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Found 4475 Enz. Inhib. hit(s) with Target = 'TGF-beta receptor type-1'
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM412734(N-(3-fluoropyridin-4-yl)-2-(6-methylpyridin-2-yl)-...)
Affinity DataKi:  0.140nMAssay 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
Ligand InfoPurchase
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50454871(CHEMBL4209835)
Affinity DataKi:  0.140nMAssay 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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM412755(N-(4-((2-(6-(trifluoromethyl)pyridin-2-yl)-7H-pyrr...)
Affinity DataKi:  0.150nMAssay 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
Ligand Info
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM412745(N-(3-fluoropyridin-4-yl)-2-(6-(trifluoromethyl)pyr...)
Affinity DataKi:  0.220nMAssay 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
Ligand InfoPurchasePDB
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50255960(4-(6-methylpyridin-2-yl)-5-(quinoxalin-6-yl)thiazo...)
Affinity DataKi:  0.330nMAssay Description:Binding affinity to human TGFBR1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50255959(4-(5-fluoro-6-methylpyridin-2-yl)-5-(quinoxalin-6-...)
Affinity DataKi:  0.700nMAssay Description:Binding affinity to human TGFBR1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM282825(6-(4-(3-chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-...)
Affinity DataKi:  0.800nMAssay Description:Inhibition of TGFBR1 in human whole blood assessed as apparent inhibition constant by measuring reduction in TGFbeta-induced SMAD phosphorylationMore data for this Ligand-Target Pair
TargetTGF-beta receptor type-1(Mus musculus)
Bristol-Myers Squibb Research & Development

Curated by ChEMBL
LigandPNGBDBM282825(6-(4-(3-chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-...)
Affinity DataKi:  1.40nMAssay Description:Inhibition of TGFBR1 in mouse whole blood assessed as apparent inhibition constant by measuring reduction in TGFbeta-induced SMAD phosphorylationMore data for this Ligand-Target Pair
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50255228(CHEMBL517068 | N-(5-([1,2,4]triazolo[1,5-a]pyridin...)
Affinity DataKi:  2.07nMAssay Description:Binding affinity to human TGFBR1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50255227(CHEMBL450161 | N-(5-([1,2,4]triazolo[1,5-a]pyridin...)
Affinity DataKi:  2.95nMAssay Description:Binding affinity to human TGFBR1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50255958(6-(4-(5-fluoro-6-methylpyridin-2-yl)-2-(4-(methyls...)
Affinity DataKi:  3nMAssay Description:Binding affinity to human TGFBR1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50304836(1,2-dimethyl-4-(6-methylpyridin-2-yl)-5-(quinoxali...)
Affinity DataKi:  5nMAssay Description:Displacement of [3H]HTS446284 from human recombinant His-tagged TGFbetaR1 after 1 hr by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50304849(4-(3-ethylphenyl)-1,2-dimethyl-5-(quinoxalin-6-yl)...)
Affinity DataKi:  6nMAssay Description:Displacement of [3H]HTS446284 from human recombinant His-tagged TGFbetaR1 after 1 hr by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50015639(CHEMBL3260567 | USRE47141, Example 2)
Affinity DataKi:  6.30nMAssay Description:Competitive inhibition of ALK5 (unknown origin) assessed as enzyme/ATP complex by Michaelis-Menten plot analysis in presence of ATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50255179(CHEMBL519939 | N-(4-(5-fluoro-6-methylpyridin-2-yl...)
Affinity DataKi:  7.10nMAssay Description:Binding affinity to human TGFBR1More data for this Ligand-Target Pair
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50255231(CHEMBL479262 | N-(4-(5-fluoro-6-methylpyridin-2-yl...)
Affinity DataKi:  7.20nMAssay Description:Binding affinity to human TGFBR1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50255230(CHEMBL521441 | N-(4-(5-fluoro-6-methylpyridin-2-yl...)
Affinity DataKi:  8.80nMAssay Description:Binding affinity to human TGFBR1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50304835(1,2-dimethyl-4-(pyridin-2-yl)-5-(quinoxalin-6-yl)-...)
