BindingDB PrimarySearch_ki

Found 84 with Last Name = 'augustine-rauch' and Initial = 'k'

TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM282825(6-(4-(3-chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-...)

Ki: 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

PDB MMDB Reactome pathway
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3D Structure (crystal)

TGF-beta receptor type-1(Mus musculus)
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM282825(6-(4-(3-chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-...)

Ki: 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

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3D Structure (crystal)

TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM50509622(CHEMBL4455462)

IC50: 0.700nMAssay Description:Inhibition of His-tagged TGFBR1 kinase domain T204D mutant (unknown origin) incubated for 1 hr by HTRF analysisMore data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM50509619(CHEMBL4440988)

IC50: 0.900nMAssay Description:Inhibition of His-tagged TGFBR1 kinase domain T204D mutant (unknown origin) incubated for 1 hr by HTRF analysisMore data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM50468184(CHEMBL4284170)

IC50: 1nMAssay Description:Inhibition of TGFbetaR1 T204D mutant (unknown origin) kinase domain after 1 hr by HTRF assayMore data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM50509621(CHEMBL4458215)

IC50: 1nMAssay Description:Inhibition of His-tagged TGFBR1 kinase domain T204D mutant (unknown origin) incubated for 1 hr by HTRF analysisMore data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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3D Structure (crystal)

TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM282792(6-(1-(2,2-difluoroethyl)-4-(4-fluorophenyl)-1H- im...)

IC50: 1.60nMAssay Description:Inhibition of His-tagged TGFBR1 kinase domain T204D mutant (unknown origin) incubated for 1 hr by HTRF analysisMore data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM282825(6-(4-(3-chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-...)

IC50: 1.60nMAssay Description:Inhibition of His-tagged TGFBR1 kinase domain T204D mutant (unknown origin) incubated for 1 hr by HTRF analysisMore data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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3D Structure (crystal)

TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM50468188(CHEMBL4280660)

IC50: 2nMAssay Description:Inhibition of TGFbetaR1 T204D mutant (unknown origin) kinase domain after 1 hr by HTRF assayMore data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM50468186(CHEMBL4276907)

IC50: 2nMAssay Description:Inhibition of TGFbetaR1 T204D mutant (unknown origin) kinase domain after 1 hr by HTRF assayMore data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM50468182(CHEMBL4292047)

IC50: 2nMAssay Description:Inhibition of TGFbetaR1 T204D mutant (unknown origin) kinase domain after 1 hr by HTRF assayMore data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM50468183(CHEMBL4280731)

IC50: 2nMAssay Description:Inhibition of TGFbetaR1 T204D mutant (unknown origin) kinase domain after 1 hr by HTRF assayMore data for this Ligand-Target Pair

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TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM50468191(CHEMBL4279160)

IC50: 3nMAssay Description:Inhibition of TGFbetaR1 T204D mutant (unknown origin) kinase domain after 1 hr by HTRF assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM50468190(CHEMBL4291307)

IC50: 3nMAssay Description:Inhibition of TGFbetaR1 T204D mutant (unknown origin) kinase domain after 1 hr by HTRF assayMore data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM50468189(CHEMBL4285292)

IC50: 5nMAssay Description:Inhibition of TGFbetaR1 T204D mutant (unknown origin) kinase domain after 1 hr by HTRF assayMore data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM50468187(CHEMBL4288634)

IC50: 6nMAssay Description:Inhibition of TGFbetaR1 T204D mutant (unknown origin) kinase domain after 1 hr by HTRF assayMore data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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3D Structure (crystal)

TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM282805(6-(4-(4-fluorophenyl)-1-(2-hydroxyethyl)-1H-imidaz...)

IC50: 6.70nMAssay Description:Inhibition of His-tagged TGFBR1 kinase domain T204D mutant (unknown origin) incubated for 1 hr by HTRF analysisMore data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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TGF-beta receptor type-2(Homo sapiens (Human))
Bristol-Myers Squibb Research And Development

Curated by ChEMBL

PNG

BDBM50468181(CHEMBL4289841)

IC50: 7nMAssay Description:Inhibition of wild type TGFbetaR2 (unknown origin) kinase domain after 1 hr by HTRF assayMore data for this Ligand-Target Pair

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TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM50468185(CHEMBL4277338)

IC50: 11nMAssay Description:Inhibition of TGFbetaR1 T204D mutant (unknown origin) kinase domain after 1 hr by HTRF assayMore data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM50468183(CHEMBL4280731)

IC50: 17nMAssay Description:Inhibition of TGFbetaR1 in human T cells assessed as reduction in TGFbeta-stimulated PSMAD3 phosphorylation preincubated for 1 hr followed by TGFbeta...More data for this Ligand-Target Pair

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TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM50509620(CHEMBL4534989)

IC50: 17nMAssay Description:Inhibition of His-tagged TGFBR1 kinase domain T204D mutant (unknown origin) incubated for 1 hr by HTRF analysisMore data for this Ligand-Target Pair

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TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM50468181(CHEMBL4289841)

IC50: 22nMAssay Description:Inhibition of TGFbetaR1 T204D mutant (unknown origin) kinase domain after 1 hr by HTRF assayMore data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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TGF-beta receptor type-2(Homo sapiens (Human))
Bristol-Myers Squibb Research And Development

Curated by ChEMBL

PNG

BDBM50468191(CHEMBL4279160)

IC50: 40nMAssay Description:Inhibition of wild type TGFbetaR2 (unknown origin) kinase domain after 1 hr by HTRF assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM50468184(CHEMBL4284170)

IC50: 50nMAssay Description:Inhibition of TGFbetaR1 in human Treg cells assessed as reduction in TGFbeta-stimulated induction of Treg cells by measuring FOXP3/CD25 expression le...More data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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TGF-beta receptor type-1(Mus musculus)
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM282825(6-(4-(3-chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-...)

IC50: 50nMAssay Description:Inhibition of TGFbetaR1 in TGFbeta-stimulated mouse NIH3T3 cells assessed as reduction in SMAD3 phosphorylationMore data for this Ligand-Target Pair

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3D Structure (crystal)

TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM50468184(CHEMBL4284170)

IC50: 68nMAssay Description:Inhibition of TGFbetaR1 in NHLF assessed as reduction in TGFbeta-stimulated TSMAD phosphorylation preincubated for 1 hr followed by TGFbeta addition ...More data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM282792(6-(1-(2,2-difluoroethyl)-4-(4-fluorophenyl)-1H- im...)

IC50: 80nMAssay Description:Inhibition of TGFBR1 in TGFbeta-stimulated human NHLF cells assessed as reduction in SMAD2 nuclear translocationMore data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM50509621(CHEMBL4458215)

IC50: 90nMAssay Description:Inhibition of TGFBR1 in TGFbeta-stimulated human NHLF cells assessed as reduction in SMAD2 nuclear translocationMore data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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3D Structure (crystal)

TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM50468184(CHEMBL4284170)

IC50: 94nMAssay Description:Inhibition of TGFbetaR1 in human T cells assessed as reduction in TGFbeta-stimulated PSMAD3 phosphorylation preincubated for 1 hr followed by TGFbeta...More data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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Mitogen-activated protein kinase 14(Homo sapiens (Human))
Bristol-Myers Squibb Research And Development

Curated by ChEMBL

PNG

BDBM50468183(CHEMBL4280731)

IC50: <100nMAssay Description:Inhibition of p38alpha (unknown origin)More data for this Ligand-Target Pair

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Activin receptor type-1B(Homo sapiens (Human))
Bristol-Myers Squibb Research And Development

Curated by ChEMBL

PNG

BDBM50468184(CHEMBL4284170)

IC50: <100nMAssay Description:Inhibition of ALK4 (unknown origin)More data for this Ligand-Target Pair

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Mitogen-activated protein kinase 14(Homo sapiens (Human))
Bristol-Myers Squibb Research And Development

Curated by ChEMBL

PNG

BDBM50468184(CHEMBL4284170)

IC50: <100nMAssay Description:Inhibition of p38alpha (unknown origin)More data for this Ligand-Target Pair

PDB MMDB NCI pathway Reactome pathway KEGG
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Activin receptor type-1B(Homo sapiens (Human))
Bristol-Myers Squibb Research And Development

Curated by ChEMBL

PNG

BDBM50468183(CHEMBL4280731)

IC50: <100nMAssay Description:Inhibition of ALK4 (unknown origin)More data for this Ligand-Target Pair

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TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM50468183(CHEMBL4280731)

IC50: 110nMAssay Description:Inhibition of TGFbetaR1 in human Treg cells assessed as reduction in TGFbeta-stimulated induction of Treg cells by measuring FOXP3/CD25 expression le...More data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM50509622(CHEMBL4455462)

IC50: 130nMAssay Description:Inhibition of TGFBR1 in TGFbeta-stimulated human NHLF cells assessed as reduction in SMAD2 nuclear translocationMore data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM282825(6-(4-(3-chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-...)

IC50: 150nMAssay Description:Inhibition of TGFbetaR1 in TGFbeta-stimulated human T cells assessed as reduction in SMAD3 phosphorylation preincubated for 1 hr followed by TGFbeta-...More data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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3D Structure (crystal)

TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM282825(6-(4-(3-chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-...)

IC50: 190nMAssay Description:Inhibition of TGFBR1 in TGFbeta-stimulated human NHLF cells assessed as reduction in SMAD2 nuclear translocationMore data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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3D Structure (crystal)

TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM282792(6-(1-(2,2-difluoroethyl)-4-(4-fluorophenyl)-1H- im...)

IC50: 200nMAssay Description:Inhibition of TGFbetaR1 in TGFbeta-stimulated mink Mv1Lu cells assessed as reduction in SMAD nuclear translocation preincubated for 1 hr followed by ...More data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM282825(6-(4-(3-chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-...)

IC50: 230nMAssay Description:Inhibition of TGFbetaR1 in anti-CD3/anti-CD28/IL-2/TGFbeta -stimulated human Treg cells assessed as downregulation of FOXP3 expression incubated for ...More data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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3D Structure (crystal)

TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM282825(6-(4-(3-chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-...)

