ChEMBL ligand: CHEMBL474133
Excitatory amino acid transporter 1 in Human [ChEMBL: CHEMBL3085] [GtoPdb: 868] [UniProtKB: P43003] Excitatory amino acid transporter 1 in Rat [ChEMBL: CHEMBL4190] [GtoPdb: 868] [UniProtKB: P24942] There should be some charts here, you may need to enable JavaScript!

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 by [3H]D-Asp uptake assay	B	6.18	pIC50	660.69	nM	IC50	J Med Chem (2010) 53: 7180-7191 [PMID:20857912]
ChEMBL	Displacement of [3H]D-Asp from human EAAT1 receptor expressed in HEK293 cells	B	6.18	pIC50	660.69	nM	IC50	J Med Chem (2009) 52: 912-915 [PMID:19161278]
ChEMBL	Inhibition of EAAT1 (unknown origin) stably expressed in HEK293 cells assessed as reduction in [14C]glutamate uptake incubated for 5 mins by microbeta scintillation counting method	B	6.18	pIC50	660	nM	IC50	J Med Chem (2020) 63: 3834-3867 [PMID:31774679]
ChEMBL	Inhibition of human EAAT1 expressed in HEK293 cells assessed as inhibition of 3[H]-D-Aspartate uptake after 6 mins by scintillation counting method	B	6.18	pIC50	660	nM	IC50	J Med Chem (2012) 55: 5403-5412 [PMID:22594609]
ChEMBL	Displacement of [3H]D-Asp from human EAAT1 receptor expressed in HEK293 cells	B	6.18	pIC50	660	nM	IC50	J Med Chem (2009) 52: 912-915 [PMID:19161278]
ChEMBL	Inhibition of human EAAT1 expressed in HEK293 cells by [3H]D-Asp uptake assay	B	6.18	pIC50	660	nM	IC50	J Med Chem (2010) 53: 7180-7191 [PMID:20857912]
GtoPdb	-	-	6.9	pIC50	120	nM	IC50	J Med Chem (2009) 52: 912-5 [PMID:19161278]
ChEMBL	Activity at human EAAT1 expressed in HEK293 cells assessed as inhibition of Glu-induced fluorescent response by FLIPR membrane potential blue assay	B	6.91	pIC50	123.03	nM	IC50	J Med Chem (2009) 52: 912-915 [PMID:19161278]
ChEMBL	Activity at human EAAT1 expressed in HEK293 cells assessed as inhibition of Glu-induced fluorescent response by FLIPR membrane potential blue assay	B	6.92	pIC50	120	nM	IC50	J Med Chem (2009) 52: 912-915 [PMID:19161278]
Excitatory amino acid transporter 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4190] [GtoPdb: 868] [UniProtKB: P24942]
ChEMBL	Activity at rat EAAT1 expressed in TSA201 cells assessed as inhibition of Glu-induced fluorescent response by FLIPR membrane potential blue assay	B	6.01	pIC50	970	nM	IC50	J Med Chem (2009) 52: 912-915 [PMID:19161278]
ChEMBL	Activity at rat EAAT1 expressed in TSA201 cells assessed as inhibition of Glu-induced fluorescent response by FLIPR membrane potential blue assay	B	6.02	pIC50	954.99	nM	IC50	J Med Chem (2009) 52: 912-915 [PMID:19161278]

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]