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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB (change energy unit to kcal/mol)

Found 5 hits in this display   

TargetProbable G-protein coupled receptor 139(Homo sapiens (Human))
Takeda Pharmaceutical

US Patent
LigandPNGBDBM263471((s)-2-(7-methoxy-4-oxobenzo[d][1,2,3]triazin-3(4h)...)
Affinity DataKi:  437nM ΔG°:  -33.7kJ/molepH: 7.4 T: 2°CAssay Description:This membrane based assay measures the ability of compounds to competitively bind GPR139 in stably transfected CHO-TRex membranes. CHO-TRex (Life Tec...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetProbable G-protein coupled receptor 139(Homo sapiens (Human))
Takeda Pharmaceutical

US Patent
LigandPNGBDBM263471((s)-2-(7-methoxy-4-oxobenzo[d][1,2,3]triazin-3(4h)...)
Affinity DataKi:  437nMAssay Description:Membranes were removed from −80° C., thawed and diluted in cold radioligand assay buffer (20 mM HEPES pH 7.4/5 mM MgCl2/1 mM CaCl2/Roche protea...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetProbable G-protein coupled receptor 139(Homo sapiens (Human))
Takeda Pharmaceutical

US Patent
LigandPNGBDBM263471((s)-2-(7-methoxy-4-oxobenzo[d][1,2,3]triazin-3(4h)...)
Affinity DataKi:  437nMAssay Description:Displacement of (S)-N-(1-(2-[3H]-4-methoxyphenyl)propan-2-yl)-2-(2,3-dimethyl-7-oxothieno[2,3-d]pyridazin-6(7H)-yl)acetamide from human GPR139 expres...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetProbable G-protein coupled receptor 139(Homo sapiens (Human))
Takeda Pharmaceutical

US Patent
LigandPNGBDBM263471((s)-2-(7-methoxy-4-oxobenzo[d][1,2,3]triazin-3(4h)...)
Affinity DataKi:  4.37E+5nMAssay Description:This membrane based assay measures the ability of compounds to competitively bind GPR139 in stably transfected CHO-TRex membranes. CHO-TRex (Life Tec...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetProbable G-protein coupled receptor 139(Homo sapiens (Human))
Takeda Pharmaceutical

US Patent
LigandPNGBDBM263471((s)-2-(7-methoxy-4-oxobenzo[d][1,2,3]triazin-3(4h)...)
Affinity DataEC50:  19nMAssay Description:Agonist activity at human GPR139 expressed in CHO-TRex cells assessed as stimulation of calcium signalling incubated for 15 mins by FLIPR assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed