Cdc2-like kinase inhibitor [Ligand Id: 5942] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL408982
  • bromodomain containing 9/Bromodomain-containing protein 9 in Human [ChEMBL: CHEMBL3108640] [GtoPdb: 2728] [UniProtKB: Q9H8M2]
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  • casein kinase 1 delta/Casein kinase I delta in Human [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730]
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  • casein kinase 1 epsilon/Casein kinase I epsilon in Human [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674]
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  • casein kinase 1 gamma 2/Casein kinase I gamma 2 in Human [ChEMBL: CHEMBL2543] [GtoPdb: 2000] [UniProtKB: P78368]
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  • casein kinase 1 gamma 3/Casein kinase I isoform gamma-3 in Human [ChEMBL: CHEMBL5084] [GtoPdb: 2001] [UniProtKB: Q9Y6M4]
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  • CDC like kinase 1/Dual specificity protein kinase CLK1 in Mouse [ChEMBL: CHEMBL1075280] [GtoPdb: 1990] [UniProtKB: P22518]
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  • CDC like kinase 2/Dual specificity protein kinase CLK2 in Human [ChEMBL: CHEMBL4225] [GtoPdb: 1991] [UniProtKB: P49760]
  • CDC like kinase 2/Dual specificity protein kinase CLK2 in Mouse [ChEMBL: CHEMBL1075281] [GtoPdb: 1991] [UniProtKB: O35491]
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  • CDC like kinase 3/Dual specificity protein kinase CLK3 in Human [ChEMBL: CHEMBL4226] [GtoPdb: 1992] [UniProtKB: P49761]
  • CDC like kinase 3/Dual specificity protein kinase CLK3 in Mouse [ChEMBL: CHEMBL1075282] [GtoPdb: 1992] [UniProtKB: O35492]
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  • CDC like kinase 4/Dual specificity protein kinase CLK4 in Human [ChEMBL: CHEMBL4203] [GtoPdb: 1993] [UniProtKB: Q9HAZ1]
  • CDC like kinase 4/Dual specificity protein kinase CLK4 in Mouse [ChEMBL: CHEMBL1075283] [GtoPdb: 1993] [UniProtKB: O35493]
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  • dual specificity tyrosine phosphorylation regulated kinase 1A/Dual-specificity tyrosine-phosphorylation regulated kinase 1A in Human [ChEMBL: CHEMBL2292] [GtoPdb: 2009] [UniProtKB: Q13627]
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  • dual specificity tyrosine phosphorylation regulated kinase 1B/Dual specificity tyrosine-phosphorylation-regulated kinase 1B in Human [ChEMBL: CHEMBL5543] [GtoPdb: 2010] [UniProtKB: Q9Y463]
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  • CDC like kinase 1/Dual specificty protein kinase CLK1 in Human [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759]
  • CDC like kinase 1 in Mouse [GtoPdb: 1990] [UniProtKB: P22518]
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  • Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309]
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  • Pim-3 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM3 in Human [ChEMBL: CHEMBL5407] [GtoPdb: 2160] [UniProtKB: Q86V86]
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  • mitogen-activated protein kinase kinase kinase 19/SPS1/STE20-related protein kinase YSK4 in Human [ChEMBL: CHEMBL6191] [GtoPdb: 2076] [UniProtKB: Q56UN5]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
bromodomain containing 9/Bromodomain-containing protein 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3108640] [GtoPdb: 2728] [UniProtKB: Q9H8M2]
ChEMBL Binding affinity to recombinant human His-tagged BRD9 (134 to 239 residues) expressed in Escherichia coli BL21 DE3 assessed as dissociation constant by isothermal titration calorimetry B 4.8 pKd 16000 nM Kd J Med Chem (2020) 63: 3227-3237 [PMID:32091206]
ChEMBL Binding affinity to BRD9 (unknown origin) assessed as dissociation constant by qPCR analysis B 5.1 pKd 8000 nM Kd J Med Chem (2020) 63: 3227-3237 [PMID:32091206]
casein kinase 1 delta/Casein kinase I delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730]
ChEMBL Binding affinity to CSNK1D assessed as dissociation constant B 6.82 pKd 150 nM Kd Bioorg. Med. Chem. Lett. (2009) 19: 6700-6705 [PMID:19837585]
casein kinase 1 epsilon/Casein kinase I epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674]
ChEMBL Binding affinity to CSNK1E assessed as dissociation constant B 6.52 pKd 300 nM Kd Bioorg. Med. Chem. Lett. (2009) 19: 6700-6705 [PMID:19837585]
casein kinase 1 gamma 2/Casein kinase I gamma 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2543] [GtoPdb: 2000] [UniProtKB: P78368]
ChEMBL Binding affinity to CSNK1G2 assessed as dissociation constant B 6.57 pKd 270 nM Kd Bioorg. Med. Chem. Lett. (2009) 19: 6700-6705 [PMID:19837585]
casein kinase 1 gamma 3/Casein kinase I isoform gamma-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5084] [GtoPdb: 2001] [UniProtKB: Q9Y6M4]
ChEMBL Binding affinity to CSNK1G3 assessed as dissociation constant B 6.54 pKd 290 nM Kd Bioorg. Med. Chem. Lett. (2009) 19: 6700-6705 [PMID:19837585]
CDC like kinase 1/Dual specificity protein kinase CLK1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075280] [GtoPdb: 1990] [UniProtKB: P22518]
GtoPdb - - 8 pKi 10 nM Ki Proc Natl Acad Sci USA (2007) 104: 20523-8 [PMID:18077363]
ChEMBL Inhibition of mouse Clk1 B 8 pKi 10 nM Ki Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
ChEMBL Inhibition of mouse Clk1 B 7.7 pIC50 20 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
ChEMBL Inhibition of mouse recombinant GST-tagged CLK1 expressed in Escherichia coli DH5[alpha] using NH2-RSPSYGRSRSRSRSRSRSRSRSNSRSRSY-OH as substrate by liquid scintillation counting analysis B 7.7 pIC50 20 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 3654-3661 [PMID:23642479]
GtoPdb - - 7.7 pIC50 20 nM IC50 Proc Natl Acad Sci USA (2007) 104: 20523-8 [PMID:18077363]
CDC like kinase 2/Dual specificity protein kinase CLK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4225] [GtoPdb: 1991] [UniProtKB: P49760]
ChEMBL Binding affinity to Clk2 assessed as dissociation constant B 7.02 pKd 95 nM Kd Bioorg. Med. Chem. Lett. (2009) 19: 6700-6705 [PMID:19837585]
CDC like kinase 2/Dual specificity protein kinase CLK2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075281] [GtoPdb: 1991] [UniProtKB: O35491]
ChEMBL Inhibition of mouse Clk2 B 6.7 pIC50 200 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
ChEMBL Inhibition of mouse recombinant GST-tagged CLK2 expressed in Escherichia coli DH5[alpha] using NH2-RSPSYGRSRSRSRSRSRSRSRSNSRSRSY-OH as substrate by liquid scintillation counting analysis B 6.7 pIC50 200 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 3654-3661 [PMID:23642479]
GtoPdb - - 6.7 pIC50 200 nM IC50 Proc Natl Acad Sci USA (2007) 104: 20523-8 [PMID:18077363]
CDC like kinase 3/Dual specificity protein kinase CLK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4226] [GtoPdb: 1992] [UniProtKB: P49761]
ChEMBL Binding affinity to Clk3 assessed as dissociation constant B 5.52 pKd 3000 nM Kd Bioorg. Med. Chem. Lett. (2009) 19: 6700-6705 [PMID:19837585]
CDC like kinase 3/Dual specificity protein kinase CLK3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075282] [GtoPdb: 1992] [UniProtKB: O35492]
ChEMBL Inhibition of mouse Clk3 B 5 pIC50 >10000 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
CDC like kinase 4/Dual specificity protein kinase CLK4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4203] [GtoPdb: 1993] [UniProtKB: Q9HAZ1]
ChEMBL Binding affinity to Clk4 assessed as dissociation constant B 7.52 pKd 30 nM Kd Bioorg. Med. Chem. Lett. (2009) 19: 6700-6705 [PMID:19837585]
CDC like kinase 4/Dual specificity protein kinase CLK4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075283] [GtoPdb: 1993] [UniProtKB: O35493]
ChEMBL Inhibition of mouse Clk4 B 7.82 pIC50 15 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
ChEMBL Inhibition of mouse recombinant GST-tagged CLK4 expressed in Escherichia coli DH5[alpha] using NH2-RSPSYGRSRSRSRSRSRSRSRSNSRSRSY-OH as substrate by liquid scintillation counting analysis B 7.82 pIC50 15 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 3654-3661 [PMID:23642479]
ChEMBL Inhibition of GST-tagged mouse CLK4 expressed in Escherichia coli using NH2-RSPSYGRSRSRSRSRSRSRSRSNSRSRSY-OH as substrate after 10 mins in presence of [gamma-32]-ATP by scintillation counting method B 7.82 pIC50 15 nM IC50 J Med Chem (2017) 60: 5377-5391 [PMID:28561591]
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 Dyrk1A assessed as dissociation constant B 7.92 pKd 12 nM Kd Bioorg. Med. Chem. Lett. (2009) 19: 6700-6705 [PMID:19837585]
ChEMBL Inhibition of DYRK1A (unknown origin) B 6.03 pIC50 930 nM IC50 J. Med. Chem. (2013) 56: 9569-9585 [PMID:24188002]
ChEMBL Inhibition of Dyrk1A (unknown origin) B 6.03 pIC50 930 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 2948-2952 [PMID:26048785]
ChEMBL Inhibition of human recombinant full length GST-tagged DYRK1A expressed in baculovirus expression system after 10 mins in presence of [gamma33P-ATP] by liquid scintillation counting analysis B 6.03 pIC50 930 nM IC50 J Med Chem (2018) 61: 9791-9810 [PMID:29985601]
ChEMBL Inhibition of recombinant Dyrk1A (unknown origin) using KKISGRLSPIMTEQ-NH2 peptide substrate B 6.08 pIC50 830 nM IC50 ACS Med. Chem. Lett. (2014) 5: 963-967 [PMID:25221649]
ChEMBL Inhibition of Dyrk1A kinase B 7.92 pIC50 12 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 3152-3158 [PMID:21450467]
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 Binding affinity to Dyrk1B assessed as dissociation constant B 6.89 pKd 130 nM Kd Bioorg. Med. Chem. Lett. (2009) 19: 6700-6705 [PMID:19837585]
CDC like kinase 1/Dual specificty protein kinase CLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759]
ChEMBL Binding affinity to Clk1 assessed as dissociation constant B 7.72 pKd 19 nM Kd Bioorg. Med. Chem. Lett. (2009) 19: 6700-6705 [PMID:19837585]
ChEMBL Inhibition of recombinant Clk1 (unknown origin) using GRSRSRSRSR peptide substrate B 6.77 pIC50 170 nM IC50 ACS Med. Chem. Lett. (2014) 5: 963-967 [PMID:25221649]
ChEMBL Inhibition of human C-terminus CLK1 (148 to 484 residues) expressed in Escherichia coli BL21(DE3) using AFRREWSPGKEAKK as substrate preincubated for 10 mins followed by ATP addition by pyruvate kinase-lactate dehydrogenase coupled assay B 7.31 pIC50 49 nM IC50 J Med Chem (2017) 60: 5377-5391 [PMID:28561591]
ChEMBL Inhibition of recombinant human CLK1 expressed in insect cells using ERMRPRKRQGSVRRRV peptide as substrate after 40 mins in presence of [gamma-33P]-ATP by scintillation counting B 7.77 pIC50 17 nM IC50 J Med Chem (2017) 60: 6337-6352 [PMID:28692292]
CDC like kinase 1 in Mouse [GtoPdb: 1990] [UniProtKB: P22518]
GtoPdb - - 8 pKi 10 nM Ki Proc Natl Acad Sci USA (2007) 104: 20523-8 [PMID:18077363]
GtoPdb - - 7.7 pIC50 20 nM IC50 Proc Natl Acad Sci USA (2007) 104: 20523-8 [PMID:18077363]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309]
ChEMBL Binding affinity to PIM1 assessed as dissociation constant B 6.89 pKd 130 nM Kd Bioorg. Med. Chem. Lett. (2009) 19: 6700-6705 [PMID:19837585]
Pim-3 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5407] [GtoPdb: 2160] [UniProtKB: Q86V86]
ChEMBL Binding affinity to PIM3 assessed as dissociation constant B 6.55 pKd 280 nM Kd Bioorg. Med. Chem. Lett. (2009) 19: 6700-6705 [PMID:19837585]
mitogen-activated protein kinase kinase kinase 19/SPS1/STE20-related protein kinase YSK4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6191] [GtoPdb: 2076] [UniProtKB: Q56UN5]
ChEMBL Binding affinity to Ysk4 assessed as dissociation constant B 6.54 pKd 290 nM Kd Bioorg. Med. Chem. Lett. (2009) 19: 6700-6705 [PMID:19837585]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]