 nM Ki J. Neurochem. (2001) 79: 297-302 [PMID:11677257]
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 5.64 pIC50 2300 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 5.64 pIC50 2290.87 nM IC50 J Med Chem (2018) 61: 7741-7753 [PMID:30011368]
Excitatory amino acid transporter 5 in Human [GtoPdb: 872] [UniProtKB: O00341]
GtoPdb - - 5.5 pKi 3200 nM Ki J. Neurochem. (2001) 79: 297-302 [PMID:11677257]

ChEMBL data shown on this page come from version 27:

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]