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GAT1

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Target not currently curated in GtoImmuPdb

Target id: 929

Nomenclature: GAT1

Systematic Nomenclature: SLC6A1

Family: GABA transporter subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 12 599 3p25.3 SLC6A1 solute carrier family 6 member 1
Mouse 12 599 6 E3 Slc6a1 solute carrier family 6 (neurotransmitter transporter, GABA), member 1
Rat 12 599 4q42 Slc6a1 solute carrier family 6 member 1
Previous and Unofficial Names Click here for help
GAT-A | GABATR | GABA transporter protein | Gabt1 | sodium- and chloride-dependent GABA transporter 1 | Gabt | XT-1 | Xtrp1 | GABATHG | solute carrier family 6 (neurotransmitter transporter), member 1 | solute carrier family 6 (neurotransmitter transporter
Database Links Click here for help
Specialist databases
Bioparadigms SLC Tables SLC6A1 (Hs)
RESOLUTE SLC6A1 (Hs)
Other databases
Alphafold P30531 (Hs), P31648 (Mm), P23978 (Rn)
ChEMBL Target CHEMBL1903 (Hs), CHEMBL5445 (Mm), CHEMBL4054 (Rn)
DrugBank Target P30531 (Hs)
Ensembl Gene ENSG00000157103 (Hs), ENSMUSG00000030310 (Mm), ENSRNOG00000006527 (Rn)
Entrez Gene 6529 (Hs), 232333 (Mm), 79212 (Rn)
Human Protein Atlas ENSG00000157103 (Hs)
KEGG Gene hsa:6529 (Hs), mmu:232333 (Mm), rno:79212 (Rn)
OMIM 137165 (Hs)
Pharos P30531 (Hs)
UniProtKB P30531 (Hs), P31648 (Mm), P23978 (Rn)
Wikipedia SLC6A1 (Hs)
Substrates and Reaction Kinetics Click here for help
Substrate Sp. Property Value Units Standard property Standard value Assay description Assay conditions Comments Reference
GABA Substrate is endogenous in the given species Hs -
nipecotic acid Hs -
guvacine Hs -
Stoichiometry Click here for help
2Na+: 1Cl-: 1GABA

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
NNC-711 Small molecule or natural product Ligand has a PDB structure Hs Inhibition 7.4 pIC50 1
⤷ pIC50 7.4 (IC50 4x10-8 M) [1]
tiagabine Small molecule or natural product Approved drug Primary target of this compound Ligand has a PDB structure Hs Inhibition 7.2 pIC50 1
⤷ pIC50 7.2 (IC50 7x10-8 M) [1]
SKF89976A Small molecule or natural product Hs Inhibition 6.9 pIC50 2
⤷ pIC50 6.9 (IC50 1.3x10-7 M) [2]
CI-966 Small molecule or natural product Hs Inhibition 6.6 pIC50 1
⤷ pIC50 6.6 (IC50 2.6x10-7 M) [1]
LU32-176B Small molecule or natural product Click here for species-specific activity table Mm Inhibition 5.4 pIC50 3
⤷ pIC50 5.4 (IC50 4x10-6 M) [3]
(R/S) EF-1500 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 4.9 – 5.7 pIC50
⤷ pIC50 4.9 – 5.7 (IC50 1.3x10-5 – 2x10-6 M)
(R)-EF-1520 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.1 – 5.4 pIC50
⤷ pIC50 5.1 – 5.4 (IC50 8.9x10-6 – 4x10-6 M)
(S)-EF-1520 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 3.6 – 3.9 pIC50
⤷ pIC50 3.6 – 3.9 (IC50 2.5x10-4 – 1.2x10-4 M)
[3H]tiagabine Small molecule or natural product Ligand is labelled Ligand is radioactive Ligand has a PDB structure Hs Inhibition - -
⤷
View species-specific inhibitor tables

References

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1. Borden LA, Murali Dhar TG, Smith KE, Weinshank RL, Branchek TA, Gluchowski C. (1994) Tiagabine, SK&F 89976-A, CI-966, and NNC-711 are selective for the cloned GABA transporter GAT-1. Eur J Pharmacol, 269 (2): 219-24. [PMID:7851497]

2. Dhar TGM, Nakanishi H, Borden LA, Gluchowski C. (1996) On the bioactive conformation of the GABA uptake inhibitor SK&F 89976-A. Bioorg Med Chem Lett, 6 (13): 1535 -1540. DOI: 10.1016/S0960-894X(96)00268-5

3. White HS, Watson WP, Hansen SL, Slough S, Perregaard J, Sarup A, Bolvig T, Petersen G, Larsson OM, Clausen RP et al.. (2005) First demonstration of a functional role for central nervous system betaine/{gamma}-aminobutyric acid transporter (mGAT2) based on synergistic anticonvulsant action among inhibitors of mGAT1 and mGAT2. J Pharmacol Exp Ther, 312 (2): 866-74. [PMID:15550575]

Contributors

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