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ChEMBL ligand: CHEMBL1628669 (WAY-213613) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Excitatory amino acid transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3085] [GtoPdb: 868] [UniProtKB: P43003] | ||||||||
ChEMBL | Inhibitory concentration against glutamate uptake in HEK cells expressing human Excitatory amino acid transporter 1 | B | 5.3 | pIC50 | 5000 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 4985-4988 [PMID:16165356] |
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 | 6.07 | pIC50 | 860 | 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 | 6.07 | pIC50 | 851.14 | 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 | Inhibitory concentration against glutamate uptake in oocytes expressing in human Excitatory amino acid transporter 2 | B | 6.89 | pIC50 | 130 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 4985-4988 [PMID:16165356] |
ChEMBL | Inhibitory concentration against glutamate uptake in HEK cells expressing human Excitatory amino acid transporter 2 | B | 7.1 | pIC50 | 80 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 4985-4988 [PMID:16165356] |
GtoPdb | - | - | 7.1 | pIC50 | 85 | nM | IC50 | Mol Pharmacol (2005) 68: 974-82 [PMID:16014807] |
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 | 7.15 | pIC50 | 71 | 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 | 7.15 | pIC50 | 70.79 | 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 | Inhibitory concentration against glutamate uptake in HEK cells expressing human Excitatory amino acid transporter 3 | B | 5.42 | pIC50 | 3800 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 4985-4988 [PMID:16165356] |
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 | 5.72 | pIC50 | 1900 | 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 | 5.73 | pIC50 | 1862.09 | 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 | 5.82 | pIC50 | 1500 | 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 | 5.97 | pIC50 | 1071.52 | nM | IC50 | J Med Chem (2018) 61: 7741-7753 [PMID:30011368] |
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]