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PDGFRβ LanthaScreen Assay from US Patent US20240109917: "PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS"
Assay data:478 Active, 11 Activity ≤ 1 nM, 468 Activity ≤ 1 µM, 485 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
PDGFRβ HTRF Assay from US Patent US20240109917: "PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS"
Assay data:485 Active, 377 Activity ≤ 1 nM, 483 Activity ≤ 1 µM, 485 Tested
Inhibition of PDGFRbeta (unknown origin) preincubated for 60 mins followed by ATP addition and measured after 1 hr by ADP-Glo assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of PDGFRbeta (unknown origin) assessed as residual activity at 1 uM preincubated for 60 mins followed by ATP addition and measured after 1 hr by ADP-Glo assay relative to control
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of His-tagged human recombinant PDGFR-beta (558 to 1106 residues) expressed in baculovirus expression system at 200 nM by Z'-lyte assay
Inhibition of PDGFRbeta (unknown origin) at 1 uM relative to control
Inhibition of PDGFRB (unknown origin) by Ambit kinase assay
Assay data:4 Tested
Inhibition of PDGFR (unknown origin) autophosphorylation expressed in mouse BALB/3T3 clone A31 cells by ELISA-based assay
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Inhibition of PDGFRbeta (unknown origin)
Inhibition of N-terminal 6-His tagged recombinant PDGFRbeta Kinase domain (unknown origin) expressed in baculovirus expression system incubated for 30 mins in the presence of [33p]-ATP by scintillation counting analysis
Inhibition of PDGFR-beta (unknown origin)
Inhibition of recombinant PDGFRbeta (unknown origin) incubated for 60 mins by ELISA analysis
Protac activity at PDGFRbeta in human U87 cells assessed as reduction in PDGFRbeta protein level at 10 uM preincubated with Leupeptin for 2hrs followed by compound treatment and measured after 48 hrs by Western blot analysis
Protac activity at PDGFRbeta in human U87 cells assessed as reduction in PDGFRbeta protein level at 0.1 to 15 uM incubated for 72 hrs by Western blot analysis
Assay data:1 Active, 2 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Protac activity at PDGFRbeta in human U87 cells assessed as reduction in PDGFRbeta protein level at 10 uM preincubated with Carfilzomib for 2hrs followed by compound treatment and measured after 48 hrs by Western blot analysis
Assay data:1 Active, 1 Tested
Protac activity at PDGFRbeta in human U87 cells assessed as reduction in PDGFRbeta protein level at 10 uM preincubated with MG-132 for 2hrs followed by compound treatment and measured after 48 hrs by Western blot analysis
Protac activity at PDGFRbeta in human U87 cells assessed as reduction in PDGFRbeta protein level at 10 uM preincubated with sorafenib for 2hrs followed by compound treatment and measured after 48 hrs by Western blot analysis
Protac activity at PDGFRbeta in human U87 cells assessed as reduction in PDGFRbeta protein level at 10 uM preincubated with VH032 for 2hrs followed by compound treatment and measured after 48 hrs by Western blot analysis
Protac activity at PDGFRbeta in human U87 cells assessed as reduction in PDGFRbeta protein level at 10 uM incubated for 4 to 16 hrs by Western blot analysis
Protac activity at PDGFRbeta in human U87 cells assessed as increase in VEGFR-2 protein level at 10 uM incubated for 72 hrs by Western blot analysis
Assay data:3 Active, 3 Tested
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