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

Found 23 hits in this display   

TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50015640(GALUNISERTIB | LY-2157299)
Affinity DataIC50:  4.10nMAssay Description:Inhibition of human His-tagged TGFbetaR1 T204D mutant expressed in Sf9 insect cells after 1 hr by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor-interacting serine/threonine-protein kinase 2(Homo sapiens (Human))
Ewha Womans University

Curated by ChEMBL
LigandPNGBDBM50015640(GALUNISERTIB | LY-2157299)
Affinity DataIC50:  44nMAssay Description:Inhibition of RIPK2 (unknown origin) by radioisotopic assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50015640(GALUNISERTIB | LY-2157299)
Affinity DataIC50:  51nMAssay Description:Inhibition of human ALK5 expressed in Sf9 insect cells using casein as substrate in presence of [gamma-33P]ATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50015640(GALUNISERTIB | LY-2157299)
Affinity DataIC50:  56nMAssay Description:Inhibition of TGFBR1 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50015640(GALUNISERTIB | LY-2157299)
Affinity DataIC50:  69nMAssay Description:Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 insect cells using casein as substrate by proprietary radioisotopic protein kinase as...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Mus musculus)
Ewha Womans University

Curated by ChEMBL
LigandPNGBDBM50015640(GALUNISERTIB | LY-2157299)
Affinity DataIC50: >100nMAssay Description:Inhibition of ALK5 in mouse 4T1 cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50015640(GALUNISERTIB | LY-2157299)
Affinity DataIC50: >100nMAssay Description:Inhibition of ALK5 in human HaCaT cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50015640(GALUNISERTIB | LY-2157299)
Affinity DataIC50:  119nMAssay Description:Inhibition of recombinant GST-tagged human ALK5 expressed in baculovirus infected Sf9 insect cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50015640(GALUNISERTIB | LY-2157299)
Affinity DataIC50:  119nMAssay Description:Inhibition of human recombinant GST-tagged ALK5 expressed in Sf9 insect cells using casein as substrate incubated for 60 mins in presence of [33P]-AT...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50015640(GALUNISERTIB | LY-2157299)
Affinity DataIC50:  127nMAssay Description:Inhibition of human TGFbeta receptor 1 in human HEK293 cells preincubated for 24 hrs followed by addition of TGFbeta1 and measured after 24 hrs by lu...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50015640(GALUNISERTIB | LY-2157299)
Affinity DataIC50:  129nMAssay Description:Inhibition of recombinant human GST-fused ALK5 expressed in baculovirus infected Sf9 cells assessed as incoporation of [33]Pi after 60 mins in presen...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50015640(GALUNISERTIB | LY-2157299)
Affinity DataIC50:  129nMAssay Description:Inhibition of human recombinant GST-tagged ALK5 expressed in Sf9 insect cells using casein as substrate incubated for 60 mins in presence of [33P]-AT...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50015640(GALUNISERTIB | LY-2157299)
Affinity DataIC50:  170nMAssay Description:Inhibition of human TGF-beta-R1 using TMB substrate incubated for 2.5 hrs by microplate reader analysisMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetActivin receptor type-1B(Homo sapiens (Human))
Ewha Womans University

Curated by ChEMBL
LigandPNGBDBM50015640(GALUNISERTIB | LY-2157299)
Affinity DataIC50:  199nMAssay Description:Inhibition of ALK4 (unknown origin) by radioisotopic assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase kinase kinase kinase 4(Homo sapiens (Human))
University Of Arkansas For Medical Sciences

Curated by ChEMBL
LigandPNGBDBM50015640(GALUNISERTIB | LY-2157299)
Affinity DataIC50:  263nMAssay Description:Inhibition of recombinant human GST-tagged MAP4K4 expressed in baculovirus expression system using 5-FAM-KRELVEPLTPSGEAPNQALLR-CONH2 substrate preinc...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase kinase kinase kinase 4(Homo sapiens (Human))
University Of Arkansas For Medical Sciences

Curated by ChEMBL
LigandPNGBDBM50015640(GALUNISERTIB | LY-2157299)
Affinity DataIC50:  280nMAssay Description:Inhibition of wild type partial length human MAP4K4 (M1 to R310 residues) expressed in bacterial expression system measured by Kinomescan assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50015640(GALUNISERTIB | LY-2157299)
Affinity DataIC50:  405nMAssay Description:Inhibition of human recombinant p38alpha expressed in Escherichia coli using ATF2 as substrate by proprietary radioisotopic protein kinase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Ewha Womans University

Curated by ChEMBL
LigandPNGBDBM50015640(GALUNISERTIB | LY-2157299)
Affinity DataIC50:  442nMAssay Description:Inhibition of VEGFR2 (unknown origin) by radioisotopic assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Yanbian University

Curated by ChEMBL
LigandPNGBDBM50015640(GALUNISERTIB | LY-2157299)
Affinity DataIC50:  487nMAssay Description:Inhibition of recombinant human p38alpha expressed in Escherichia coliMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Yanbian University

Curated by ChEMBL
LigandPNGBDBM50015640(GALUNISERTIB | LY-2157299)
Affinity DataIC50:  490nMAssay Description:Inhibition of human recombinant untagged p38alpha expressed in Escherichia coli using ATF2 as substrate incubated for 60 mins in presence of [33P]-AT...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Yanbian University

Curated by ChEMBL
LigandPNGBDBM50015640(GALUNISERTIB | LY-2157299)
Affinity DataIC50:  493nMAssay Description:Inhibition of human recombinant untagged p38alpha expressed in Escherichia coli using ATF2 as substrate incubated for 60 mins in presence of [33P]-AT...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Yanbian University

Curated by ChEMBL
LigandPNGBDBM50015640(GALUNISERTIB | LY-2157299)
Affinity DataIC50:  493nMAssay Description:Inhibition of recombinant human p38alpha expressed in Escherichia coli assessed as incoporation of [33]Pi after 60 mins in presence of [gamma-33P]-AT...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-2(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50015640(GALUNISERTIB | LY-2157299)
Affinity DataIC50:  1.30E+3nMAssay Description:Inhibition of wild type His-tagged TGFbetaR2 (unknown origin) after 1 hr by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed