BDBM50081174 CHEMBL3421968
SMILES COc1cc(ccc1Nc1nccc(n1)-c1cn(C)c2cnccc12)N1CCN(C)CC1
InChI Key InChIKey=ZYVXTMKTGDARKR-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 30 hits for monomerid = 50081174
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Homo sapiens (Human))
Ach£
Curated by ChEMBL
Ach£
Curated by ChEMBL
Affinity DataKi: 4.40nMAssay Description:Inhibition of human DYRK1A incubated for 90 mins in presence of ATP by Z-LYTE based FRET assayMore data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1B(Homo sapiens (Human))
Ach£
Curated by ChEMBL
Ach£
Curated by ChEMBL
Affinity DataKi: 11nMAssay Description:Inhibition of human DYRK1B incubated for 130 mins in presence of ATP by ADP-Glo kinase assayMore data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1B(Homo sapiens (Human))
Ach£
Curated by ChEMBL
Ach£
Curated by ChEMBL
Affinity DataIC50: 3nMAssay Description:Inhibition of recombinant Dyrk1B (unknown origin) using FITC-Asp-His-Thr-Gly-Phe-Leu-Thr-Glu-Tyr-Val-Ala-Thr-Arg-NH2 as substrate after 60 minsMore data for this Ligand-Target Pair
Affinity DataIC50: 779nMAssay Description:Inhibition of human recombinant N-terminal His6-tagged IGF-1R using fluorescence substrate after 80 mins by caliper off-chip incubation mobility shif...More data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1B(Homo sapiens (Human))
Ach£
Curated by ChEMBL
Ach£
Curated by ChEMBL
Affinity DataIC50: 42nMAssay Description:Inhibition of human full length C-terminal c-Myc tagged Dyrk1B phosphorylation overexpressed in monkey COS1 cells after 5 hrs by ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 4.47E+3nMAssay Description:Inhibition of human recombinant full length C-terminal His6-tagged CDK2 expressed in baculovirus infected Sf21 insect cells using fluorescence substr...More data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Homo sapiens (Human))
Ach£
Curated by ChEMBL
Ach£
Curated by ChEMBL
Affinity DataIC50: 153nMAssay Description:Inhibition of NanoLuc-fused human DYRK1A expressed in HEK293 cells using Nano-Glo as substrate incubated for 2 hrs by NanoBRET assayMore data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1B(Homo sapiens (Human))
Ach£
Curated by ChEMBL
Ach£
Curated by ChEMBL
Affinity DataIC50: 81nMAssay Description:Inhibition of NanoLuc-fused human DYRK1B expressed in HEK293T cells using Nano-Glo as substrate incubated for 2 hrs by NanoBRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 1.06E+3nMAssay 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: 568nMAssay 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: 3.50E+3nMAssay 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: 403nMAssay 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))
Ach£
Curated by ChEMBL
Ach£
Curated by ChEMBL
Affinity DataIC50: 200nMAssay 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))
Ach£
Curated by ChEMBL
Ach£
Curated by ChEMBL
Affinity DataIC50: 18nMAssay 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 1A(Homo sapiens (Human))
Ach£
Curated by ChEMBL
Ach£
Curated by ChEMBL
Affinity DataIC50: 17nMAssay Description:Inhibition of DYRK1A (unknown origin)More data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1B(Homo sapiens (Human))
Ach£
Curated by ChEMBL
Ach£
Curated by ChEMBL
Affinity DataIC50: 17nMAssay Description:Inhibition of DYRK1B (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 764nMAssay 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
Affinity DataIC50: 1.22E+3nMAssay 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
Affinity DataIC50: 6.25E+3nMAssay 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: >1.00E+4nMAssay 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: 175nMAssay 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))
Ach£
Curated by ChEMBL
Ach£
Curated by ChEMBL
Affinity DataIC50: 19nMAssay 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))
Ach£
Curated by ChEMBL
Ach£
Curated by ChEMBL
Affinity DataIC50: 8.30nMAssay 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))
Ach£
Curated by ChEMBL
Ach£
Curated by ChEMBL
Affinity DataKd: 2.60nMAssay 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: 7.40nMAssay 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
Affinity DataKd: >1.00E+4nMAssay 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
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Homo sapiens (Human))
Ach£
Curated by ChEMBL
Ach£
Curated by ChEMBL
Affinity DataIC50: 3.00E+4nMAssay Description:Inhibition of Dyrk1A (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 1.90E+5nMAssay Description:Inhibition of Dyrk2 (unknown origin)More data for this Ligand-Target Pair