ChEMBL ligand: CHEMBL458273
Excitatory amino acid transporter 1 in Human [ChEMBL: CHEMBL3085] [GtoPdb: 868] [UniProtKB: P43003] There should be some charts here, you may need to enable JavaScript!
Excitatory amino acid transporter 2 in Human [ChEMBL: CHEMBL4973] [GtoPdb: 869] [UniProtKB: P43004] There should be some charts here, you may need to enable JavaScript!
Excitatory amino acid transporter 3 in Human [ChEMBL: CHEMBL2721] [GtoPdb: 870] [UniProtKB: P43005] 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 [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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]