Proteins > Sodium- and chloride-dependent GABA transporter 1
Page last updated: 2024-08-07 16:29:13
Sodium- and chloride-dependent GABA transporter 1
A sodium- and chloride-dependent GABA transporter 1 that is encoded in the genome of mouse. [OMA:P31648, PRO:DNx]
Synonyms
GAT-1;
Solute carrier family 6 member 1
Research
Bioassay Publications (27)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 3 (11.11) | 29.6817 |
| 2010's | 21 (77.78) | 24.3611 |
| 2020's | 3 (11.11) | 2.80 |
Compounds (19)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| no 711 | Mus musculus (house mouse) | Kd | 0.0265 | 1 | 1 |
Novel mouse GABA uptake inhibitors with enhanced inhibitory activity toward mGAT3/4 and their effect on pain threshold in mice.European journal of medicinal chemistry, , Feb-15, Volume: 188, 2020
Application of the concept of oxime library screening by mass spectrometry (MS) binding assays to pyrrolidine-3-carboxylic acid derivatives as potential inhibitors of γ-aminobutyric acid transporter 1 (GAT1).Bioorganic & medicinal chemistry, , 07-01, Volume: 27, Issue:13, 2019
Synthesis and evaluation of N-substituted nipecotic acid derivatives with an unsymmetrical bis-aromatic residue attached to a vinyl ether spacer as potential GABA uptake inhibitors.Bioorganic & medicinal chemistry, , Jun-01, Volume: 21, Issue:11, 2013
Focused pseudostatic hydrazone libraries screened by mass spectrometry binding assay: optimizing affinities toward γ-aminobutyric acid transporter 1.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
Development of imidazole alkanoic acids as mGAT3 selective GABA uptake inhibitors.European journal of medicinal chemistry, , Volume: 46, Issue:5, 2011
Novel mouse GABA uptake inhibitors with enhanced inhibitory activity toward mGAT3/4 and their effect on pain threshold in mice.European journal of medicinal chemistry, , Feb-15, Volume: 188, 2020
Synthesis of N-substituted acyclic β-amino acids and their investigation as GABA uptake inhibitors.European journal of medicinal chemistry, , Volume: 65, 2013
Development of imidazole alkanoic acids as mGAT3 selective GABA uptake inhibitors.European journal of medicinal chemistry, , Volume: 46, Issue:5, 2011
Straightforward and effective synthesis of γ-aminobutyric acid transporter subtype 2-selective acyl-substituted azaspiro[4.5]decanes.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 26, Issue:2, 2016
Focused pseudostatic hydrazone libraries screened by mass spectrometry binding assay: optimizing affinities toward γ-aminobutyric acid transporter 1.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
Synthesis and biological evaluation of aminomethylphenol derivatives as inhibitors of the murine GABA transporters mGAT1-mGAT4.European journal of medicinal chemistry, , Volume: 43, Issue:11, 2008
Synthesis of 4-substituted nipecotic acid derivatives and their evaluation as potential GABA uptake inhibitors.Bioorganic & medicinal chemistry, , May-01, Volume: 24, Issue:9, 2016
Synthesis of N-substituted acyclic β-amino acids and their investigation as GABA uptake inhibitors.European journal of medicinal chemistry, , Volume: 65, 2013
Synthesis and evaluation of N-substituted nipecotic acid derivatives with an unsymmetrical bis-aromatic residue attached to a vinyl ether spacer as potential GABA uptake inhibitors.Bioorganic & medicinal chemistry, , Jun-01, Volume: 21, Issue:11, 2013
Focused pseudostatic hydrazone libraries screened by mass spectrometry binding assay: optimizing affinities toward γ-aminobutyric acid transporter 1.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
Synthesis and biological evaluation of aminomethylphenol derivatives as inhibitors of the murine GABA transporters mGAT1-mGAT4.European journal of medicinal chemistry, , Volume: 43, Issue:11, 2008
Novel mouse GABA uptake inhibitors with enhanced inhibitory activity toward mGAT3/4 and their effect on pain threshold in mice.European journal of medicinal chemistry, , Feb-15, Volume: 188, 2020
Application of the concept of oxime library screening by mass spectrometry (MS) binding assays to pyrrolidine-3-carboxylic acid derivatives as potential inhibitors of γ-aminobutyric acid transporter 1 (GAT1).Bioorganic & medicinal chemistry, , 07-01, Volume: 27, Issue:13, 2019
Straightforward and effective synthesis of γ-aminobutyric acid transporter subtype 2-selective acyl-substituted azaspiro[4.5]decanes.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 26, Issue:2, 2016
