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Kinase Assay from US Patent US20240199649: "4-AMINOPYRROLO[2,1-F][1,2,4]TRIAZINES AND PREPARATION AND USES THEREOF"
Assay data:158 Active, 42 Activity ≤ 1 nM, 157 Activity ≤ 1 µM, 158 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
ADP-Glo Assay Promega from US Patent US20240199561: "INHIBITORS OF DYRK AND PIM"
Assay data:17 Active, 17 Activity ≤ 1 µM, 17 Tested
DYRK1A SGC Tm panel (DSF)
Assay data:1 Tested
SummaryRelated BioAssays by Target
Inhibition of recombinant human GST-tagged DYRK1A expressed in Escherichia coli using Woodtide as substrate in presence of [gamma-33P] ATP incubated for 30 mins by scintillation counter analysis
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of wild type human DYRK1A in presence of ATP by radiometric kinase assay
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of wild type human DYRK1A at 1 uM by DiscoverX scanMAX assay relative to control
Inhibition of DYRK1B (unknown origin)
Assay data:5 Active, 5 Activity ≤ 1 µM, 5 Tested
Inhibition of DYRK1A (unknown origin)
Assay data:21 Active, 1 Activity ≤ 1 nM, 17 Activity ≤ 1 µM, 25 Tested
Inhibition of DYRK1A (unknown origin) in presence of ATP
Assay data:1 Active, 1 Activity ≤ 1 µM, 2 Tested
Competitive inhibition of DYRK1A (unknown origin) assessed as michaelis-constant (Km)
Binding affinity to DYRK1A (unknown origin) assessed as inhibition constant
Assay data:2 Active, 1 Activity ≤ 1 µM, 2 Tested
Inhibition of DYRK1A (unknown origin) autophosphorylation
Assay data:1 Active, 2 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of C-terminal his tagged mCherry-DYRK1A (26 to 490 residues) in HEK293T cells assessed as restoration of DYRK1A overexpression mediated calcinurin/NFAT pathway inhibition by measuring ionomycin-stimulated nuclear translocation and accumulation of EGFP-NFAT at 5 uM incubated for 3 hrs followed by ionomycin stimulation for 1 hr by Hoechst 33258 staining based fluorescence microscopic analysis
Assay data:2 Active, 2 Tested
Inhibition of human C-terminal his tagged DYRK1A (26 to 490 residues) transfected in HEK293T cells assessed as inhibition of cyclin D1 phosphorylation at 10 uM incubated for 3 hrs by by Western blot analysis
Assay data:2 Active, 3 Tested
Stabilization of human C-terminal his tagged DYRK1A (26 to 490 residues) expressed in Escherichia coli assessed as change in melting temperature at 10 uM by SYPRO orange dye based thermal shift assay
Assay data:3 Tested
Inhibition of human C-terminal his tagged DYRK1A (26 to 490 residues) expressed in Escherichia coli using DYRKtide (RRRFRPASPLRGPPK) as peptide substrate incubated for 1 hr in presence of ATP by cook activity assay
Assay data:2 Active, 2 Activity ≤ 1 µM, 3 Tested
Binding affinity to human C-terminal his tagged DYRK1A (26 to 490 residues) expressed in Escherichia coli assessed as apparent dissociation constant
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