ChEMBL ligand: CHEMBL1027 (A-70569-1, ABBOTT-70569, ABBOTT-70569-1, ABBOTT-705691 FREE BASE, ABBOTT-70569 FREE BASE, ABT-569, ABT-569 FREE BASE, Gabitril, NNC-05-0328, NNC-050328 FREE BASE, NO-05-0328, NO-050328 FREE BASE, Tiagabine)
GAT1/GABA transporter 1 in Human [ChEMBL: CHEMBL1903] [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!
BGT1/GABA transporter 2 in Mouse [ChEMBL: CHEMBL4228] [GtoPdb: 932] [UniProtKB: P31651] 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/GABA transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1903] [GtoPdb: 929] [UniProtKB: P30531]
ChEMBL	Competitive inhibition of human GAT1 expressed in COS cells assessed as reduction in [2H6]GABA uptake by measuring [2H6]GABA Kd(app) at 1 uM preincubated for 25 mins followed by [2H6]GABA addition and measured after 4 mins by liquid scintillation counting method (Rvb = 28.3 +/- 1.5 nM)	B	6.83	pKd	146.8	nM	Kd	J Med Chem (2018) 61: 10310-10332 [PMID:30376325]
ChEMBL	Competitive inhibition of human GAT1 expressed in COS cells assessed as reduction in [2H6]GABA uptake by measuring [2H6]GABA Kd(app) at 100 nM preincubated for 25 mins followed by [2H6]GABA addition and measured after 4 mins by liquid scintillation counting method (Rvb = 28.3 +/- 1.5 nM)	B	7.39	pKd	40.5	nM	Kd	J Med Chem (2018) 61: 10310-10332 [PMID:30376325]
ChEMBL	Binding affinity to human GAT1 expressed in HEK293 cells using NO71156 as unlabelled marker by LC-ESI-MS-MS based competitive MS binding assay	B	7.32	pKi	47.86	nM	Ki	Bioorg Med Chem (2015) 23: 1284-1306 [PMID:25698617]
ChEMBL	Displacement of [3H]Tiagabine from human recombinant GAT1 expressed in HEK293 cells by equilibrium binding assay	B	7.77	pKi	16.98	nM	Ki	Bioorg Med Chem Lett (2011) 21: 602-605 [PMID:21134748]
ChEMBL	Inhibition of human GAT1 expressed in HEK293 cells by [3H]GABA uptake assay	B	6.42	pIC50	380.19	nM	IC50	Bioorg Med Chem (2015) 23: 1284-1306 [PMID:25698617]
ChEMBL	Inhibition of GAT1 transport activity	B	6.55	pIC50	280	nM	IC50	Bioorg Med Chem Lett (2006) 16: 225-227 [PMID:16246548]
ChEMBL	Inhibition of NO711 binding to human GAT1 expressed in COS cell membranes preincubated for 25 mins by LC-ESI-MS/MS analysis	B	6.81	pIC50	154.88	nM	IC50	J Med Chem (2018) 61: 10310-10332 [PMID:30376325]
ChEMBL	Inhibitory activity against human GABA transporter-1 (hGAT1)	B	7.15	pIC50	70	nM	IC50	J Med Chem (1994) 37: 2334-2342 [PMID:8057281]
GtoPdb	-	-	7.2	pIC50	70	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	Binding affinity to mouse GAT-1 expressed in HEK293 cells after 4 hrs in presence of NO711 by LC-ESI-MS/ms analysis	B	7.26	pKi	54.95	nM	Ki	Bioorg Med Chem (2019) 27: 1232-1245 [PMID:30777661]
ChEMBL	Binding affinity to mouse GAT1 stably transfected in HEK293 cells by NO-711 binding assay	B	7.41	pKi	38.9	nM	Ki	Bioorg Med Chem (2013) 21: 5154-5167 [PMID:23859778]
ChEMBL	Displacement of NO 711 from mouse GAT1 expressed in HEK293 cell membranes after 40 mins by LC-ESI-MS-MS-based MS binding assay	B	7.43	pKi	37.15	nM	Ki	Bioorg Med Chem (2016) 24: 2072-2096 [PMID:27039250]
ChEMBL	Inhibition of [2H10]NO 711 binding to mouse GAT1 expressed in HEK293 cell membranes by mass spectrometric analysis	B	7.43	pKi	37.15	nM	Ki	Bioorg Med Chem (2018) 26: 3668-3687 [PMID:29886082]
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	7.43	pKi	37.15	nM	Ki	Bioorg Med Chem (2019) 27: 2753-2763 [PMID:31097402]
ChEMBL	Binding affinity to mouse GAT-1 expressed in human HEK293 cells assessed as inhibition constant in presence of NO711 marker by competitive binding assay	B	7.43	pKi	37.15	nM	Ki	Eur J Med Chem (2022) 234: 114269-114269 [PMID:35306287]
ChEMBL	Binding affinity to mouse GAT1 expressed in HEK293 cells using NO71156 as unlabelled marker by LC-ESI-MS-MS based competitive MS binding assay	B	7.43	pKi	37.15	nM	Ki	Bioorg Med Chem (2015) 23: 1284-1306 [PMID:25698617]
