| Assay ID | Title | Year | Journal | Article |
|---|
| AID72446 | Inhibitory activity against human sodium and chloride dependent GABA transporter 3 | 1994 | Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
| Design, synthesis and evaluation of substituted triarylnipecotic acid derivatives as GABA uptake inhibitors: identification of a ligand with moderate affinity and selectivity for the cloned human GABA transporter GAT-3. |
| AID1188933 | Inhibition of human BGT1 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis | 2014 | ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
| Conformationally Restricted GABA with Bicyclo[3.1.0]hexane Backbone as the First Highly Selective BGT-1 Inhibitor. |
| AID370903 | Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK cells | 2008 | European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
| Synthesis and biological evaluation of aminomethylphenol derivatives as inhibitors of the murine GABA transporters mGAT1-mGAT4. |
| AID764585 | Analgesic activity in albino Swiss CD-1 mouse assessed as reduction in formalin-induced inflammatory pain at 30 mg/kg, ip administered 30 mins prior to formalin challenge measured up to 5 mins relative to control | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| 2-Substituted 4-hydroxybutanamides as potential inhibitors of γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation. |
| AID764590 | Analgesic effect in albino Swiss CD-1 mouse assessed as inhibition of acetic acid-induced writhing at 3.75 mg/kg, ip administered 30 mins prior to acetic acid challenge measured for 30 mins relative to control | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| 2-Substituted 4-hydroxybutanamides as potential inhibitors of γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation. |
| AID1573771 | Inhibition of mouse GAT4 expressed in HEK cells assessed as reduction in [3H]GABA uptake by measuring remaining [3H]GABA uptake levels preincubated for 25 mins followed by [3H]GABA addition and measured after 4 mins by microbeta liquid scintillation count | 2019 | Bioorganic & medicinal chemistry, 01-01, Volume: 27, Issue:1
| Generation and screening of pseudostatic hydrazone libraries derived from 5-substituted nipecotic acid derivatives at the GABA transporter mGAT4. |
| AID1778999 | Inhibition of mouse GAT3 expressed in human HEK293 cell line assessed as inhibition of [3H]GABA uptake measured after 40 mins by LC-ESI-MS/MS analysis | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Development of tricyclic N-benzyl-4-hydroxybutanamide derivatives as inhibitors of GABA transporters mGAT1-4 with anticonvulsant, antinociceptive, and antidepressant activity. |
| AID764592 | Analgesic effect in albino Swiss CD-1 mouse assessed as inhibition of acetic acid-induced writhing at 15 mg/kg, ip administered 30 mins prior to acetic acid challenge measured for 30 mins relative to control | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| 2-Substituted 4-hydroxybutanamides as potential inhibitors of γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation. |
| AID1779018 | Inhibition of mouse GAT2 expressed in human HEK293 cell line assessed as inhibition of [3H]GABA uptake at 100 uM measured after 40 mins by LC-ESI-MS/MS analysis | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Development of tricyclic N-benzyl-4-hydroxybutanamide derivatives as inhibitors of GABA transporters mGAT1-4 with anticonvulsant, antinociceptive, and antidepressant activity. |
| AID1192143 | Inhibition of mouse GAT4 expressed in HEK293 cells by [3H]GABA uptake assay | 2015 | Bioorganic & medicinal chemistry, Mar-15, Volume: 23, Issue:6
| Design, synthesis and SAR studies of GABA uptake inhibitors derived from 2-substituted pyrrolidine-2-yl-acetic acids. |
| AID764598 | Inhibition of mouse GAT2-mediated [3H]GABA uptake stably transfected in HEK293 cells assessed as residual uptake at 100 uM relative to control | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| 2-Substituted 4-hydroxybutanamides as potential inhibitors of γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation. |
| AID1573772 | Inhibition of human GAT3 expressed in COS7 cells assessed as reduction in [2H6]GABA uptake preincubated for 25 mins followed by [2H6]GABA addition and measured after 6 mins by LC-MS/MS analysis | 2019 | Bioorganic & medicinal chemistry, 01-01, Volume: 27, Issue:1
| Generation and screening of pseudostatic hydrazone libraries derived from 5-substituted nipecotic acid derivatives at the GABA transporter mGAT4. |