Focused pseudostatic hydrazone libraries screened by mass spectrometry binding assay: optimizing affinities toward γ-aminobutyric acid transporter 1.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
Synthesis and biological evaluation of aminomethylphenol derivatives as inhibitors of the murine GABA transporters mGAT1-mGAT4.European journal of medicinal chemistry, , Volume: 43, Issue:11, 2008
Nipecotic acid as potential lead molecule for the development of GABA uptake inhibitors; structural insights and design strategies.European journal of medicinal chemistry, , Apr-15, Volume: 234, 2022
Development of tricyclic N-benzyl-4-hydroxybutanamide derivatives as inhibitors of GABA transporters mGAT1-4 with anticonvulsant, antinociceptive, and antidepressant activity.European journal of medicinal chemistry, , Oct-05, Volume: 221, 2021
Screening oxime libraries by means of mass spectrometry (MS) binding assays: Identification of new highly potent inhibitors to optimized inhibitors γ-aminobutyric acid transporter 1.Bioorganic & medicinal chemistry, , 04-01, Volume: 27, Issue:7, 2019
Synthesis and biological evaluation of novel N-substituted nipecotic acid derivatives with a cis-alkene spacer as GABA uptake inhibitors.Bioorganic & medicinal chemistry, , 03-01, Volume: 27, Issue:5, 2019
Application of the concept of oxime library screening by mass spectrometry (MS) binding assays to pyrrolidine-3-carboxylic acid derivatives as potential inhibitors of γ-aminobutyric acid transporter 1 (GAT1).Bioorganic & medicinal chemistry, , 07-01, Volume: 27, Issue:13, 2019
Development of New Photoswitchable Azobenzene Based γ-Aminobutyric Acid (GABA) Uptake Inhibitors with Distinctly Enhanced Potency upon Photoactivation.Journal of medicinal chemistry, , 07-26, Volume: 61, Issue:14, 2018
Novel Allosteric Ligands of γ-Aminobutyric Acid Transporter 1 (GAT1) by MS Based Screening of Pseudostatic Hydrazone Libraries.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Synthesis and biological evaluation of novel N-substituted nipecotic acid derivatives with an alkyne spacer as GABA uptake inhibitors.Bioorganic & medicinal chemistry, , 07-23, Volume: 26, Issue:12, 2018
Synthesis and biological evaluation of a series of N-alkylated imidazole alkanoic acids as mGAT3 selective GABA uptake inhibitors.European journal of medicinal chemistry, , Nov-29, Volume: 124, 2016
Synthesis of 4-substituted nipecotic acid derivatives and their evaluation as potential GABA uptake inhibitors.Bioorganic & medicinal chemistry, , May-01, Volume: 24, Issue:9, 2016
Structure activity relationship of selective GABA uptake inhibitors.Bioorganic & medicinal chemistry, , May-15, Volume: 23, Issue:10, 2015
Design, synthesis and SAR studies of GABA uptake inhibitors derived from 2-substituted pyrrolidine-2-yl-acetic acids.Bioorganic & medicinal chemistry, , Mar-15, Volume: 23, Issue:6, 2015
Selective mGAT2 (BGT-1) GABA uptake inhibitors: design, synthesis, and pharmacological characterization.Journal of medicinal chemistry, , Mar-14, Volume: 56, Issue:5, 2013
2-Substituted 4-hydroxybutanamides as potential inhibitors of γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation.Bioorganic & medicinal chemistry, , Sep-01, Volume: 21, Issue:17, 2013
Synthesis and evaluation of N-substituted nipecotic acid derivatives with an unsymmetrical bis-aromatic residue attached to a vinyl ether spacer as potential GABA uptake inhibitors.Bioorganic & medicinal chemistry, , Jun-01, Volume: 21, Issue:11, 2013
Focused pseudostatic hydrazone libraries screened by mass spectrometry binding assay: optimizing affinities toward γ-aminobutyric acid transporter 1.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
Synthesis and biological evaluation of 4-fluoroproline and 4-fluoropyrrolidine-2-acetic acid derivatives as new GABA uptake inhibitors.Bioorganic & medicinal chemistry, , Sep-15, Volume: 17, Issue:18, 2009
Synthesis and biological evaluation of aminomethylphenol derivatives as inhibitors of the murine GABA transporters mGAT1-mGAT4.European journal of medicinal chemistry, , Volume: 43, Issue:11, 2008
Synthesis of 4-substituted nipecotic acid derivatives and their evaluation as potential GABA uptake inhibitors.Bioorganic & medicinal chemistry, , May-01, Volume: 24, Issue:9, 2016