ChEMBL	Inhibition of NO711 binding to mouse GAT1 expressed in HEK293 cell membranes assessed as residual binding preincubated for 4 hrs followed by NO711 addition and measured after 40 mins by LC-ESI-MS/MS analysis	B	7.56	pKi	27.54	nM	Ki	J Med Chem (2018) 61: 10310-10332 [PMID:30376325]
ChEMBL	Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 3 mins by scintillation counting analysis	B	6.1	pIC50	800	nM	IC50	J Med Chem (2013) 56: 2160-2164 [PMID:23398473]
ChEMBL	Inhibition of mouse mGAT1 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis	B	6.1	pIC50	800	nM	IC50	Bioorg Med Chem (2015) 23: 2480-2488 [PMID:25882526]
ChEMBL	Inhibition of GAT1 in mouse D8 cells assessed as [3H]GABA transport by liquid scintillation counting	B	6.72	pIC50	191	nM	IC50	Bioorg Med Chem (2009) 17: 6540-6546 [PMID:19703775]
ChEMBL	Inhibition of mouse GAT-1 expressed in human HEK293 cells assessed as inhibition of [3H]GABA uptake	B	6.88	pIC50	131.83	nM	IC50	Eur J Med Chem (2022) 234: 114269-114269 [PMID:35306287]
ChEMBL	Inhibition of mouse GAT1 expressed in HEK293 cells assessed as reduction in [3H]GABA uptake preincubated for 25 mins followed by [3H]GABA addition and measured after 4 mins by liquid scintillation counting method	B	6.88	pIC50	131.83	nM	IC50	J Med Chem (2018) 61: 10310-10332 [PMID:30376325]
ChEMBL	Inhibition of mouse GAT1 expressed in human HEK293 cell line assessed as inhibition of [3H]GABA uptake measured after 40 mins by LC-ESI-MS/MS analysis	B	6.88	pIC50	131.83	nM	IC50	Eur J Med Chem (2021) 221: 113512-113512 [PMID:34015586]
ChEMBL	Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK cells	B	6.88	pIC50	131.83	nM	IC50	Eur J Med Chem (2008) 43: 2404-2411 [PMID:18395300]
ChEMBL	Inhibition of mouse GAT1 expressed in HEK cells assessed as inhibition of [3H]-GABA uptake after 25 mins by liquid scintillation counting analysis	B	6.88	pIC50	131.83	nM	IC50	Bioorg Med Chem (2013) 21: 3363-3378 [PMID:23598250]
ChEMBL	Inhibition of mouse GAT1-mediated [3H]GABA uptake stably transfected in HEK293 cells	B	6.88	pIC50	131.83	nM	IC50	Bioorg Med Chem (2013) 21: 5154-5167 [PMID:23859778]
ChEMBL	Inhibition of mouse GAT1 expressed in HEK293 cells by [3H]GABA uptake assay	B	6.88	pIC50	131.83	nM	IC50	Bioorg Med Chem (2015) 23: 1284-1306 [PMID:25698617]
ChEMBL	Inhibition of mouse GAT1 expressed in HEK293 cells assessed as decrease in [3H]GABA uptake preincubated for 25 mins followed by [3H]GABA addition measured after 4 mins by liquid scintillation counter method	B	6.88	pIC50	131.83	nM	IC50	Eur J Med Chem (2016) 124: 852-880 [PMID:27654218]
ChEMBL	Inhibition of mouse GAT1 expressed in HEK293 cells assessed as decrease in [3H]GABA uptake	B	6.88	pIC50	131.83	nM	IC50	Bioorg Med Chem (2018) 26: 3668-3687 [PMID:29886082]
ChEMBL	Inhibition of mouse GAT1 assessed as reduction in GABA uptake	B	6.88	pIC50	131.83	nM	IC50	J Med Chem (2018) 61: 6211-6235 [PMID:29924931]
ChEMBL	Inhibition of mouse GAT1 expressed in HEK293 cells assessed as reduction in [3H]GABA uptake preincubated for 25 mins followed by [3H]GABA addition and measured after 4 mins by liquid scintillation counting method	B	6.88	pIC50	131.83	nM	IC50	Bioorg Med Chem (2019) 27: 2753-2763 [PMID:31097402]
ChEMBL	Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 25 mins by scintillation counting analysis	B	7.15	pIC50	70	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	7.2	pIC50	63.1	nM	IC50	J Med Chem (2013) 56: 1323-1340 [PMID:23336362]
ChEMBL	Inhibition of [3H]NO711 binding to mouse GAT1 expressed in human HEK293 cell line by MS binding assay	B	7.43	pIC50	37.15	nM	IC50	Eur J Med Chem (2021) 221: 113512-113512 [PMID:34015586]
GAT1/GABA transporter 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4054] [GtoPdb: 929] [UniProtKB: P23978]
