Affinity DataIC50: 0.25nMAssay Description:Inhibition of N-terminal FLAG-tagged PKCtheta (unknown origin) expressed in baculovirus preincubated for 5 mins using fluorescein-PKC substrate measu...More data for this Ligand-Target Pair
Affinity DataIC50: 0.460nMAssay Description:Inhibition of N-terminal FLAG-tagged PKCtheta (unknown origin) expressed in baculovirus preincubated for 5 mins using fluorescein-PKC substrate measu...More data for this Ligand-Target Pair
Affinity DataIC50: 0.650nMAssay Description:Inhibition of recombinant human full length GST-tagged GRK3 expressed in baculovirus using ulight topo2alpha as substrate preincubated for 60 mins fo...More data for this Ligand-Target Pair
Affinity DataIC50: 0.700nMpH: 7.5Assay Description:The EGFR, HER2 and HER4 kinase assay were performed using radiolabeled [gamma-32P] ATP from GE Healthcare. More data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Takeda Pharmaceutical
Curated by ChEMBL
Takeda Pharmaceutical
Curated by ChEMBL
Affinity DataIC50: 1.20nMAssay Description:Inhibition of VEGFR2 in HUVEC assessed as reduction of VGF-stimulated cell proliferation after 5 daysMore data for this Ligand-Target Pair
Affinity DataIC50: 1.20nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged GRK2 expressed in baculovirus expression system using ulight topo2alpha as substrate preincubat...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 11/12/13/14(Homo sapiens (Human))
Takeda Pharmaceutical
Curated by ChEMBL
Takeda Pharmaceutical
Curated by ChEMBL
Affinity DataIC50: 1.20nMAssay Description:Inhibition of MAPK p38 in human THP1 cells assessed as reduction in LPS-induced TNFalpha production preincubated for 60 mins followed by LPS addition...More data for this Ligand-Target Pair
Affinity DataIC50: 1.30nMAssay Description:Displacement of BODIPY-labeled-(R)-N-(2-(3,5-difluoro-4-(trimethylsilyl)phenylamino)-1-(4-(methoxymethyl)phenyl)-2-oxoethyl)-5-(2-((1-(difluoroboryl)...More data for this Ligand-Target Pair
Affinity DataIC50: 1.60nMAssay Description:Displacement of BODIPY-labeled-(R)-N-(2-(3,5-difluoro-4-(trimethylsilyl)phenylamino)-1-(4-(methoxymethyl)phenyl)-2-oxoethyl)-5-(2-((1-(difluoroboryl)...More data for this Ligand-Target Pair
Affinity DataIC50: 1.60nMAssay Description:Displacement of BODIPY-labeled-(R)-N-(2-(3,5-difluoro-4-(trimethylsilyl)phenylamino)-1-(4-(methoxymethyl)phenyl)-2-oxoethyl)-5-(2-((1-(difluoroboryl)...More data for this Ligand-Target Pair
Affinity DataIC50: 1.70nMAssay Description:Inhibition of human GRK2 expressed in HEK-B2 cells assessed as isoproterenol-stimulated cAMP accumulation preincubation for 20 mins followed by isopr...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Takeda Pharmaceutical
Curated by ChEMBL
Takeda Pharmaceutical
Curated by ChEMBL
Affinity DataIC50: 1.80nMAssay Description:Inhibition of recombinant human FLAG-tagged p38alpha expressed in baculovirus expression system using GFP-ATF2 (19 to 96 residues) as substrate prein...More data for this Ligand-Target Pair
Affinity DataIC50: 1.80nMAssay Description:Inhibition of recombinant human full length GST-tagged GRK3 expressed in baculovirus using ulight topo2alpha as substrate preincubated for 60 mins fo...More data for this Ligand-Target Pair
Affinity DataIC50: 1.80nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged GRK2 expressed in baculovirus expression system using ulight topo2alpha as substrate preincubat...More data for this Ligand-Target Pair
Affinity DataIC50: 1.90nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged GRK2 expressed in baculovirus expression system using ulight topo2alpha as substrate preincubat...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Takeda Pharmaceutical
Curated by ChEMBL
Takeda Pharmaceutical
Curated by ChEMBL
Affinity DataIC50: 2.20nMAssay Description:Inhibition of recombinant human FLAG-tagged p38alpha expressed in baculovirus expression system using GFP-ATF2 (19 to 96 residues) as substrate prein...More data for this Ligand-Target Pair
Affinity DataIC50: 2.5nMAssay Description:Displacement of BODIPY-labeled-(R)-N-(2-(3,5-difluoro-4-(trimethylsilyl)phenylamino)-1-(4-(methoxymethyl)phenyl)-2-oxoethyl)-5-(2-((1-(difluoroboryl)...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Takeda Pharmaceutical
Curated by ChEMBL
Takeda Pharmaceutical
Curated by ChEMBL
Affinity DataIC50: 2.70nMAssay Description:Inhibition of recombinant human FLAG-tagged p38alpha expressed in baculovirus expression system using GFP-ATF2 (19 to 96 residues) as substrate prein...More data for this Ligand-Target Pair
Affinity DataIC50: 3nMpH: 7.5Assay Description:The EGFR, HER2 and HER4 kinase assay were performed using radiolabeled [gamma-32P] ATP from GE Healthcare. More data for this Ligand-Target Pair
Affinity DataIC50: 3nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged GRK2 expressed in baculovirus expression system using ulight topo2alpha as substrate preincubat...More data for this Ligand-Target Pair
Affinity DataIC50: 3.30nMAssay Description:Displacement of BODIPY-labeled-5-((2Z)-2-((1-(difluoroboryl)-3,5-dimethyl-1H-pyrrol-2-yl)-methylene)-2H-pyrrol-5-yl)-N-(2-((3,5-difluoro-4-(trimethyl...More data for this Ligand-Target Pair
Affinity DataIC50: 3.30nMAssay Description:Inhibition of recombinant human full length GST-tagged GRK3 expressed in baculovirus using ulight topo2alpha as substrate preincubated for 60 mins fo...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 11/12/13/14(Homo sapiens (Human))
Takeda Pharmaceutical
Curated by ChEMBL
Takeda Pharmaceutical
Curated by ChEMBL
Affinity DataIC50: 3.5nMAssay Description:Inhibition of MAPK p38 in human THP1 cells assessed as reduction in LPS-induced TNFalpha production preincubated for 60 mins followed by LPS addition...More data for this Ligand-Target Pair
Affinity DataIC50: 3.60nMAssay Description:Displacement of BODIPY-labeled-(R)-N-(2-(3,5-difluoro-4-(trimethylsilyl)phenylamino)-1-(4-(methoxymethyl)phenyl)-2-oxoethyl)-5-(2-((1-(difluoroboryl)...More data for this Ligand-Target Pair
Affinity DataIC50: 3.90nMAssay Description:Displacement of BODIPY-labeled-(R)-N-(2-(3,5-difluoro-4-(trimethylsilyl)phenylamino)-1-(4-(methoxymethyl)phenyl)-2-oxoethyl)-5-(2-((1-(difluoroboryl)...More data for this Ligand-Target Pair
Affinity DataIC50: 3.90nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged GRK2 expressed in baculovirus expression system using ulight topo2alpha as substrate preincubat...More data for this Ligand-Target Pair
Affinity DataIC50: 4.30nMAssay Description:Inhibition of N-terminal FLAG-tagged PKCtheta (unknown origin) expressed in baculovirus preincubated for 5 mins using fluorescein-PKC substrate measu...More data for this Ligand-Target Pair
Affinity DataIC50: 4.30nMAssay Description:Inhibition of recombinant human full length GST-tagged GRK3 expressed in baculovirus using ulight topo2alpha as substrate preincubated for 60 mins fo...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Takeda Pharmaceutical
Curated by ChEMBL
Takeda Pharmaceutical
Curated by ChEMBL
Affinity DataIC50: 4.40nMAssay Description:Inhibition of recombinant human FLAG-tagged p38alpha expressed in baculovirus expression system using GFP-ATF2 (19 to 96 residues) as substrate prein...More data for this Ligand-Target Pair
Affinity DataIC50: 4.80nMAssay Description:Displacement of BODIPY-labeled-(R)-N-(2-(3,5-difluoro-4-(trimethylsilyl)phenylamino)-1-(4-(methoxymethyl)phenyl)-2-oxoethyl)-5-(2-((1-(difluoroboryl)...More data for this Ligand-Target Pair
Affinity DataIC50: 4.90nMAssay Description:Displacement of BODIPY-labeled-(R)-N-(2-(3,5-difluoro-4-(trimethylsilyl)phenylamino)-1-(4-(methoxymethyl)phenyl)-2-oxoethyl)-5-(2-((1-(difluoroboryl)...More data for this Ligand-Target Pair
Affinity DataIC50: 5nMAssay Description:Inverse agonist activity at RORgammat (unknown origin) expressed in human Jurkat cells assessed as inhibition of transcriptional activity after overn...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Takeda Pharmaceutical
Curated by ChEMBL
Takeda Pharmaceutical
Curated by ChEMBL