IC50: 350nMAssay Description:Inhibition of TGFbetaR1 in TGFbeta-stimulated mink Mv1Lu cells assessed as reduction in SMAD nuclear translocation preincubated for 1 hr followed by ...More data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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3D Structure (crystal)

TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM282805(6-(4-(4-fluorophenyl)-1-(2-hydroxyethyl)-1H-imidaz...)

IC50: 350nMAssay Description:Inhibition of TGFBR1 in TGFbeta-stimulated human NHLF cells assessed as reduction in SMAD2 nuclear translocationMore data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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TGF-beta receptor type-2(Homo sapiens (Human))
Bristol-Myers Squibb Research And Development

Curated by ChEMBL

PNG

BDBM50468190(CHEMBL4291307)

IC50: 390nMAssay Description:Inhibition of wild type TGFbetaR2 (unknown origin) kinase domain after 1 hr by HTRF assayMore data for this Ligand-Target Pair

PDB MMDB NCI pathway Reactome pathway KEGG
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TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM50509619(CHEMBL4440988)

IC50: 420nMAssay Description:Inhibition of TGFBR1 in TGFbeta-stimulated human NHLF cells assessed as reduction in SMAD2 nuclear translocationMore data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM50509621(CHEMBL4458215)

IC50: 420nMAssay Description:Inhibition of TGFbetaR1 in TGFbeta-stimulated mink Mv1Lu cells assessed as reduction in SMAD nuclear translocation preincubated for 1 hr followed by ...More data for this Ligand-Target Pair

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3D Structure (crystal)

TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM50468183(CHEMBL4280731)

IC50: 450nMAssay Description:Inhibition of TGFbetaR1 in NHLF assessed as reduction in TGFbeta-stimulated TSMAD phosphorylation preincubated for 1 hr followed by TGFbeta addition ...More data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM50509622(CHEMBL4455462)

IC50: 560nMAssay Description:Inhibition of TGFbetaR1 in TGFbeta-stimulated mink Mv1Lu cells assessed as reduction in SMAD nuclear translocation preincubated for 1 hr followed by ...More data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM50509619(CHEMBL4440988)

IC50: 660nMAssay Description:Inhibition of TGFbetaR1 in TGFbeta-stimulated mink Mv1Lu cells assessed as reduction in SMAD nuclear translocation preincubated for 1 hr followed by ...More data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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TGF-beta receptor type-2(Homo sapiens (Human))
Bristol-Myers Squibb Research And Development

Curated by ChEMBL

PNG

BDBM50468182(CHEMBL4292047)

IC50: 730nMAssay Description:Inhibition of wild type TGFbetaR2 (unknown origin) kinase domain after 1 hr by HTRF assayMore data for this Ligand-Target Pair

PDB MMDB NCI pathway Reactome pathway KEGG
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TGF-beta receptor type-1(Homo sapiens (Human))
Bristol-Myers Squibb Research & Development

Curated by ChEMBL

PNG

BDBM282805(6-(4-(4-fluorophenyl)-1-(2-hydroxyethyl)-1H-imidaz...)

IC50: 800nMAssay Description:Inhibition of TGFbetaR1 in TGFbeta-stimulated mink Mv1Lu cells assessed as reduction in SMAD nuclear translocation preincubated for 1 hr followed by ...More data for this Ligand-Target Pair

PDB MMDB Reactome pathway
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TGF-beta receptor type-2(Homo sapiens (Human))
Bristol-Myers Squibb Research And Development

Curated by ChEMBL

PNG

BDBM50509622(CHEMBL4455462)

IC50: 820nMAssay Description:Inhibition of wild type His-tagged TGFBR2 kinase domain (unknown origin) incubated for 1 hr by HTRF analysisMore data for this Ligand-Target Pair

PDB MMDB NCI pathway Reactome pathway KEGG
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Displayed 1 to 50 (of 84 total ) | Next | Last >>

Filter my 84 hits

Targets 13▿
- TGF-beta receptor type-1 41
- TGF-beta receptor type-2 18
- Cytochrome P450 1A2 3
- Cytochrome P450 2C9 3
- Cytochrome P450 2C19 3
- Cytochrome P450 2D6 3
- Cytochrome P450 2C8 3
- Cytochrome P450 3A4 3
- Mitogen-activated protein kinase 14 2
- Activin receptor type-1B 2
- cAMP-specific 3',5'-cyclic phosphodiesterase 4A/4B/4C/4D 1
- Nuclear receptor subfamily 1 group I member 2 1
- Potassium voltage-gated channel subfamily H member 2 1
Publications 2▿
- ACS Med Chem Lett 9: 1117-1122 (2018) 44
- ACS Med Chem Lett 11: 172-178 (2020) 40
Institutions 2▿
- Bristol-Myers Squibb Research And Development 44
- Bristol-Myers Squibb Research & Development 40
Affinity: 0.70 to 2.4E+4 nM▿
- Ki 2
- IC50 81
- EC50 1
- Affinity ≤ nM
Xtal structures: 4
Docked structures: 0
Catalog Cmpds: 3