ChEMBL	H-bonding interaction between amino acid residue (Ser-133) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determined	B	5.53	pIC50	2920	nM	IC50	J Med Chem (2004) 47: 5620-5629 [PMID:15509161]
ChEMBL	H-bonding interaction between amino acid residue (Ser-133) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determined	B	5.54	pIC50	2880	nM	IC50	J Med Chem (2004) 47: 5620-5629 [PMID:15509161]
ChEMBL	H-bonding interaction between amino acid residue (Tyr-140) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determined	B	5.56	pIC50	2760	nM	IC50	J Med Chem (2004) 47: 5620-5629 [PMID:15509161]
ChEMBL	H-bonding interaction between amino acid residue (Asn-137) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound	B	5.57	pIC50	2720	nM	IC50	J Med Chem (2004) 47: 5620-5629 [PMID:15509161]
ChEMBL	H-bonding interaction between amino acid residue (Thr-89) of Sodium- and chloride-dependent GABA transporter 1TM2 and compound	B	5.57	pIC50	2680	nM	IC50	J Med Chem (2004) 47: 5620-5629 [PMID:15509161]
ChEMBL	H-bonding interaction between amino acid residue (Asn-137) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound	B	5.6	pIC50	2520	nM	IC50	J Med Chem (2004) 47: 5620-5629 [PMID:15509161]
ChEMBL	H-bonding interaction between amino acid residue (Tyr-140) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determined	B	5.6	pIC50	2500	nM	IC50	J Med Chem (2004) 47: 5620-5629 [PMID:15509161]
ChEMBL	H-bonding interaction between amino acid residue (Ser-133) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determined	B	5.67	pIC50	2140	nM	IC50	J Med Chem (2004) 47: 5620-5629 [PMID:15509161]
ChEMBL	H-bonding interaction between amino acid residue (Asn-137) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound	B	5.67	pIC50	2130	nM	IC50	J Med Chem (2004) 47: 5620-5629 [PMID:15509161]
ChEMBL	H-bonding interaction between amino acid residue (Ser-133) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determined	B	5.67	pIC50	2120	nM	IC50	J Med Chem (2004) 47: 5620-5629 [PMID:15509161]
ChEMBL	H-bonding interaction between amino acid residue (Tyr-140) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determined	B	5.73	pIC50	1870	nM	IC50	J Med Chem (2004) 47: 5620-5629 [PMID:15509161]
ChEMBL	H-bonding interaction between amino acid residue (Thr-89) of Sodium- and chloride-dependent GABA transporter 1TM2 and compound	B	5.75	pIC50	1790	nM	IC50	J Med Chem (2004) 47: 5620-5629 [PMID:15509161]
ChEMBL	H-bonding interaction between amino acid residue (Asn-137) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound	B	5.75	pIC50	1780	nM	IC50	J Med Chem (2004) 47: 5620-5629 [PMID:15509161]
ChEMBL	H-bonding interaction between amino acid residue (Tyr-140) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determined	B	5.77	pIC50	1710	nM	IC50	J Med Chem (2004) 47: 5620-5629 [PMID:15509161]
ChEMBL	Inhibition of rat GAT1 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake by liquid scintillation counting	B	6.19	pIC50	640	nM	IC50	J Med Chem (2015) 58: 2149-2158 [PMID:25679268]
ChEMBL	Inhibition of rat brain synaptosomes GAT1 assessed as inhibition of [3H]GABA uptake by liquid scintillation counting	B	7.15	pIC50	70	nM	IC50	J Med Chem (2015) 58: 2149-2158 [PMID:25679268]
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	7.15	pIC50	70	nM	IC50	Bioorg Med Chem (2019) 27: 1232-1245 [PMID:30777661]
BGT1/GABA transporter 2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4228] [GtoPdb: 932] [UniProtKB: P31651]
ChEMBL	Inhibition of [3H]GABA uptake at GAT2 in mouse neurons after 3 mins by scintillation counting analysis	B	6.44	pIC50	360	nM	IC50	J Med Chem (2013) 56: 2160-2164 [PMID:23398473]
ChEMBL	Inhibition of [3H]GABA uptake at GAT2 in mouse astrocytes after 3 mins by scintillation counting analysis	B	6.74	pIC50	180	nM	IC50	J Med Chem (2013) 56: 2160-2164 [PMID:23398473]

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]