Affinity DataIC50: 5.40nMAssay Description:Inhibition of recombinant human FLAG-tagged p38alpha expressed in baculovirus expression system using GFP-ATF2 (19 to 96 residues) as substrate prein...More data for this Ligand-Target Pair
Affinity DataIC50: 5.40nMAssay Description:Inhibition of human ACC2More data for this Ligand-Target Pair
Affinity DataIC50: 5.40nMAssay Description:Inhibition of recombinant human full length GST-tagged GRK3 expressed in baculovirus using ulight topo2alpha as substrate preincubated for 60 mins fo...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Takeda Pharmaceutical
Curated by ChEMBL
Takeda Pharmaceutical
Curated by ChEMBL
Affinity DataIC50: 5.40nMAssay Description:Inhibition of recombinant human FLAG-tagged p38alpha expressed in baculovirus expression system using GFP-ATF2 (19 to 96 residues) as substrate prein...More data for this Ligand-Target Pair
Affinity DataIC50: 5.5nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged GRK2 expressed in baculovirus expression system using ulight topo2alpha as substrate preincubat...More data for this Ligand-Target Pair
Affinity DataIC50: 5.90nMAssay Description:Displacement of BODIPY-labeled-(R)-N-(2-(3,5-difluoro-4-(trimethylsilyl)phenylamino)-1-(4-(methoxymethyl)phenyl)-2-oxoethyl)-5-(2-((1-(difluoroboryl)...More data for this Ligand-Target Pair
Affinity DataIC50: 6nMAssay Description:Displacement of BODIPY-labeled-5-((2Z)-2-((1-(difluoroboryl)-3,5-dimethyl-1H-pyrrol-2-yl)-methylene)-2H-pyrrol-5-yl)-N-(2-((3,5-difluoro-4-(trimethyl...More data for this Ligand-Target Pair
Affinity DataIC50: 6.10nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged GRK2 expressed in baculovirus expression system using ulight topo2alpha as substrate preincubat...More data for this Ligand-Target Pair
Affinity DataIC50: 6.80nMAssay Description:Inhibition of human GRK2 expressed in HEK-B2 cells assessed as isoproterenol-stimulated cAMP accumulation preincubation for 20 mins followed by isopr...More data for this Ligand-Target Pair
Affinity DataIC50: 7.20nMAssay Description:Inverse agonist activity at RORgammat (unknown origin) expressed in human Jurkat cells assessed as inhibition of transcriptional activity after overn...More data for this Ligand-Target Pair
Affinity DataIC50: 7.20nMAssay Description:Displacement of BODIPY-labeled-5-((2Z)-2-((1-(difluoroboryl)-3,5-dimethyl-1H-pyrrol-2-yl)-methylene)-2H-pyrrol-5-yl)-N-(2-((3,5-difluoro-4-(trimethyl...More data for this Ligand-Target Pair
Affinity DataIC50: 7.30nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged ROCK2 catalytic domain (1 to 553 residues) expressed in baculovirus expression system using STK...More data for this Ligand-Target Pair
Affinity DataIC50: 7.5nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged GRK2 expressed in baculovirus expression system using ulight topo2alpha as substrate preincubat...More data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Takeda Pharmaceutical
Curated by ChEMBL
Takeda Pharmaceutical
Curated by ChEMBL
Affinity DataIC50: 7.5nMAssay Description:Displacement of BODIPY-labeled-(R)-N-(2-(3,5-difluoro-4-(trimethylsilyl)phenylamino)-1-(4-(methoxymethyl)phenyl)-2-oxoethyl)-5-(2-((1-(difluoroboryl)...More data for this Ligand-Target Pair
Affinity DataIC50: 7.5nMAssay Description:Displacement of BODIPY-labeled-(R)-N-(2-(3,5-difluoro-4-(trimethylsilyl)phenylamino)-1-(4-(methoxymethyl)phenyl)-2-oxoethyl)-5-(2-((1-(difluoroboryl)...More data for this Ligand-Target Pair
Affinity DataIC50: 7.80nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged GRK2 expressed in baculovirus expression system using ulight topo2alpha as substrate preincubat...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Takeda Pharmaceutical
Curated by ChEMBL
Takeda Pharmaceutical
Curated by ChEMBL
Affinity DataIC50: 8.30nMAssay Description:Inhibition of N-terminal FLAG-tagged wild type BRAF (unknown origin) expressed in baculovirus system using GST-MEK1(K96R) as substrate after 20 minsMore data for this Ligand-Target Pair