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In Vitro Assay from US Patent US20240116948: "PYRIDO OXAZINE DERIVATIVES AS ALK5 INHIBITORS"
Assay data:48 Active, 12 Activity ≤ 1 nM, 47 Activity ≤ 1 µM, 49 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Enzymatic Activity Assay from US Patent US20240116947: "PYRIDO OXAZINE DERIVATIVES AS ALK5 INHIBITORS"
Assay data:57 Active, 41 Activity ≤ 1 nM, 56 Activity ≤ 1 µM, 58 Tested
Inhibition of ALK5 (unknown origin)
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of TGFBR1 (unknown origin) at 1 uM relative to control
Assay data:3 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of TGF-beta1-induced Smad3 phosphorylation in human Hs-578T cells at 1.4 to 333 nM by immunoblotting analysis
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of ALK5 in human Hs-578T cells assessed as effect of TGF-beta-induced Smad3/4 phosphorylation
Assay data:27 Active, 29 Activity ≤ 1 µM, 29 Tested
Inhibition of human ALK5 by Kinase Glo luminescence assay
Assay data:3 Active, 3 Activity ≤ 1 µM, 4 Tested
Inhibition of ALK5 (unknown origin) assessed as dissociation constant
Inhibition of GST tagged TbetaR-1 (unknown origin) by Westernblot assay
Inhibition of GST tagged TbetaR-1 (unknown origin) in the presence of 33 P-gamma ATP
Inhibition of TbetaR-1 (unknown origin) assessed as inhibition constant by ELISA assay
Inhibition of human His-tagged TbetaR-1 assessed as inhibition of SMAD3 phosphorylation by western blot analysis
Inhibition of human GST tagged TGFbeta 1 using 3,3',5,5'-tetramethylbenzidine as substrate incubated for 30 mins in presence of ATP
Inhibition of TbetaR-1 (unknown origin)
Assay data:8 Active, 8 Activity ≤ 1 µM, 8 Tested
Inhibition of TGFbeta receptor 1-mediated SMAD2 phosphorylation in TGFbeta-stimulated human MDA-MB-231 cells at 0.5 uM relative to control
Assay data:23 Tested
Inhibition of human ALK5 autophosphorylation
Assay data:23 Active, 22 Activity ≤ 1 µM, 23 Tested
Inhibition of ALK1 (unknown origin)
Inhibition of ALK4 (unknown origin)
Inhibition of ALK5 (unknown origin) at 1 uM relative to control
Assay data:1 Tested
Inhibition of ALK4 (unknown origin) at 1 uM relative to control
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