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 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	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	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 [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 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 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 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 [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 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]