| AID1272002 | Inhibition of mouse GAT1 mediated [3]GABA uptake expressed in HEK293 cells after 3 mins by scintillation counting | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
| Straightforward and effective synthesis of γ-aminobutyric acid transporter subtype 2-selective acyl-substituted azaspiro[4.5]decanes. |
| AID1188934 | Selectivity index, ratio of IC50 for human GAT3 to IC50 for human BGT1 | 2014 | ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
| Conformationally Restricted GABA with Bicyclo[3.1.0]hexane Backbone as the First Highly Selective BGT-1 Inhibitor. |
| AID1498407 | Inhibition of [2H10]NO 711 binding to mouse GAT1 expressed in HEK293 cell membranes after 40 mins by LC-ESI-MS-MS analysis | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
| Synthesis and biological evaluation of novel N-substituted nipecotic acid derivatives with an alkyne spacer as GABA uptake inhibitors. |
| AID1779000 | Inhibition of mouse GAT4 expressed in human HEK293 cell line assessed as inhibition of [3H]GABA uptake measured after 40 mins by LC-ESI-MS/MS analysis | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Development of tricyclic N-benzyl-4-hydroxybutanamide derivatives as inhibitors of GABA transporters mGAT1-4 with anticonvulsant, antinociceptive, and antidepressant activity. |
| AID1192156 | Inhibition of mouse GAT2 expressed in HEK293 cells assessed as remaining [3H]GABA uptake at 100 uM by [3H]GABA uptake assay | 2015 | Bioorganic & medicinal chemistry, Mar-15, Volume: 23, Issue:6
| Design, synthesis and SAR studies of GABA uptake inhibitors derived from 2-substituted pyrrolidine-2-yl-acetic acids. |
| AID595476 | Inhibition of mouse GAT4-mediated [3H]GABA uptake expressed in human HEK cells | 2011 | European journal of medicinal chemistry, May, Volume: 46, Issue:5
| Development of imidazole alkanoic acids as mGAT3 selective GABA uptake inhibitors. |
| AID764602 | Inhibition of mouse GAT1-mediated [3H]GABA uptake stably transfected in HEK293 cells | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| 2-Substituted 4-hydroxybutanamides as potential inhibitors of γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation. |
| AID487220 | Selectivity ratio of IC50 for GAT3 to IC50 for GAT1 | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
| Azetidine derivatives as novel gamma-aminobutyric acid uptake inhibitors: synthesis, biological evaluation, and structure-activity relationship. |
| AID764588 | Analgesic effect in ip dosed albino Swiss CD-1 mouse assessed as inhibition of acetic acid-induced writhing administered 30 mins prior to acetic acid challenge measured for 30 mins | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| 2-Substituted 4-hydroxybutanamides as potential inhibitors of γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation. |
| AID595475 | Inhibition of mouse GAT3-mediated [3H]GABA uptake expressed in human HEK cells | 2011 | European journal of medicinal chemistry, May, Volume: 46, Issue:5
| Development of imidazole alkanoic acids as mGAT3 selective GABA uptake inhibitors. |
| AID631158 | Selectivity ratio of IC50 for mouse GAT4 to IC50 for mouse GAT2 | 2011 | Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21
| Aminomethyltetrazoles as potential inhibitors of the γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation. |
| AID764975 | Inhibition of human BGT1 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| Cyclopropane-based conformational restriction of GABA by a stereochemical diversity-oriented strategy: identification of an efficient lead for potent inhibitors of GABA transports. |
| AID1615010 | Inhibition of mouse GAT4 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 microbeta liquid scintillation counting method | 2019 | Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
| Synthesis and biological evaluation of novel N-substituted nipecotic acid derivatives with a cis-alkene spacer as GABA uptake inhibitors. |
| AID764589 | Analgesic effect in albino Swiss CD-1 mouse assessed as inhibition of acetic acid-induced writhing at 7.5 mg/kg, ip administered 30 mins prior to acetic acid challenge measured for 30 mins relative to control | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| 2-Substituted 4-hydroxybutanamides as potential inhibitors of γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation. |
| AID1272003 | Inhibition of mouse BGT1 mediated [3]GABA uptake expressed in HEK293 cells after 3 mins by scintillation counting | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
| Straightforward and effective synthesis of γ-aminobutyric acid transporter subtype 2-selective acyl-substituted azaspiro[4.5]decanes. |
