BDBM50039251 (R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)piperidine-3-carboxylic acid hydrochloride::(R)-1-[4,4-Bis-(3-methyl-thiophen-2-yl)-but-3-enyl]-piperidine-3-carboxylic acid::(R)-1-[4,4-Bis-(3-methyl-thiophen-2-yl)-but-3-enyl]-piperidine-3-carboxylic acid; hydrochloride::(S)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)piperidine-3-carboxylic acid::1-[4,4-Bis-(3-methyl-4,5-dihydro-thiophen-2-yl)-but-3-enyl]-piperidine-3-carboxylic acid::1-[4,4-Bis-(3-methyl-thiophen-2-yl)-but-3-enyl]-piperidine-3-carboxylic acid; hydrochloride::A-70569-1::ABBOTT-70569::ABBOTT-70569-1::ABT-569::CHEMBL1027::Gabitril::NNC-05-0328::NO-05-0328::TIAGABINE::Tiagabine hydrochloride

SMILES [#6]-c1ccsc1\[#6](=[#6]/[#6]-[#6]-[#7]-1-[#6]-[#6]-[#6]-[#6@H](-[#6]-1)-[#6](-[#8])=O)-c1sccc1-[#6]

InChI Key InChIKey=PBJUNZJWGZTSKL-MRXNPFEDSA-N

Data  12 KI  49 IC50  2 Kd

PDB links: 2 PDB IDs match this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 63 hits for monomerid = 50039251   

TargetSodium- and chloride-dependent GABA transporter 1(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataKi:  17.0nMAssay Description:Displacement of [3H]Tiagabine from human recombinant GAT1 expressed in HEK293 cells by equilibrium binding assayMore data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataKi:  28nMAssay Description:Inhibition of NO711 binding to mouse GAT1 expressed in HEK293 cell membranes assessed as residual binding preincubated for 4 hrs followed by NO711 ad...More data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataKi:  37nMAssay Description:Binding affinity to mouse GAT1 expressed in HEK293 cells using NO71156 as unlabelled marker by LC-ESI-MS-MS based competitive MS binding assayMore data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataKi:  37nMAssay Description:Displacement of NO711 from mouse GAT1 expressed in stable HEK293 cell membranes preincubated for 10 mins followed by NO711 addition and measured afte...More data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataKi:  37nMAssay Description:Displacement of NO 711 from mouse GAT1 expressed in HEK293 cell membranes after 40 mins by LC-ESI-MS-MS-based MS binding assayMore data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataKi:  37nMAssay Description:Displacement of NO711 from mouse GAT1 expressed in stable HEK293 cell membranes preincubated for 10 mins followed by NO711 addition and measured afte...More data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataKi:  37nMAssay Description:Inhibition of [2H10]NO 711 binding to mouse GAT1 expressed in HEK293 cell membranes by mass spectrometric analysisMore data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataKi:  37nMAssay Description:Binding affinity to mouse GAT-1 expressed in human HEK293 cells assessed as inhibition constant in presence of NO711 marker by competitive binding as...More data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataKi:  37nMAssay Description:Inhibition of NO711 binding to mouse GAT1 expressed in HEK293 cell membranes assessed as reduction in NO711 binding at incubated for 4 hrs in presenc...More data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataKi:  39nMAssay Description:Binding affinity to mouse GAT1 stably transfected in HEK293 cells by NO-711 binding assayMore data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataKi:  48nMAssay Description:Binding affinity to human GAT1 expressed in HEK293 cells using NO71156 as unlabelled marker by LC-ESI-MS-MS based competitive MS binding assayMore data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataKi:  55nMAssay Description:Binding affinity to mouse GAT-1 expressed in HEK293 cells after 4 hrs in presence of NO711 by LC-ESI-MS/ms analysisMore data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  640nMAssay Description:Inhibition of rat GAT1 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake by liquid scintillation countingMore data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Mus musculus)
Institute Of Microbiology

