ChEMBL ligand: CHEMBL1628669 (WAY-213613)
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!
Excitatory amino acid transporter 4 in Rat [ChEMBL: CHEMBL3700] [GtoPdb: 871] [UniProtKB: O35921] 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	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 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]