| AID1188931 | Inhibition of human GAT2 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis | 2014 | ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
| Conformationally Restricted GABA with Bicyclo[3.1.0]hexane Backbone as the First Highly Selective BGT-1 Inhibitor. |
| AID1188930 | Inhibition of human GAT1 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis | 2014 | ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
| Conformationally Restricted GABA with Bicyclo[3.1.0]hexane Backbone as the First Highly Selective BGT-1 Inhibitor. |
| AID1736158 | Inhibition of mouse GAT3 expressed in HEK293 cell line assessed as inhibition of [3H]GABA uptake measured after 35 mins by liquid scintillation method | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Novel mouse GABA uptake inhibitors with enhanced inhibitory activity toward mGAT3/4 and their effect on pain threshold in mice. |
| AID1156746 | Anticonvulsant activity against pilocarpine-induced seizure in albino Swiss (CD-1) mouse assessed as prolongation of latency time to death at 100 mg/kg, ip administered 60 mins before pilocarpine challenge | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Synthesis, biological evaluation and structure-activity relationship of new GABA uptake inhibitors, derivatives of 4-aminobutanamides. |
| AID631075 | Inhibition of human BGT1 assessed as [3H]GABA uptake | 2011 | Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21
| Aminomethyltetrazoles as potential inhibitors of the γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation. |
| AID759054 | Inhibition of GABA uptake at murine GAT-3 expressed in HEK293 cells | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Synthesis of N-substituted acyclic β-amino acids and their investigation as GABA uptake inhibitors. |
| AID631076 | Inhibition of rat GAT2 assessed as [3H]GABA uptake | 2011 | Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21
| Aminomethyltetrazoles as potential inhibitors of the γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation. |
| AID764976 | Inhibition of human GAT3 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| Cyclopropane-based conformational restriction of GABA by a stereochemical diversity-oriented strategy: identification of an efficient lead for potent inhibitors of GABA transports. |
| AID370908 | Inhibition of [3H]GABA uptake at mouse GAT2 expressed in HEK cells assessed as remaining [3H]GABA uptake at 100 uM relative to control | 2008 | European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
| Synthesis and biological evaluation of aminomethylphenol derivatives as inhibitors of the murine GABA transporters mGAT1-mGAT4. |
| AID1156748 | Anticonvulsant activity against pilocarpine-induced seizure in albino Swiss (CD-1) mouse assessed as prolongation of latency time to seizures at 200 mg/kg, ip administered 60 mins before pilocarpine challenge | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Synthesis, biological evaluation and structure-activity relationship of new GABA uptake inhibitors, derivatives of 4-aminobutanamides. |
| AID595473 | Inhibition of mouse GAT1-mediated [3H]GABA uptake expressed in human HEK cells | 2011 | European journal of medicinal chemistry, May, Volume: 46, Issue:5
| Development of imidazole alkanoic acids as mGAT3 selective GABA uptake inhibitors. |
| AID631073 | Inhibition of human GAT1 assessed as [3H]GABA uptake | 2011 | Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21
| Aminomethyltetrazoles as potential inhibitors of the γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation. |
| AID1573769 | Inhibition of mouse GAT3 expressed in HEK cells assessed as reduction in [3H]GABA uptake by measuring remaining [3H]GABA uptake levels preincubated for 25 mins followed by [3H]GABA addition and measured after 4 mins by microbeta liquid scintillation count | 2019 | Bioorganic & medicinal chemistry, 01-01, Volume: 27, Issue:1
| Generation and screening of pseudostatic hydrazone libraries derived from 5-substituted nipecotic acid derivatives at the GABA transporter mGAT4. |
| AID595474 | Inhibition of mouse GAT2-mediated [3H]GABA uptake expressed in human HEK cells | 2011 | European journal of medicinal chemistry, May, Volume: 46, Issue:5
| Development of imidazole alkanoic acids as mGAT3 selective GABA uptake inhibitors. |
| AID1498411 | Inhibition of mouse GAT2 expressed in HEK293 cells assessed as decrease in [3H]GABA uptake at 100 uM preincubated for 25 mins followed by [3H]GABA addition measured after 10 mins by liquid scintillation counting analysis relative to control | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
| Synthesis and biological evaluation of novel N-substituted nipecotic acid derivatives with an alkyne spacer as GABA uptake inhibitors. |
| AID1156750 | Anticonvulsant activity against pilocarpine-induced seizure in albino Swiss (CD-1) mouse assessed as prolongation of latency time to death at 200 mg/kg, ip administered 60 mins before pilocarpine challenge | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Synthesis, biological evaluation and structure-activity relationship of new GABA uptake inhibitors, derivatives of 4-aminobutanamides. |
| AID1498412 | Inhibition of mouse GAT3 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 counting analysis | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
| Synthesis and biological evaluation of novel N-substituted nipecotic acid derivatives with an alkyne spacer as GABA uptake inhibitors. |
| AID1156721 | Inhibition of mouse GAT1 expressed in HEK293 cells assessed as decrease in [3H]GABA uptake | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Synthesis, biological evaluation and structure-activity relationship of new GABA uptake inhibitors, derivatives of 4-aminobutanamides. |
| AID1195451 | Inhibition of mouse mGAT4 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
| Structure activity relationship of selective GABA uptake inhibitors. |
| AID764978 | Inhibition of human GAT1 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| Cyclopropane-based conformational restriction of GABA by a stereochemical diversity-oriented strategy: identification of an efficient lead for potent inhibitors of GABA transports. |
| AID1156751 | Antidepressant-like activity in albino Swiss (CD-1) mouse assessed as reduction in immobility time at 15 mg/kg, ip by forced swim test | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Synthesis, biological evaluation and structure-activity relationship of new GABA uptake inhibitors, derivatives of 4-aminobutanamides. |
| AID1778993 | 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 | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Development of tricyclic N-benzyl-4-hydroxybutanamide derivatives as inhibitors of GABA transporters mGAT1-4 with anticonvulsant, antinociceptive, and antidepressant activity. |
| AID487212 | Inhibition of GAT1-mediated [3H]GABA uptake in bovine brain stem | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
| Azetidine derivatives as novel gamma-aminobutyric acid uptake inhibitors: synthesis, biological evaluation, and structure-activity relationship. |
| AID759053 | Inhibition of GABA uptake at murine GAT-2 expressed in HEK293 cells | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Synthesis of N-substituted acyclic β-amino acids and their investigation as GABA uptake inhibitors. |
| AID1498409 | 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 counting analysis | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
| Synthesis and biological evaluation of novel N-substituted nipecotic acid derivatives with an alkyne spacer as GABA uptake inhibitors. |
| AID1498414 | Inhibition of mouse GAT4 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 counting analysis | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
| Synthesis and biological evaluation of novel N-substituted nipecotic acid derivatives with an alkyne spacer as GABA uptake inhibitors. |
| AID1573765 | Inhibition of mouse GAT1 expressed in HEK cells assessed as reduction in [3H]GABA uptake by measuring remaining [3H]GABA uptake levels preincubated for 25 mins followed by [3H]GABA addition and measured after 4 mins by microbeta liquid scintillation count | 2019 | Bioorganic & medicinal chemistry, 01-01, Volume: 27, Issue:1
| Generation and screening of pseudostatic hydrazone libraries derived from 5-substituted nipecotic acid derivatives at the GABA transporter mGAT4. |
| AID764977 | Inhibition of human GAT2 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| Cyclopropane-based conformational restriction of GABA by a stereochemical diversity-oriented strategy: identification of an efficient lead for potent inhibitors of GABA transports. |
| AID1156745 | Anticonvulsant activity against pilocarpine-induced seizure in albino Swiss (CD-1) mouse assessed as prolongation of latency time to seizures at 100 mg/kg, ip administered 60 mins before pilocarpine challenge | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Synthesis, biological evaluation and structure-activity relationship of new GABA uptake inhibitors, derivatives of 4-aminobutanamides. |