Synthesis of N-substituted acyclic β-amino acids and their investigation as GABA uptake inhibitors.European journal of medicinal chemistry, , Volume: 65, 2013
Focused pseudostatic hydrazone libraries screened by mass spectrometry binding assay: optimizing affinities toward γ-aminobutyric acid transporter 1.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
Synthesis and biological evaluation of aminomethylphenol derivatives as inhibitors of the murine GABA transporters mGAT1-mGAT4.European journal of medicinal chemistry, , Volume: 43, Issue:11, 2008
Development of New Photoswitchable Azobenzene Based γ-Aminobutyric Acid (GABA) Uptake Inhibitors with Distinctly Enhanced Potency upon Photoactivation.Journal of medicinal chemistry, , 07-26, Volume: 61, Issue:14, 2018
Synthesis of N-substituted acyclic β-amino acids and their investigation as GABA uptake inhibitors.European journal of medicinal chemistry, , Volume: 65, 2013
Selective mGAT2 (BGT-1) GABA uptake inhibitors: design, synthesis, and pharmacological characterization.Journal of medicinal chemistry, , Mar-14, Volume: 56, Issue:5, 2013
Synthesis and biological evaluation of aminomethylphenol derivatives as inhibitors of the murine GABA transporters mGAT1-mGAT4.European journal of medicinal chemistry, , Volume: 43, Issue:11, 2008
Synthesis and biological evaluation of (R)-N-(diarylmethylthio/sulfinyl)ethyl/propyl-piperidine-3-carboxylic acid hydrochlorides as novel GABA uptake inhibitors.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 17, Issue:13, 2007
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).Journal of medicinal chemistry, , 11-09, Volume: 60, Issue:21, 2017
Structure activity relationship of selective GABA uptake inhibitors.Bioorganic & medicinal chemistry, , May-15, Volume: 23, Issue:10, 2015
Aminomethyltetrazoles as potential inhibitors of the γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation.Bioorganic & medicinal chemistry, , Nov-01, Volume: 19, Issue:21, 2011
Development of tricyclic N-benzyl-4-hydroxybutanamide derivatives as inhibitors of GABA transporters mGAT1-4 with anticonvulsant, antinociceptive, and antidepressant activity.European journal of medicinal chemistry, , Oct-05, Volume: 221, 2021
Novel mouse GABA uptake inhibitors with enhanced inhibitory activity toward mGAT3/4 and their effect on pain threshold in mice.European journal of medicinal chemistry, , Feb-15, Volume: 188, 2020
Generation and screening of pseudostatic hydrazone libraries derived from 5-substituted nipecotic acid derivatives at the GABA transporter mGAT4.Bioorganic & medicinal chemistry, , 01-01, Volume: 27, Issue:1, 2019
Synthesis and biological evaluation of novel N-substituted nipecotic acid derivatives with a cis-alkene spacer as GABA uptake inhibitors.Bioorganic & medicinal chemistry, , 03-01, Volume: 27, Issue:5, 2019
Synthesis and biological evaluation of novel N-substituted nipecotic acid derivatives with an alkyne spacer as GABA uptake inhibitors.Bioorganic & medicinal chemistry, , 07-23, Volume: 26, Issue:12, 2018
Straightforward and effective synthesis of γ-aminobutyric acid transporter subtype 2-selective acyl-substituted azaspiro[4.5]decanes.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 26, Issue:2, 2016
Design, synthesis and SAR studies of GABA uptake inhibitors derived from 2-substituted pyrrolidine-2-yl-acetic acids.Bioorganic & medicinal chemistry, , Mar-15, Volume: 23, Issue:6, 2015
Structure activity relationship of selective GABA uptake inhibitors.Bioorganic & medicinal chemistry, , May-15, Volume: 23, Issue:10, 2015
Synthesis, biological evaluation and structure-activity relationship of new GABA uptake inhibitors, derivatives of 4-aminobutanamides.European journal of medicinal chemistry, , Aug-18, Volume: 83, 2014
Synthesis of N-substituted acyclic β-amino acids and their investigation as GABA uptake inhibitors.European journal of medicinal chemistry, , Volume: 65, 2013
2-Substituted 4-hydroxybutanamides as potential inhibitors of γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation.Bioorganic & medicinal chemistry, , Sep-01, Volume: 21, Issue:17, 2013
Development of imidazole alkanoic acids as mGAT3 selective GABA uptake inhibitors.European journal of medicinal chemistry, , Volume: 46, Issue:5, 2011
Synthesis and biological evaluation of aminomethylphenol derivatives as inhibitors of the murine GABA transporters mGAT1-mGAT4.European journal of medicinal chemistry, , Volume: 43, Issue:11, 2008