General Information of the Protein
Protein ID
PT02528
Protein Name
Sodium- and chloride-dependent GABA transporter 1
Secondarily
Protein Name
Solute carrier family 6 member 1
Gene Name
SLC6A1
Secondarily
Gene Name
GABATR
GABT1
GAT1
Sequence
MATNGSKVADGQISTEVSEAPVANDKPKTLVVKVQKKAADLPDRDTWKGRFDFLMSCVGYAIGLGNVWRFPYLCGKNGGGAFLIPYFLTLIFAGVPLFLLECSLGQYTSIGGLGVWKLAPMFKGVGLAAAVLSFWLNIYYIVIISWAIYYLYNSFTTTLPWKQCDNPWNTDRCFSNYSMVNTTNMTSAVVEFWERNMHQMTDGLDKPGQIRWPLAITLAIAWILVYFCIWKGVGWTGKVVYFSATYPYIMLIILFFRGVTLPGAKEGILFYITPNFRKLSDSEVWLDAATQIFFSYGLGLGSLIALGSYNSFHNNVYRDSIIVCCINSCTSMFAGFVIFSIVGFMAHVTKRSIADVAASGPGLAFLAYPEAVTQLPISPLWAILFFSMLLMLGIDSQFCTVEGFITALVDEYPRLLRNRRELFIAAVCIISYLIGLSNITQGGIYVFKLFDYYSASGMSLLFLVFFECVSISWFYGVNRFYDNIQEMVGSRPCIWWKLCWSFFTPIIVAGVFIFSAVQMTPLTMGNYVFPKWGQGVGWLMALSSMVLIPGYMAYMFLTLKGSLKQRIQVMVQPSEDIVRPENGPEQPQAGSSTSKEAYI
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Organism
Homo sapiens, Human
Protein Classification
Transporter
>
Electrochemical transporter
>
SLC superfamily of solute carriers
>
SLC06 neurotransmitter transporter family
Function
Mediates transport of gamma-aminobutyric acid (GABA) together with sodium and chloride and is responsible for the reuptake of GABA from the synapse (PubMed:30132828). The translocation of GABA, however, may also occur in the reverse direction leading to the release of GABA (By similarity). The direction and magnitude of GABA transport is a consequence of the prevailing thermodynamic conditions, determined by membrane potential and the intracellular and extracellular concentrations of Na(+), Cl(-) and GABA (By similarity). Can also mediate sodium- and chloride-dependent transport of hypotaurine but to a much lower extent as compared to GABA (By similarity).
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Uniprot ID
Primary ID:
P30531

Secondarily ID:
Q8N4K8
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Ensembl ID
ENSG00000157103
HGNC ID
HGNC:11042
Subcellular Location
Cell membrane
Presynapse
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000011 , CHO
Compound ID Compound Name Compound Formula
CP0855961
TIAGABINE HYDROCHLORIDE
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C20H26ClNO2S2
 1
1
IC50 = 49 nM
   TI
   LI
   LO
   TS
CP0059522
(R)-Piperidine-3-carboxylic acid
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C6H11NO2
 1
1
IC50 = 5900 nM
   TI
   LI
   LO
   TS
CP0390468
1-(3-carbazol-9-ylpropyl)-4-(2-methoxyphenyl)piperidin-4-ol
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C27H30N2O2
 1
1
IC50 = 11400 nM
   TI
   LI
   LO
   TS
CP0860280
trans-(1S,2R)-2-amino-1-(carboxymethyl)cyclopropane hydrochloride
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C5H10ClNO2
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0081174
(S)-1-(2-(tris(4-methoxyphenyl)methoxy)ethyl)piperidine-3-carboxylic acid
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C30H35NO6
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0386952
2-[(1S,2S)-2-aminocyclopropyl]acetic acid
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C5H9NO2
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0413260
(1S,2S,5R)-5-aminobicyclo[3.1.0]hexane-2-carboxylic acid
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C7H11NO2
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0171598
(RS)-nipecotic acid
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C6H11NO2
 2
1 IC50 = 10.1 nM
2 IC50 = 8000 nM
CP0221365
(R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)piperidine-3-carboxylic acid hydrochloride
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C20H25NO2S2
 2
1 IC50 = 70 nM
2 IC50 = 280 nM
CP0043916
(R)-1-(4,4-Diphenyl-but-3-enyl)-piperidine-3-carboxylic acid
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C22H25NO2
 1
1 IC50 = 130 nM
CP0037615
1-(4,4-Diphenyl-but-3-enyl)-piperidine-3-carboxylic acid
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C22H25NO2
 1
1 IC50 = 200 nM
CP0000066
4-amino-n-[2,3-3H]butyric acid
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C4H9NO2
 1
1 IC50 = 5000 nM
CP0059522
(R)-Piperidine-3-carboxylic acid
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C6H11NO2
 2
1 IC50 = 5900 nM
2 IC50 = 81500 nM
CP0047120
1,2,3,6-tetrahydropyridine-5-carboxylic acid;hydrochloride
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C6H9NO2
 1
1 IC50 = 14000 nM
Clinical Information about the Protein
Target 1 ( GABA transporter GAT-1 (SLC6A1) )
Target Type Successful Target
Disease 3 Target-related Diseases  3
1 Epilepsy [ICD-11: 8A60-8A68]
2 Inflammatory bowel disease [ICD-11: DD72]
3 Convulsion [ICD-11: 8A68.Z]
Approved Drug(s) 1 Approved Drug  1
1 Tiagabine Approved
Epilepsy
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 GSK683699 Phase 2
Inflammatory bowel disease
2 CI-966 Phase 1
Convulsion