Affinity DataKi:  11nMAssay Description:Displacement of [3H]HTS446284 from human recombinant His-tagged TGFbetaR1 after 1 hr by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50304864(4-(3-bromophenyl)-1,2-dimethyl-5-(quinoxalin-6-yl)...)
Affinity DataKi:  12nMAssay Description:Displacement of [3H]HTS446284 from human recombinant His-tagged TGFbetaR1 after 1 hr by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50304850(1,2-dimethyl-5-(quinoxalin-6-yl)-4-(3-vinylphenyl)...)
Affinity DataKi:  12nMAssay Description:Displacement of [3H]HTS446284 from human recombinant His-tagged TGFbetaR1 after 1 hr by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50255908(4-(5-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-4-(5-flu...)
Affinity DataKi:  15nMAssay Description:Binding affinity to human TGFBR1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50255957(1-(4-(5-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-4-(5-...)
Affinity DataKi:  15.2nMAssay Description:Binding affinity to human TGFBR1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50255909(6-(4-(5-fluoro-6-methylpyridin-2-yl)-2-(4-methylpi...)
Affinity DataKi:  16.4nMAssay Description:Binding affinity to human TGFBR1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50110208(4-(4-(benzo[d][1,3]dioxol-5-yl)-5-(pyridin-2-yl)-1...)
Affinity DataKi:  17nMAssay Description:Displacement of [3H]HTS446284 from human recombinant His-tagged TGFbetaR1 after 1 hr by scintillation countingMore data for this Ligand-Target Pair
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50304865(CHEMBL607429 | N-(3-(1,2-dimethyl-3-oxo-5-(quinoxa...)
Affinity DataKi:  19nMAssay Description:Displacement of [3H]HTS446284 from human recombinant His-tagged TGFbetaR1 after 1 hr by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50304863(4-(3-chlorophenyl)-1,2-dimethyl-5-(quinoxalin-6-yl...)
Affinity DataKi:  19nMAssay Description:Displacement of [3H]HTS446284 from human recombinant His-tagged TGFbetaR1 after 1 hr by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50255906(CHEMBL480731 | N-(4-(5-fluoro-6-methylpyridin-2-yl...)
Affinity DataKi:  19nMAssay Description:Binding affinity to human TGFBR1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50304853(4-(3-methoxyphenyl)-1,2-dimethyl-5-(quinoxalin-6-y...)
Affinity DataKi:  20nMAssay Description:Displacement of [3H]HTS446284 from human recombinant His-tagged TGFbetaR1 after 1 hr by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50304840(1,2-dimethyl-5-(quinoxalin-6-yl)-4-m-tolyl-1H-pyra...)
Affinity DataKi:  20nMAssay Description:Displacement of [3H]HTS446284 from human recombinant His-tagged TGFbetaR1 after 1 hr by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50015639(CHEMBL3260567 | USRE47141, Example 2)
Affinity DataKi:  21nMAssay Description:Competitive inhibition of ALK5 (unknown origin) by Michaelis-Menten plot analysis in presence of ATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50304858(2-(3-(1,2-dimethyl-3-oxo-5-(quinoxalin-6-yl)-2,3-d...)
Affinity DataKi:  24nMAssay Description:Displacement of [3H]HTS446284 from human recombinant His-tagged TGFbetaR1 after 1 hr by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50304855(4-(3-(methoxymethyl)phenyl)-1,2-dimethyl-5-(quinox...)
Affinity DataKi:  35nMAssay Description:Displacement of [3H]HTS446284 from human recombinant His-tagged TGFbetaR1 after 1 hr by scintillation countingMore data for this Ligand-Target Pair
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50255907(6-(4-(5-fluoro-6-methylpyridin-2-yl)-2-(piperidin-...)
Affinity DataKi:  53.2nMAssay Description:Binding affinity to human TGFBR1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50304872(1,2-dimethyl-5-(quinoxalin-6-yl)-4-(thiophen-3-yl)...)
Affinity DataKi:  54nMAssay Description:Displacement of [3H]HTS446284 from human recombinant His-tagged TGFbetaR1 after 1 hr by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50304852(1,2-dimethyl-4-(3-(methylthio)phenyl)-5-(quinoxali...)
