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 Human [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759]
  • 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]
  • dual specificity tyrosine phosphorylation regulated kinase 1A/Dual-specificity tyrosine-phosphorylation regulated kinase 1A in Mouse [ChEMBL: CHEMBL4750] [GtoPdb: 2009] [UniProtKB: Q61214]
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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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  • 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 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 CLK1 (unknown origin) B 7.7 pIC50 20 nM IC50 Bioorg Med Chem (2022) 62: 116706-116706 [PMID:35364524]
ChEMBL Inhibition of Clk1 (unknown origin) using synthetic peptide of SF2/ASF RS domain by [gamma-32P]ATP binding assay B 7.7 pIC50 20 nM IC50 Eur J Med Chem (2023) 250: 115168-115168 [PMID:36780830]
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/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]
ChEMBL Inhibition of mouse glutathione S-transferase-tagged Clk1 expressed in Escherichia coli DH5alpha using NH2-RSPSYGRSRSRSRSRSRSRSRSNSRSRSY-OH peptide as substrate in presence of [gamma 32P-ATP] and ATP by liquid scintillation counting method B 7.7 pIC50 20 nM IC50 Eur J Med Chem (2022) 238: 114411-114411 [PMID:35635953]
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]
ChEMBL Binding affinity to CLK2 (unknown origin) assessed as dissociation constant B 7.72 pKd 19 nM Kd Bioorg Med Chem (2022) 70: 116921-116921 [PMID:35863237]
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]
ChEMBL Inhibition of mouse glutathione S-transferase-tagged Clk2 expressed in Escherichia coli DH5alpha using NH2-RSPSYGRSRSRSRSRSRSRSRSNSRSRSY-OH peptide as substrate in presence of [gamma 32P-ATP] and ATP by liquid scintillation counting method B 6.7 pIC50 200 nM IC50 Eur J Med Chem (2022) 238: 114411-114411 [PMID:35635953]
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]
ChEMBL Inhibition of GST-tagged recombinant mouse CLK4 expressed in Escherichia coli using RSPSYGRSRSRSRSRSRSRSRSNSRSRSY as substrate in presence of [gamma-32P]ATP by a liquid scintillation counter method B 7.82 pIC50 15 nM IC50 Bioorg Med Chem (2022) 70: 116914-116914 [PMID:35872347]
ChEMBL Inhibition of mouse glutathione S-transferase-tagged Clk4 expressed in Escherichia coli DH5alpha using NH2-RSPSYGRSRSRSRSRSRSRSRSNSRSRSY-OH peptide as substrate in presence of [gamma 32P-ATP] and ATP by liquid scintillation counting method B 7.82 pIC50 15 nM IC50 Eur J Med Chem (2022) 238: 114411-114411 [PMID:35635953]
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 Binding affinity to DYRK1A (unknown origin) assessed as dissociation constant B 7.92 pKd 12 nM Kd Bioorg Med Chem (2022) 70: 116921-116921 [PMID:35863237]
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 (unknown origin) B 7.4 pIC50 40 nM IC50 Eur J Med Chem (2023) 250: 115168-115168 [PMID:36780830]
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 1A/Dual-specificity tyrosine-phosphorylation regulated kinase 1A in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4750] [GtoPdb: 2009] [UniProtKB: Q61214]
ChEMBL Inhibition of mouse glutathione S-transferase-tagged Dyrk1A expressed in Escherichia coli DH5alpha using NH2-RSPSYGRSRSRSRSRSRSRSRSNSRSRSY-OH peptide as substrate in presence of [gamma 32P-ATP] and ATP by liquid scintillation counting method B 7.92 pIC50 12 nM IC50 Eur J Med Chem (2022) 238: 114411-114411 [PMID:35635953]
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]
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 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]