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Kinase (PDGFRα, PDGFRβ, ABL1 and FLT3) Inhibition Test of Compounds from US Patent US20230312529: "PYRIMIDINE SMALL-MOLECULE COMPOUND AND APPLICATION THEREOF"
Assay data:13 Active, 13 Activity ≤ 1 µM, 13 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
PDGFRα Kinase Assay from US Patent US11679110: "Methods of treating disorders using CSF1R inhibitors"
Assay data:2 Active, 1 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Enzyme-linked immunosorbent assay (ELISA) from US Patent US11655239: "Fused ring pyrimidine amino compound and preparation method, pharmaceutical composition, and use thereof"
Assay data:32 Active, 18 Activity ≤ 1 nM, 32 Activity ≤ 1 µM, 32 Tested
Kinase Activity Assay from US Patent US11591328: "Highly active CSF1R inhibitor compound"
Selectivity interaction (Kinase Profiler (Millipore)) EUB0000603a PDGFRA
Assay data:1 Tested
SummaryRelated BioAssays by Target
Selectivity interaction (NanoBRET assay (HEK293T cells)) EUB0000321b PDGFRA
Selectivity interaction (KinomeScan (DiscoverX)) EUB0000321b PDGFRA
Selectivity interaction (SelectScreen (Invitrogen)) EUB0000679a PDGFRA
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Selectivity interaction (Ambit kinome screening platform (Ambit phage-based competition binding assay)) EUB0000624a PDGFRA
Inhibition of PDGFRA (unknown origin) at 1 uM in presence of ATP by Z'-LYTE assay relative to control
Assay data:2 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of PDGFRalpha (unknown origin)
Inhibition of PDGFR-alpha (unknown origin)
Assay data:3 Tested
Binding affinity to PDGFRalpha (unknown origin)
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of PDGFRalpha (unknown origin) by caliper mobility shift assay
Assay data:14 Active, 14 Activity ≤ 1 µM, 14 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of PDGFRalpha (unknown origin) at 100 nM by caliper mobility shift assay relative to control
Assay data:20 Tested
Inhibition of PDGFRalpha (unknown origin) at 50 nM by Z'LYTE screening method relative to control
Inhibition of PDGFRA V561D mutant (unknown origin) at 0.1 uM relative to control
Inhibition of PDGFRA V561D mutant (unknown origin) at 1 uM relative to control
Inhibition of human PDGFRalpha assessed as residual activity at 30 uM relative to control
Inhibition of PDGFRA V561D mutant (unknown origin) at 100 nM relative to control
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