| AID1615004 | 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 microbeta liquid scintillation counting method | 2019 | Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
| Synthesis and biological evaluation of novel N-substituted nipecotic acid derivatives with a cis-alkene spacer as GABA uptake inhibitors. |
| AID764571 | Neurotoxicity in albino Swiss CD-1 mouse assessed as mean time spent on the rotarod with 6 rpm at 30 mg/kg, ip after 30 mins by rotarod test (Rvb = 60.0 +/- 0.0 seconds) | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| 2-Substituted 4-hydroxybutanamides as potential inhibitors of γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation. |
| AID764570 | Neurotoxicity in albino Swiss CD-1 mouse assessed as mean time spent on the rotarod with 18 rpm at 30 mg/kg, ip after 30 mins by rotarod test (Rvb = 60.0 +/- 0.0 seconds) | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| 2-Substituted 4-hydroxybutanamides as potential inhibitors of γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation. |
| AID1573768 | Inhibition of mouse GAT2 expressed in HEK cells assessed as reduction in [3H]GABA uptake at 100 uM by measuring remaining [3H]GABA uptake levels preincubated for 25 mins followed by [3H]GABA addition and measured after 4 mins by microbeta liquid scintilla | 2019 | Bioorganic & medicinal chemistry, 01-01, Volume: 27, Issue:1
| Generation and screening of pseudostatic hydrazone libraries derived from 5-substituted nipecotic acid derivatives at the GABA transporter mGAT4. |
| AID1192137 | Inhibition of mouse GAT1 expressed in HEK293 cells by [3H]GABA uptake assay | 2015 | Bioorganic & medicinal chemistry, Mar-15, Volume: 23, Issue:6
| Design, synthesis and SAR studies of GABA uptake inhibitors derived from 2-substituted pyrrolidine-2-yl-acetic acids. |
| AID1192141 | Inhibition of mouse GAT3 expressed in HEK293 cells by [3H]GABA uptake assay | 2015 | Bioorganic & medicinal chemistry, Mar-15, Volume: 23, Issue:6
| Design, synthesis and SAR studies of GABA uptake inhibitors derived from 2-substituted pyrrolidine-2-yl-acetic acids. |
| AID487208 | Inhibition of GAT3-mediated [3H]GABA uptake in bovine brain stem | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
| Azetidine derivatives as novel gamma-aminobutyric acid uptake inhibitors: synthesis, biological evaluation, and structure-activity relationship. |
| AID631074 | Inhibition of human GAT3 assessed as [3H]GABA uptake | 2011 | Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21
| Aminomethyltetrazoles as potential inhibitors of the γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation. |
| AID1195449 | Inhibition of mouse mGAT2 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
| Structure activity relationship of selective GABA uptake inhibitors. |
| AID764581 | Analgesic activity in albino Swiss CD-1 mouse assessed as reduction in formalin-induced inflammatory pain at 30 mg/kg, ip administered 30 mins prior to formalin challenge measured for 15 to 30 mins relative to control | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| 2-Substituted 4-hydroxybutanamides as potential inhibitors of γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation. |
| AID205447 | Inhibitory activity against rat GABA transporter-2 (rGAT2) | 1994 | Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
| Design, synthesis and evaluation of substituted triarylnipecotic acid derivatives as GABA uptake inhibitors: identification of a ligand with moderate affinity and selectivity for the cloned human GABA transporter GAT-3. |
| AID1195448 | 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 | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
| Structure activity relationship of selective GABA uptake inhibitors. |
| AID764572 | Antinociceptive activity against formalin-induced inflammatory pain in albino Swiss CD-1 mouse assessed as duration of licking response at 30 mg/kg, ip administered 30 mins prior to formalin challenge measured for 15 to 30 mins (Rvb = 78.8 +/- 15.9 second | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| 2-Substituted 4-hydroxybutanamides as potential inhibitors of γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation. |
| AID1615008 | Inhibition of mouse GAT3 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 microbeta liquid scintillation counting method | 2019 | Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
| Synthesis and biological evaluation of novel N-substituted nipecotic acid derivatives with a cis-alkene spacer as GABA uptake inhibitors. |
| AID1156754 | Antinociceptive activity in ip dosed albino Swiss (CD-1) mouse measured after 60 mins by hot plate test | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Synthesis, biological evaluation and structure-activity relationship of new GABA uptake inhibitors, derivatives of 4-aminobutanamides. |
| AID1272004 | Inhibition of mouse GAT2 mediated [3]GABA uptake expressed in HEK293 cells after 3 mins by scintillation counting | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
| Straightforward and effective synthesis of γ-aminobutyric acid transporter subtype 2-selective acyl-substituted azaspiro[4.5]decanes. |
| AID1615007 | Inhibition of mouse GAT2 expressed in HEK293 cells assessed as remaining [3H]GABA uptake at 100 uM preincubated for 25 mins followed by [3H]GABA addition and measured after 10 mins by liquid scintillation counting method relative to control | 2019 | Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
| Synthesis and biological evaluation of novel N-substituted nipecotic acid derivatives with a cis-alkene spacer as GABA uptake inhibitors. |
| AID759056 | Inhibition of GABA uptake at murine GAT-1 expressed in HEK293 cells | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Synthesis of N-substituted acyclic β-amino acids and their investigation as GABA uptake inhibitors. |
| AID205304 | Inhibition of human GABA transporter (hBGT-1) activity. | 1994 | Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
| Design, synthesis and evaluation of substituted triarylnipecotic acid derivatives as GABA uptake inhibitors: identification of a ligand with moderate affinity and selectivity for the cloned human GABA transporter GAT-3. |
| AID764576 | Antinociceptive activity against formalin-induced inflammatory pain in albino Swiss CD-1 mouse assessed as duration of licking response at 30 mg/kg, ip administered 30 mins prior to formalin challenge measured up to 5 mins (Rvb = 34.8 +/- 9.4 seconds) | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| 2-Substituted 4-hydroxybutanamides as potential inhibitors of γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation. |
| AID759055 | Inhibition of GABA uptake at murine BGT-1 expressed in HEK293 cells | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Synthesis of N-substituted acyclic β-amino acids and their investigation as GABA uptake inhibitors. |
| AID631159 | Selectivity ratio of IC50 for mouse GAT4 to IC50 for mouse GAT1 | 2011 | Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21
| Aminomethyltetrazoles as potential inhibitors of the γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation. |
| AID1156727 | Anticonvulsant activity in albino Swiss (CD-1) mouse assessed as current intensity required to induce 50% tonic hind limb extensions at 100 mg/kg, ip after 60 mins by electroconvulsive threshold test (Rvb = 6.61 mA) | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Synthesis, biological evaluation and structure-activity relationship of new GABA uptake inhibitors, derivatives of 4-aminobutanamides. |
| AID764599 | Inhibition of mouse GAT4-mediated [3H]GABA uptake stably transfected in HEK293 cells | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| 2-Substituted 4-hydroxybutanamides as potential inhibitors of γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation. |
| AID1615003 | Displacement of NO711 from mouse GAT1 expressed in stable HEK293 cell membranes preincubated for 10 mins followed by NO711 addition and measured after 40 mins by LC-ESI-MS/MS analysis | 2019 | Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
| Synthesis and biological evaluation of novel N-substituted nipecotic acid derivatives with a cis-alkene spacer as GABA uptake inhibitors. |
| AID1736188 | Inhibition of mouse GAT4 expressed in HEK293 cell line assessed as inhibition of [3H]GABA uptake measured after 35 mins by liquid scintillation method | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Novel mouse GABA uptake inhibitors with enhanced inhibitory activity toward mGAT3/4 and their effect on pain threshold in mice. |
| AID1156722 | Inhibition of mouse GAT2 expressed in HEK293 cells assessed as decrease in [3H]GABA uptake | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Synthesis, biological evaluation and structure-activity relationship of new GABA uptake inhibitors, derivatives of 4-aminobutanamides. |
| AID1156724 | Inhibition of mouse GAT4 expressed in HEK293 cells assessed as decrease in [3H]GABA uptake | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Synthesis, biological evaluation and structure-activity relationship of new GABA uptake inhibitors, derivatives of 4-aminobutanamides. |
