ChEMBL ligand: CHEMBL473104
GAT1 in Human [GtoPdb: 929] [UniProtKB: P30531] GAT1/GABA transporter 1 in Mouse [ChEMBL: CHEMBL5445] [GtoPdb: 929] [UniProtKB: P31648] GAT1/GABA transporter 1 in Rat [ChEMBL: CHEMBL4054] [GtoPdb: 929] [UniProtKB: P23978] 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
GAT1 in Human [GtoPdb: 929] [UniProtKB: P30531]
GtoPdb	-	-	7.4	pIC50	40	nM	IC50	Eur J Pharmacol (1994) 269: 219-24 [PMID:7851497]
GAT1/GABA transporter 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5445] [GtoPdb: 929] [UniProtKB: P31648]
ChEMBL	Inhibition of NO711 binding to mouse GAT1 expressed in HEK293 cell membranes assessed as reduction in NO711 binding at incubated for 4 hrs in presence of NO711 by LC-ESI-MS/MS analysis relative to control	B	7.58	pKd	26.5	nM	Kd	Bioorg Med Chem (2019) 27: 2753-2763 [PMID:31097402]
ChEMBL	Binding affinity to mouse GAT1 expressed in HEK293 cells membranes using LC-ESI-MS/MS analysis by [2H10]NO711 binding inhibition assay	B	6.28	pIC50	<=530	nM	IC50	J Med Chem (2013) 56: 1323-1340 [PMID:23336362]
ChEMBL	Inhibition of mouse GAT1 mediated [3]GABA uptake expressed in HEK293 cells after 3 mins by scintillation counting	B	6.74	pIC50	180	nM	IC50	Bioorg Med Chem Lett (2016) 26: 417-423 [PMID:26706177]
ChEMBL	Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK cells	B	6.83	pIC50	147.91	nM	IC50	Eur J Med Chem (2008) 43: 2404-2411 [PMID:18395300]
ChEMBL	Inhibition of mouse GAT1 expressed in HEK293 cell line assessed as inhibition of [3H]GABA uptake measured after 35 mins by liquid scintillation method	B	6.83	pIC50	147.91	nM	IC50	Eur J Med Chem (2020) 188: 111920-111920 [PMID:31901745]
ChEMBL	Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 25 mins by scintillation counting analysis	B	7.4	pIC50	40	nM	IC50	J Med Chem (2013) 56: 1323-1340 [PMID:23336362]
ChEMBL	Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 25 mins by scintillation counting analysis	B	7.4	pIC50	39.81	nM	IC50	J Med Chem (2013) 56: 1323-1340 [PMID:23336362]
GAT1/GABA transporter 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4054] [GtoPdb: 929] [UniProtKB: P23978]
ChEMBL	Inhibition of GAT-1 in rat brain homogenate assessed as decrease in [3H]GABA uptake preincubated for 8 mins followed by [3H]GABA addition and measured after 8 mins by scintillation counting analysis	B	7.4	pIC50	40	nM	IC50	Bioorg Med Chem (2019) 27: 1232-1245 [PMID:30777661]

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]