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  191nMAssay Description:Inhibition of GAT1 in mouse D8 cells assessed as [3H]GABA transport by liquid scintillation countingMore data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  1.78E+3nMAssay Description:H-bonding interaction between amino acid residue (Asn-137) of Sodium- and chloride-dependent GABA transporter 1TM3 and compoundMore data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  2.50E+3nMAssay Description:H-bonding interaction between amino acid residue (Tyr-140) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determinedMore data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  2.52E+3nMAssay Description:H-bonding interaction between amino acid residue (Asn-137) of Sodium- and chloride-dependent GABA transporter 1TM3 and compoundMore data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  2.50E+3nMAssay Description:H-bonding interaction between amino acid residue (Tyr-140) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determinedMore data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  2.50E+3nMAssay Description:H-bonding interaction between amino acid residue (Tyr-140) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determinedMore data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  2.68E+3nMAssay Description:H-bonding interaction between amino acid residue (Thr-89) of Sodium- and chloride-dependent GABA transporter 1TM2 and compoundMore data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  1.78E+3nMAssay Description:H-bonding interaction between amino acid residue (Asn-137) of Sodium- and chloride-dependent GABA transporter 1TM3 and compoundMore data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  2.88E+3nMAssay Description:H-bonding interaction between amino acid residue (Ser-133) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determinedMore data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  2.76E+3nMAssay Description:H-bonding interaction between amino acid residue (Tyr-140) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determinedMore data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  2.92E+3nMAssay Description:H-bonding interaction between amino acid residue (Ser-133) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determinedMore data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  1.78E+3nMAssay Description:H-bonding interaction between amino acid residue (Asn-137) of Sodium- and chloride-dependent GABA transporter 1TM3 and compoundMore data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  2.92E+3nMAssay Description:H-bonding interaction between amino acid residue (Ser-133) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determinedMore data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  2.68E+3nMAssay Description:H-bonding interaction between amino acid residue (Thr-89) of Sodium- and chloride-dependent GABA transporter 1TM2 and compoundMore data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  2.92E+3nMAssay Description:H-bonding interaction between amino acid residue (Ser-133) of Sodium- and chloride-dependent GABA transporter 1TM3 and compound was determinedMore data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  280nMAssay Description:Inhibition of GAT1 transport activityMore data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 3(Mus musculus)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  8.00E+5nMAssay Description:Inhibition of [3H]GABA uptake at mouse GAT4 expressed in HEK293 cells after 3 mins by scintillation counting analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium- and chloride-dependent GABA transporter 2(Mus musculus)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50: >3.00E+5nMAssay Description:Inhibition of [3H]GABA uptake at mouse GAT3 expressed in HEK293 cells after 3 mins by scintillation counting analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium- and chloride-dependent betaine transporter(Mus musculus)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  3.00E+5nMAssay Description:Inhibition of [3H]GABA uptake at mouse GAT2 expressed in HEK293 cells after 3 mins by scintillation counting analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium- and chloride-dependent GABA transporter 1(Mus musculus)
Institute Of Microbiology

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  800nMAssay Description:Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 3 mins by scintillation counting analysisMore data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Mus musculus)
Institute Of Microbiology

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  63.1nMAssay Description:Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 25 mins by scintillation counting analysisMore data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  132nMAssay Description:Inhibition of mouse GAT1 expressed in HEK293 cells assessed as decrease in [3H]GABA uptake preincubated for 25 mins followed by [3H]GABA addition mea...More data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  132nMAssay Description:Inhibition of mouse GAT1 expressed in HEK293 cells assessed as decrease in [3H]GABA uptakeMore data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  132nMAssay Description:Inhibition of mouse GAT1 assessed as reduction in GABA uptakeMore data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  132nMAssay Description:Inhibition of mouse GAT1-mediated [3H]GABA uptake stably transfected in HEK293 cellsMore data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  132nMAssay Description:Inhibition of mouse GAT1 expressed in HEK cells assessed as inhibition of [3H]-GABA uptake after 25 mins by liquid scintillation counting analysisMore data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataKd:  147nMAssay Description: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 preincub...More data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataKd:  41nMAssay Description: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 preinc...More data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  155nMAssay Description:Inhibition of NO711 binding to human GAT1 expressed in COS cell membranes preincubated for 25 mins by LC-ESI-MS/MS analysisMore data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  132nMAssay Description:Inhibition of mouse GAT1 expressed in HEK293 cells assessed as reduction in [3H]GABA uptake preincubated for 25 mins followed by [3H]GABA addition an...More data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  132nMAssay Description:Inhibition of mouse GAT1 expressed in HEK293 cells assessed as reduction in [3H]GABA uptake preincubated for 25 mins followed by [3H]GABA addition an...More data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  132nMAssay Description:Inhibition of mouse GAT1 expressed in HEK293 cells assessed as reduction in [3H]GABA uptake preincubated for 25 mins followed by [3H]GABA addition an...More data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  132nMAssay Description:Inhibition of mouse GAT1 expressed in HEK293 cells assessed as reduction in [3H]GABA uptake preincubated for 25 mins followed by [3H]GABA addition an...More data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  70nMAssay Description: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 measure...More data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  37nMAssay Description:Inhibition of [3H]NO711 binding to mouse GAT1 expressed in human HEK293 cell line by MS binding assayMore data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  132nMAssay Description: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 analysi...More data for this Ligand-Target Pair
TargetSodium- and chloride-dependent GABA transporter 1(Rattus norvegicus)
Ludwig-Maximilians-Universit£T M£Nchen

Curated by ChEMBL
LigandPNGBDBM50039251((R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)pi...)
Affinity DataIC50:  132nMAssay Description:Inhibition of mouse GAT-1 expressed in human HEK293 cells assessed as inhibition of [3H]GABA uptakeMore data for this Ligand-Target Pair
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