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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 recombinant human ALK2 (147 to end residues) expressed in Sf9 infected baculovirus expression system using TRF0130 as substrate incubated for 3 hrs in presence of APT
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
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 human ALK2 by NanoBERT assay
Assay data:5 Tested
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 ALK6 (unknown origin)
Inhibition of ALK3 (unknown origin)
Inhibition of ALK2 (unknown origin)
Inhibition of BMPR1A (unknown origin)
Assay data:2 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
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 ALK3 incubated for 30 mins in presence of ATP by QSSA Kit method
Inhibition of human GST tagged TGFbeta 1 using 3,3',5,5'-tetramethylbenzidine as substrate incubated for 30 mins in presence of ATP
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