Affinity DataKi:  60nMAssay Description:Displacement of [3H]HTS446284 from human recombinant His-tagged TGFbetaR1 after 1 hr by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50304870(4-(furan-3-yl)-1,2-dimethyl-5-(quinoxalin-6-yl)-1H...)
Affinity DataKi:  73nMAssay Description:Displacement of [3H]HTS446284 from human recombinant His-tagged TGFbetaR1 after 1 hr by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50304839(1,2-dimethyl-4-phenyl-5-(quinoxalin-6-yl)-1H-pyraz...)
Affinity DataKi:  78nMAssay Description:Displacement of [3H]HTS446284 from human recombinant His-tagged TGFbetaR1 after 1 hr by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50304862(4-(3-fluorophenyl)-1,2-dimethyl-5-(quinoxalin-6-yl...)
Affinity DataKi:  78nMAssay Description:Displacement of [3H]HTS446284 from human recombinant His-tagged TGFbetaR1 after 1 hr by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50304854(1,2-dimethyl-5-(quinoxalin-6-yl)-4-(3-(trifluorome...)
Affinity DataKi:  111nMAssay Description:Displacement of [3H]HTS446284 from human recombinant His-tagged TGFbetaR1 after 1 hr by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50304869(4-(furan-2-yl)-1,2-dimethyl-5-(quinoxalin-6-yl)-1H...)
Affinity DataKi:  190nMAssay Description:Displacement of [3H]HTS446284 from human recombinant His-tagged TGFbetaR1 after 1 hr by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50304871(1,2-dimethyl-5-(quinoxalin-6-yl)-4-(thiophen-2-yl)...)
Affinity DataKi:  365nMAssay Description:Displacement of [3H]HTS446284 from human recombinant His-tagged TGFbetaR1 after 1 hr by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50304856(4-(3-(hydroxymethyl)phenyl)-1,2-dimethyl-5-(quinox...)
Affinity DataKi:  370nMAssay Description:Displacement of [3H]HTS446284 from human recombinant His-tagged TGFbetaR1 after 1 hr by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50304859(4-(3-acetylphenyl)-1,2-dimethyl-5-(quinoxalin-6-yl...)
Affinity DataKi:  410nMAssay Description:Displacement of [3H]HTS446284 from human recombinant His-tagged TGFbetaR1 after 1 hr by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50304861(CHEMBL593950 | methyl 3-(1,2-dimethyl-3-oxo-5-(qui...)
Affinity DataKi:  440nMAssay Description:Displacement of [3H]HTS446284 from human recombinant His-tagged TGFbetaR1 after 1 hr by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50304873(4-(benzo[c][1,2,5]oxadiazol-5-yl)-1,2-dimethyl-5-(...)
Affinity DataKi:  640nMAssay Description:Displacement of [3H]HTS446284 from human recombinant His-tagged TGFbetaR1 after 1 hr by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50304866(CHEMBL593945 | N-(3-(1,2-dimethyl-3-oxo-5-(quinoxa...)
Affinity DataKi:  920nMAssay Description:Displacement of [3H]HTS446284 from human recombinant His-tagged TGFbetaR1 after 1 hr by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50304875(4-(1H-indol-5-yl)-1,2-dimethyl-5-(quinoxalin-6-yl)...)
Affinity DataKi:  1.12E+3nMAssay Description:Displacement of [3H]HTS446284 from human recombinant His-tagged TGFbetaR1 after 1 hr by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50304874(4-(benzo[b]thiophen-3-yl)-1,2-dimethyl-5-(quinoxal...)
Affinity DataKi:  1.87E+3nMAssay Description:Displacement of [3H]HTS446284 from human recombinant His-tagged TGFbetaR1 after 1 hr by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50304838(1,2-dimethyl-4-(2-methylpyridin-4-yl)-5-(quinoxali...)
Affinity DataKi: >2.80E+3nMAssay Description:Displacement of [3H]HTS446284 from human recombinant His-tagged TGFbetaR1 after 1 hr by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50304837(1,2-dimethyl-4-(pyridin-3-yl)-5-(quinoxalin-6-yl)-...)
Affinity DataKi: >2.80E+3nMAssay Description:Displacement of [3H]HTS446284 from human recombinant His-tagged TGFbetaR1 after 1 hr by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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