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ChEMBL ligand: CHEMBL458273 |
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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 | Inhibition of [3H]-D-Asp uptake at human EAAT1 expressed in HEK293 cells measured after 3 mins by TopCount method | B | 4.29 | pIC50 | 51286.14 | 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 | 4.29 | pIC50 | 51000 | nM | IC50 | J Med Chem (2016) 59: 8771-8786 [PMID:27636002] |
ChEMBL | Inhibition of human EAAT1 transfected in mouse C17.2 cells assessed as inhibition of [3H]-D-aspartate uptake incubated for 5 mins by liquid scintillation counting analysis | B | 5.06 | pIC50 | 8700 | nM | IC50 | ACS Med Chem Lett (2020) 11: 2212-2220 [PMID:33214831] |
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 expressed in HEK293 cells measured after 3 mins by TopCount method | B | 4.37 | pIC50 | 42657.95 | 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 | 4.38 | pIC50 | 42000 | nM | IC50 | J Med Chem (2016) 59: 8771-8786 [PMID:27636002] |
ChEMBL | Inhibition of human EAAT2 transfected in mouse C17.2 cells assessed as inhibition of [3H]-D-aspartate uptake incubated for 5 mins by liquid scintillation counting analysis | B | 5 | pIC50 | 10000 | nM | IC50 | ACS Med Chem Lett (2020) 11: 2212-2220 [PMID:33214831] |
Excitatory amino acid transporter 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2721] [GtoPdb: 870] [UniProtKB: P43005] | ||||||||
GtoPdb | - | - | 6.1 | pKi | 800 | nM | Ki | Neuropharmacology (2005) 49: 850-61 [PMID:16183084] |
ChEMBL | Inhibition of [3H]-D-Asp uptake at human EAAT3 expressed in HEK293 cells measured after 3 mins by TopCount method | B | 4.96 | pIC50 | 11000 | 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 | 4.96 | pIC50 | 10964.78 | nM | IC50 | J Med Chem (2016) 59: 8771-8786 [PMID:27636002] |
ChEMBL | Inhibition of human EAAT3 transfected in mouse C17.2 cells assessed as inhibition of [3H]-D-aspartate uptake incubated for 5 mins by liquid scintillation counting analysis | B | 6.1 | pIC50 | 800 | nM | IC50 | ACS Med Chem Lett (2020) 11: 2212-2220 [PMID:33214831] |
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]