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PHD1, PHD2, PHD3 Enzyme Assay from US Patent US11981669: "1,7-naphthyridine derivative and preparation method and use therefor"
Assay data:5 Active, 5 Activity ≤ 1 µM, 5 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Inhibition of human PHD1 expressed in H5 insect cells
Assay data:5 Tested
SummaryPubMed CitationRelated BioAssays by Target
Vitro Assays Demonstrate PHD Inhibition from US Patent US20230295110: "PHD INHIBITOR COMPOUNDS, COMPOSITIONS, AND METHODS OF USE"
Assay data:67 Active, 62 Activity ≤ 1 µM, 67 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
HIF-PH Assay from US Patent US9409892: "4-hydroxy-isoquinoline compounds as HIF hydroxylase inhibitors"
Assay data:151 Active, 53 Activity ≤ 1 µM, 183 Tested
Enzyme Assay from US Patent US8742138: "Compounds as hypoxia mimetics, and compositions and uses thereof"
Assay data:34 Active, 34 Activity ≤ 1 µM, 34 Tested
Inhibition Assay from US Patent US8653111: "Substituted dihydropyrazolones for treating cardiovascular and hematological diseases"
Assay data:20 Active, 12 Activity ≤ 1 µM, 20 Tested
PHD Enzymatic Assay from Article 10.1021/cc100073a: "Dipeptidyl-quinolone derivatives inhibit hypoxia inducible factor-1a prolyl hydroxylases-1, -2, and -3 with altered selectivity."
Assay data:21 Active, 21 Activity ≤ 1 µM, 21 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
PHD1 Enzyme Assay from US Patent US10287286: "Compounds"
Assay data:226 Active, 179 Activity ≤ 1 µM, 226 Tested
Inhibition of recombinant full length human N-terminal FLAG-tagged PHD1 expressed in baculovirus expression system using HIF1/C35 complex as substrate preincubated for 30 mins followed by substrate addition measured after 10 mins by TR-FRET assay
Assay data:6 Active, 6 Activity ≤ 1 µM, 6 Tested
Inhibition of FLAG-tagged full-length HIF-PHD1 (unknown origin) expressed in baculovirus infected Sf9 cells using 2-oxoglutarate and HIF1alpha biotinyl-DLDLEMLAPYIPMDDDFQL as peptide substrates preincubated for 30 mins followed by substrate addition and measured after 2 hrs by LANCE assay
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
In vivo inhibition of HIF-PHD2 in Sprague-Dawley rat assessed as increase in serum erythropoietin level at 10 mg/kg, po administered as single dose measured after 8 hrs by immunoassay
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of PHD (unknown origin) expressed in mouse NIH/3T3 cells harboring HRE-driven luciferase gene assessed as transactivation of HIF1alpha at 1 to 25 uM after 6 hrs in presence of 50 uM betulinic acid by luciferase reporter gene assay
Assay data:1 Tested
Reversible inhibition of PHD (unknown origin) expressed in mouse NIH/3T3 cells harboring HRE-driven luciferase gene assessed as transactivation of HIF1alpha at 5 to 25 uM pretreated for 1 hr followed by compound washout and measured after 6 hrs by luciferase reporter gene assay
Inhibition of PHD in HEK293T cells assessed as reduction in HIF1alpha hydroxylation at 1 to 10 uM after 6 hrs in presence of proteasome inhibitor MG132
Inhibition of PHD in HEK293T cells assessed as increase in HIF1alpha expression at 1 to 10 uM after 6 hrs in presence of proteasome inhibitor MG132
Inhibition of PHD in HEK293T cells assessed as increase in HIF1alpha expression at 10 uM under normoxic condition by Western blot analysis
Inhibition of PHD in HEK293T cells assessed as increase in HIF1alpha expression at 10 uM under hypoxic condition by Western blot analysis
Inhibition of PHD in HEK293T cells assessed as increase in HIF1alpha expression at 10 uM after 15 to 180 mins by Western blot analysis
Inhibition of PHD in HEK293T cells assessed as increase in HIF1alpha expression at 1 to 10 uM after 3 hrs by Western blot analysis
Inhibition of PHD (unknown origin) expressed in mouse NIH/3T3 cells harboring HRE-driven luciferase gene assessed as transactivation of HIF1alpha after 6 hrs by luciferase reporter gene assay relative to deferoxamine
Assay data:14 Tested
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