BDBM246383 US9446044, 69
SMILES COC(=N)c1nc2ccc3ncnc(Nc4ccc(OC)cc4F)c3c2s1
InChI Key InChIKey=RYBNARZBIXTFJS-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 45 hits for monomerid = 246383
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Homo sapiens (Human))
Diaxonhit
US Patent
Diaxonhit
US Patent
Affinity DataIC50: 0.360nMpH: 7.5 T: 2°CAssay Description:The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...More data for this Ligand-Target Pair
Affinity DataKd: 160nMAssay Description:Binding affinity to human GSK-3beta assessed as equilibrium dissociation constant measured upto 240 min by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: >3.00E+3nMAssay Description:Inhibition of CLK1 (unknown origin) by NanoBRET cellular target engagement assayMore data for this Ligand-Target Pair
3D Structure (crystal)Affinity DataIC50: >3.00E+3nMAssay Description:Inhibition of CLK2 (unknown origin) by NanoBRET cellular target engagement assayMore data for this Ligand-Target Pair
Affinity DataIC50: >3.00E+3nMAssay Description:Inhibition of CLK3 (unknown origin) by NanoBRET cellular target engagement assayMore data for this Ligand-Target Pair
Affinity DataIC50: >3.00E+3nMAssay Description:Inhibition of CLK4 (unknown origin) by NanoBRET cellular target engagement assayMore data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Homo sapiens (Human))
Diaxonhit
US Patent
Diaxonhit
US Patent
Affinity DataIC50: >3.00E+3nMAssay Description:Inhibition of DYRK1A (unknown origin) by NanoBRET cellular target engagement assayMore data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1B(Homo sapiens (Human))
Masaryk University
Curated by ChEMBL
Masaryk University
Curated by ChEMBL
Affinity DataIC50: >3.00E+3nMAssay Description:Inhibition of DYRK1B (unknown origin) by NanoBRET cellular target engagement assayMore data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 2(Homo sapiens (Human))
Masaryk University
Curated by ChEMBL
Masaryk University
Curated by ChEMBL
Affinity DataIC50: >3.00E+3nMAssay Description:Inhibition of DYRK2 (unknown origin) by NanoBRET cellular target engagement assayMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase kinase kinase 9(Homo sapiens (Human))
Masaryk University
Curated by ChEMBL
Masaryk University
Curated by ChEMBL
Affinity DataIC50: >3.00E+3nMAssay Description:Inhibition of MLK1 (unknown origin) by NanoBRET cellular target engagement assayMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase kinase kinase 10(Homo sapiens (Human))
Masaryk University
Curated by ChEMBL
Masaryk University
Curated by ChEMBL
Affinity DataIC50: >3.00E+3nMAssay Description:Inhibition of MLK2 (unknown origin) by NanoBRET cellular target engagement assayMore data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Homo sapiens (Human))
Diaxonhit
US Patent
Diaxonhit
US Patent
Affinity DataIC50: 0.360nMAssay Description:Inhibition of human DYRK1A using [33P]-ATP incubated for 120 minsMore data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1B(Homo sapiens (Human))
Masaryk University
Curated by ChEMBL
Masaryk University
Curated by ChEMBL
Affinity DataIC50: 0.590nMAssay Description:Inhibition of human DYRK1B using [33P]-ATP incubated for 120 minsMore data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Homo sapiens (Human))
Diaxonhit
US Patent
Diaxonhit
US Patent
Affinity DataIC50: 0.360nMAssay Description:Inhibition of DYRK1A (unknown origin)More data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1B(Homo sapiens (Human))
Masaryk University
Curated by ChEMBL
Masaryk University
Curated by ChEMBL
Affinity DataIC50: 0.590nMAssay Description:Inhibition of DYRK1B (unknown origin)More data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 2(Homo sapiens (Human))
Masaryk University
Curated by ChEMBL
Masaryk University
Curated by ChEMBL
Affinity DataIC50: 3.20nMAssay Description:Inhibition of DYRK2 (unknown origin)More data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 3(Homo sapiens (Human))
University Of Oxford
Curated by ChEMBL
University Of Oxford
Curated by ChEMBL
Affinity DataIC50: 21nMAssay Description:Inhibition of DYRK3 (unknown origin)More data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 4(Homo sapiens (Human))
University Of Oxford
Curated by ChEMBL
University Of Oxford
Curated by ChEMBL
Affinity DataIC50: 1.57E+3nMAssay Description:Inhibition of DYRK4 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 11nMAssay Description:Inhibition of CLK1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 33nMAssay Description:Inhibition of CLK2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 1.42E+3nMAssay Description:Inhibition of CLK3 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 32nMAssay Description:Inhibition of CLK4 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 9.10nMAssay Description:Inhibition of GSK3A (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 143nMAssay Description:Inhibition of GSK3B (unknown origin)More data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Homo sapiens (Human))