| AID1156723 | Inhibition of mouse GAT3 expressed in HEK293 cells assessed as decrease in [3H]GABA uptake | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Synthesis, biological evaluation and structure-activity relationship of new GABA uptake inhibitors, derivatives of 4-aminobutanamides. |
| AID1736160 | Inhibition of mouse GAT1 expressed in HEK293 cell line assessed as inhibition of [3H]GABA uptake measured after 35 mins by liquid scintillation method | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Novel mouse GABA uptake inhibitors with enhanced inhibitory activity toward mGAT3/4 and their effect on pain threshold in mice. |
| AID1156726 | Displacement of NO711 from mouse GAT1 expressed in HEK293 cells by LC-MS/MS analysis | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Synthesis, biological evaluation and structure-activity relationship of new GABA uptake inhibitors, derivatives of 4-aminobutanamides. |
| AID1195450 | Inhibition of mouse mGAT3 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
| Structure activity relationship of selective GABA uptake inhibitors. |
| AID764569 | Neurotoxicity in albino Swiss CD-1 mouse assessed as mean time spent on the rotarod with 24 rpm at 30 mg/kg, ip after 30 mins by rotarod test (Rvb = 60.0 +/- 0.0 seconds) | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| 2-Substituted 4-hydroxybutanamides as potential inhibitors of γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation. |
| AID764604 | Antinociceptive activity in albino Swiss CD-1 mouse assessed as prolongation of latency time at 30 mg/kg, ip administered 30 mins prior to test by hot plate test | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| 2-Substituted 4-hydroxybutanamides as potential inhibitors of γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation. |
| AID1188932 | Inhibition of human GAT3 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis | 2014 | ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
| Conformationally Restricted GABA with Bicyclo[3.1.0]hexane Backbone as the First Highly Selective BGT-1 Inhibitor. |
| AID764600 | Binding affinity to mouse GAT1 stably transfected in HEK293 cells by NO-711 binding assay | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| 2-Substituted 4-hydroxybutanamides as potential inhibitors of γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation. |
| AID370906 | Inhibition of [3H]GABA uptake at mouse GAT4 expressed in HEK cells | 2008 | European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
| Synthesis and biological evaluation of aminomethylphenol derivatives as inhibitors of the murine GABA transporters mGAT1-mGAT4. |
| AID370905 | Inhibition of [3H]GABA uptake at mouse GAT3 expressed in HEK cells | 2008 | European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
| Synthesis and biological evaluation of aminomethylphenol derivatives as inhibitors of the murine GABA transporters mGAT1-mGAT4. |
| AID205303 | Inhibitory activity against human GABA transporter-1 (hGAT1) | 1994 | Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
| Design, synthesis and evaluation of substituted triarylnipecotic acid derivatives as GABA uptake inhibitors: identification of a ligand with moderate affinity and selectivity for the cloned human GABA transporter GAT-3. |
| AID1272005 | Inhibition of mouse GAT3 mediated [3]GABA uptake expressed in HEK293 cells after 3 mins by scintillation counting | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
| Straightforward and effective synthesis of γ-aminobutyric acid transporter subtype 2-selective acyl-substituted azaspiro[4.5]decanes. |
| AID487217 | Binding affinity to GAT3 | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
| Azetidine derivatives as novel gamma-aminobutyric acid uptake inhibitors: synthesis, biological evaluation, and structure-activity relationship. |
| AID1156752 | Antidepressant-like activity in albino Swiss (CD-1) mouse assessed as reduction in immobility time at 30 mg/kg, ip by forced swim test | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Synthesis, biological evaluation and structure-activity relationship of new GABA uptake inhibitors, derivatives of 4-aminobutanamides. |
| AID1346957 | Rat GAT2 (GABA transporter subfamily) | 1994 | Receptors & channels, , Volume: 2, Issue:3
| Cloning of the human homologue of the GABA transporter GAT-3 and identification of a novel inhibitor with selectivity for this site. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |