KH-CB19 [Ligand Id: 8055] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL1236620
  • casein kinase 1 epsilon/Casein kinase I epsilon in Human [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674]
There should be some charts here, you may need to enable JavaScript!
  • cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078]
There should be some charts here, you may need to enable JavaScript!
  • CDC like kinase 1/Dual specificity protein kinase CLK1 in Human [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759]
There should be some charts here, you may need to enable JavaScript!
  • CDC like kinase 2/Dual specificity protein kinase CLK2 in Human [ChEMBL: CHEMBL4225] [GtoPdb: 1991] [UniProtKB: P49760]
There should be some charts here, you may need to enable JavaScript!
  • CDC like kinase 3/Dual specificity protein kinase CLK3 in Human [ChEMBL: CHEMBL4226] [GtoPdb: 1992] [UniProtKB: P49761]
There should be some charts here, you may need to enable JavaScript!
  • CDC like kinase 4/Dual specificity protein kinase CLK4 in Human [ChEMBL: CHEMBL4203] [GtoPdb: 1993] [UniProtKB: Q9HAZ1]
There should be some charts here, you may need to enable JavaScript!
  • dual specificity tyrosine phosphorylation regulated kinase 1A/Dual-specificity tyrosine-phosphorylation regulated kinase 1A in Human [ChEMBL: CHEMBL2292] [GtoPdb: 2009] [UniProtKB: Q13627]
There should be some charts here, you may need to enable JavaScript!
  • dual specificity tyrosine phosphorylation regulated kinase 1B/Dual specificity tyrosine-phosphorylation-regulated kinase 1B in Human [ChEMBL: CHEMBL5543] [GtoPdb: 2010] [UniProtKB: Q9Y463]
There should be some charts here, you may need to enable JavaScript!
  • dual specificity tyrosine phosphorylation regulated kinase 2/Dual-specificity tyrosine-phosphorylation regulated kinase 2 in Human [ChEMBL: CHEMBL4376] [GtoPdb: 2011] [UniProtKB: Q92630]
There should be some charts here, you may need to enable JavaScript!
  • dual specificity tyrosine phosphorylation regulated kinase 3/Dual-specificity tyrosine-phosphorylation regulated kinase 3 in Human [ChEMBL: CHEMBL4575] [GtoPdb: 2012] [UniProtKB: O43781]
There should be some charts here, you may need to enable JavaScript!
  • dual specificity tyrosine phosphorylation regulated kinase 4/Dual specificity tyrosine-phosphorylation-regulated kinase 4 in Human [ChEMBL: CHEMBL1075115] [GtoPdb: 2013] [UniProtKB: Q9NR20]
There should be some charts here, you may need to enable JavaScript!
  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
casein kinase 1 epsilon/Casein kinase I epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674]
ChEMBL Inhibition of recombinant human CK1epsilon expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 5 pIC50 >10000 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078]
ChEMBL 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 scintillation counter analysis B 5 pIC50 >10000 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
CDC like kinase 1/Dual specificity protein kinase CLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759]
ChEMBL Binding affinity to human CLK1 assessed as equilibrium dissociation constant measured upto 240 min by TR-FRET assay B 8.55 pKd 2.79 nM Kd J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL Inhibition of human recombinant CLK1 (148 to 484 amino acids) expressed in Escherichia coli BL21(DE3) using AFRREWSPGKEAKK as substrate preincubated for 10 mins prior to substrate addition by LDH assay B 7.7 pIC50 20 nM IC50 Bioorg Med Chem Lett (2013) 23: 3654-3661 [PMID:23642479]
ChEMBL Inhibition of CLK1 (unknown origin) using AFRREWSPGKEAKK peptide substrate B 7.71 pIC50 19.7 nM IC50 Eur J Med Chem (2023) 250: 115168-115168 [PMID:36780830]
GtoPdb - - 7.71 pIC50 19.7 nM IC50 Chem Biol (2011) 18: 67-76 [PMID:21276940]
ChEMBL Inhibition of recombinant human CLK1 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 7.87 pIC50 13.5 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL Inhibition of recombinant human CLK1 expressed in Sf9 insect cells using myelin basic protein as substrate incubated for 110 mins in presence of ATP by non-radioactive ADP-Glo luminescence microplate reader assay B 7.9 pIC50 12.6 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL Inhibition of recombinant human CLK1 (130 to end residues) using ERMRPRKRQGSVRRRV as substrate incubated for 40 mins in presence of [gamma33P-ATP] by scintillation counting analysis B 8.1 pIC50 8 nM IC50 Bioorg Med Chem (2021) 31: 115962-115962 [PMID:33422908]
CDC like kinase 2/Dual specificity protein kinase CLK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4225] [GtoPdb: 1991] [UniProtKB: P49760]
ChEMBL Inhibition of recombinant human CLK2 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 7.3 pIC50 49.6 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL Inhibition of CLK2 (unknown origin) B 7.7 pIC50 20 nM IC50 Bioorg Med Chem (2022) 70: 116921-116921 [PMID:35863237]
CDC like kinase 3/Dual specificity protein kinase CLK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4226] [GtoPdb: 1992] [UniProtKB: P49761]
ChEMBL Inhibition of recombinant human CLK3 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 6.02 pIC50 965.5 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL Inhibition of human recombinant CLK3 (275 to 632 amino acids) expressed in Escherichia coli BL21(DE3) preincubated for 10 mins prior to substrate addition by LDH assay B 6.28 pIC50 530 nM IC50 Bioorg Med Chem Lett (2013) 23: 3654-3661 [PMID:23642479]
GtoPdb - - 6.28 pIC50 530 nM IC50 Chem Biol (2011) 18: 67-76 [PMID:21276940]
CDC like kinase 4/Dual specificity protein kinase CLK4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4203] [GtoPdb: 1993] [UniProtKB: Q9HAZ1]
ChEMBL Inhibition of recombinant human CLK4 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 7.83 pIC50 14.8 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
dual specificity tyrosine phosphorylation regulated kinase 1A/Dual-specificity tyrosine-phosphorylation regulated kinase 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2292] [GtoPdb: 2009] [UniProtKB: Q13627]
ChEMBL Binding affinity to human DYRK1A assessed as equilibrium dissociation constant measured upto 240 min by TR-FRET assay B 6.96 pKd 108.63 nM Kd J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL Inhibition of DYRK1A (unknown origin) using YRASPSRPESPRPPA peptide substrate B 7.26 pIC50 55.2 nM IC50 Eur J Med Chem (2023) 250: 115168-115168 [PMID:36780830]
ChEMBL Inhibition of DYRK1A (unknown origin) using YRASPSRPESPRPPA-NH2 as substrate preincubated for 10 mins prior to substrate addition by LDH assay B 7.26 pIC50 55 nM IC50 Bioorg Med Chem Lett (2013) 23: 3654-3661 [PMID:23642479]
ChEMBL Inhibition of DYRK1A (unknown origin) using YRASPSRPESPRPPA-amide as substrate preincubated for 10 mins followed by substrate addition and measured after 60 mins by caliper mobility shift assay B 7.26 pIC50 55 nM IC50 J Med Chem (2018) 61: 9791-9810 [PMID:29985601]
ChEMBL Inhibition of DYRK1A (unknown origin) B 7.26 pIC50 55 nM IC50 Bioorg Med Chem (2022) 70: 116921-116921 [PMID:35863237]
GtoPdb - - 7.26 pIC50 55.2 nM IC50 Chem Biol (2011) 18: 67-76 [PMID:21276940]
ChEMBL Inhibition of recombinant human DYRK1A expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 7.55 pIC50 28.1 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL Inhibition of recombinant human DYRK1A expressed in Escherichia coli using DYRKtide peptide as substrate incubated for 110 mins in presence of ATP by non-radioactive ADP-Glo luminescence microplate reader assay B 7.67 pIC50 21.5 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
dual specificity tyrosine phosphorylation regulated kinase 1B/Dual specificity tyrosine-phosphorylation-regulated kinase 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5543] [GtoPdb: 2010] [UniProtKB: Q9Y463]
ChEMBL Inhibition of recombinant human DYRK1B expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 6.73 pIC50 186.6 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL Inhibition of recombinant human DYRK1B expressed in Sf9 insect cells using DYRKtide peptide as substrate incubated for 110 mins in presence of ATP by non-radioactive ADP-Glo luminescence microplate reader assay B 7.09 pIC50 81.2 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
dual specificity tyrosine phosphorylation regulated kinase 2/Dual-specificity tyrosine-phosphorylation regulated kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4376] [GtoPdb: 2011] [UniProtKB: Q92630]
ChEMBL Inhibition of recombinant human DYRK2 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 5 pIC50 >10000 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
dual specificity tyrosine phosphorylation regulated kinase 3/Dual-specificity tyrosine-phosphorylation regulated kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4575] [GtoPdb: 2012] [UniProtKB: O43781]
ChEMBL Inhibition of recombinant human DYRK3 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 5 pIC50 >10000 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
dual specificity tyrosine phosphorylation regulated kinase 4/Dual specificity tyrosine-phosphorylation-regulated kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075115] [GtoPdb: 2013] [UniProtKB: Q9NR20]
ChEMBL Inhibition of recombinant human DYRK4 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 5 pIC50 >10000 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
ChEMBL Binding affinity to human GSK-3beta assessed as equilibrium dissociation constant measured upto 240 min by TR-FRET assay B 5 pKd >10000 nM Kd J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL 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 scintillation counter analysis B 5 pIC50 >10000 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]