Diaxonhit
US Patent
Diaxonhit
US Patent
Affinity DataKd: 7.30nMAssay Description:Binding affinity to DYRK1A (unknown origin) assessed as dissociation constant at 3 uM by ITC assayMore data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Homo sapiens (Human))
Diaxonhit
US Patent
Diaxonhit
US Patent
Affinity DataIC50: 0.360nMAssay Description:Inhibition of DYRK1A (unknown origin)More data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1B(Homo sapiens (Human))
Masaryk University
Curated by ChEMBL
Masaryk University
Curated by ChEMBL
Affinity DataIC50: 0.590nMAssay Description:Inhibition of DYRK1B (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of recombinant human CDK5/p25 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric sc...More data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of recombinant human CK1epsilon expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric ...More data for this Ligand-Target Pair
Affinity DataIC50: 1.21E+3nMAssay Description:Inhibition of recombinant human CLK1 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scinti...More data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of recombinant human CLK2 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scinti...More data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of recombinant human CLK3 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scinti...More data for this Ligand-Target Pair
Affinity DataIC50: 80nMAssay Description:Inhibition of recombinant human CLK4 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scinti...More data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Homo sapiens (Human))
Diaxonhit
US Patent
Diaxonhit
US Patent
Affinity DataIC50: 22nMAssay Description:Inhibition of recombinant human DYRK1A expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scin...More data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1B(Homo sapiens (Human))
Masaryk University
Curated by ChEMBL
Masaryk University
Curated by ChEMBL
Affinity DataIC50: 81nMAssay Description:Inhibition of recombinant human DYRK1B expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scin...More data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 2(Homo sapiens (Human))
Masaryk University
Curated by ChEMBL
Masaryk University
Curated by ChEMBL
Affinity DataIC50: 323nMAssay Description:Inhibition of recombinant human DYRK2 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scint...More data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 3(Homo sapiens (Human))
University Of Oxford
Curated by ChEMBL
University Of Oxford
Curated by ChEMBL
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of recombinant human DYRK3 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scint...More data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 4(Homo sapiens (Human))
University Of Oxford
Curated by ChEMBL
University Of Oxford
Curated by ChEMBL
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of recombinant human DYRK4 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scint...More data for this Ligand-Target Pair
Affinity DataIC50: 5.33E+3nMAssay Description:Inhibition of recombinant human GSK-3beta expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric s...More data for this Ligand-Target Pair
Affinity DataIC50: 111nMAssay Description:Inhibition of recombinant human CLK1 expressed in Sf9 insect cells using myelin basic protein as substrate incubated for 110 mins in presence of ATP ...More data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Homo sapiens (Human))
Diaxonhit
US Patent
Diaxonhit
US Patent
Affinity DataIC50: 14nMAssay Description:Inhibition of recombinant human DYRK1A expressed in Escherichia coli using DYRKtide peptide as substrate incubated for 110 mins in presence of ATP by...More data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1B(Homo sapiens (Human))
Masaryk University
Curated by ChEMBL
Masaryk University
Curated by ChEMBL
Affinity DataIC50: 25nMAssay Description:Inhibition of recombinant human DYRK1B expressed in Sf9 insect cells using DYRKtide peptide as substrate incubated for 110 mins in presence of ATP by...More data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Homo sapiens (Human))
Diaxonhit
US Patent
Diaxonhit
US Patent
Affinity DataKd: 5.20nMAssay Description:Binding affinity to human DYRK1A assessed as equilibrium dissociation constant measured upto 240 min by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataKd: 7.60nMAssay Description:Binding affinity to human CLK1 assessed as equilibrium dissociation constant measured upto 240 min by TR-FRET assayMore data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1B(Homo sapiens (Human))
Masaryk University
Curated by ChEMBL
Masaryk University
Curated by ChEMBL
Affinity DataIC50: 0.590nMpH: 7.5 T: 2°CAssay Description:The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide websit...More data for this Ligand-Target Pair