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Found 5 Enz. Inhib. hit(s) with Target = 'TGF-beta receptor type-1' and Ligand = 'BDBM282805'
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Rigel Pharmaceuticals

US Patent
LigandPNGBDBM282805(6-(4-(4-fluorophenyl)-1-(2-hydroxyethyl)-1H-imidaz...)
Affinity DataIC50:  5.30nMpH: 7.4 T: 2°CAssay Description:Assays for the compounds reported below were conducted in 1536-well plates and 2 mL reactions are prepared from addition of HIS-TGF-βR1 T204D or...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Rigel Pharmaceuticals

US Patent
LigandPNGBDBM282805(6-(4-(4-fluorophenyl)-1-(2-hydroxyethyl)-1H-imidaz...)
Affinity DataIC50:  5.30nMAssay Description:Assays for the compounds reported below were conducted in 1536-well plates and 2 mL reactions are prepared from addition of HIS-TGF-βR1 T204D or...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Rigel Pharmaceuticals

US Patent
LigandPNGBDBM282805(6-(4-(4-fluorophenyl)-1-(2-hydroxyethyl)-1H-imidaz...)
Affinity DataIC50:  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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Rigel Pharmaceuticals

US Patent
LigandPNGBDBM282805(6-(4-(4-fluorophenyl)-1-(2-hydroxyethyl)-1H-imidaz...)
Affinity DataIC50:  350nMAssay Description:Inhibition of TGFBR1 in TGFbeta-stimulated human NHLF cells assessed as reduction in SMAD2 nuclear translocationMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTGF-beta receptor type-1(Homo sapiens (Human))
Rigel Pharmaceuticals

US Patent
LigandPNGBDBM282805(6-(4-(4-fluorophenyl)-1-(2-hydroxyethyl)-1H-imidaz...)
Affinity DataIC50:  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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed