DL-threo-β-hydroxyaspartate [Ligand Id: 4497] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1231330
  • 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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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 human EAAT1 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method B 5.41 pIC50 3900 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 5.41 pIC50 3890.45 nM IC50 J Med Chem (2018) 61: 7741-7753 [PMID:30011368]
Excitatory amino acid transporter 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4973] [GtoPdb: 869] [UniProtKB: P43004]
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 5.02 pIC50 9600 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 5.02 pIC50 9549.93 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 human EAAT3 expressed in HEK293 cells assessed as reduction in [3H]-D-Asp uptake incubated for 4 mins by scintillation counting method B 5.02 pIC50 9600 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 5.02 pIC50 9549.93 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 5.55 pIC50 2818.38 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 5.55 pIC50 2800 nM IC50 J Med Chem (2018) 61: 7741-7753 [PMID:30011368]

ChEMBL data shown on this page come from version 32:

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]