Cdk1/2 inhibitor III [Ligand Id: 5946] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL261720
  • casein kinase 2, alpha prime polypeptide subunit/casein kinase 2, beta polypeptide subunit/casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II in Human [ChEMBL: CHEMBL2095191] [GtoPdb: 155015511549] [UniProtKB: P19784P67870P68400]
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  • cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535Q15078]
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  • CDC like kinase 3/Dual specificity protein kinase CLK3 in Human [ChEMBL: CHEMBL4226] [GtoPdb: 1992] [UniProtKB: P49761]
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  • CDC like kinase 1/Dual specificty protein kinase CLK1 in Human [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759]
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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
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  • eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525]
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  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
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  • fms related receptor tyrosine kinase 1 in Human [GtoPdb: 1812] [UniProtKB: P17948]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
casein kinase 2, alpha prime polypeptide subunit/casein kinase 2, beta polypeptide subunit/casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2095191] [GtoPdb: 155015511549] [UniProtKB: P19784P67870P68400]
ChEMBL Inhibition of Casein kinase-2 B 4 pIC50 >100000 nM IC50 J. Med. Chem. (2005) 48: 4208-4211 [PMID:15974571]
cyclin dependent kinase 2/CDK2/Cyclin A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038469] [GtoPdb: 1973] [UniProtKB: P20248P24941]
GtoPdb CDK2/cyclin A complex - 9.3 pIC50 0.5 nM IC50 J Med Chem (2005) 48: 4208-11 [PMID:15974571]
ChEMBL Inhibition of GST-tagged CDK2/cyclin A2 (unknown origin) expressed in Escherichia coli using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay B 9.7 pIC50 0.2 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
cyclin dependent kinase 7/CDK7/Cyclin H/MNAT1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038473] [GtoPdb: 1979] [UniProtKB: P50613P51946P51948]
ChEMBL Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay B 7.18 pIC50 66 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
cyclin dependent kinase 9/CDK9/cyclin T1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111389] [GtoPdb: 1981] [UniProtKB: O60563P50750]
ChEMBL Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay B 7.52 pIC50 30 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094127] [GtoPdb: 1961] [UniProtKB: O95067P06493P14635Q8WWL7]
GtoPdb CDK1/cyclin B complex - 9.22 pIC50 0.6 nM IC50 J Med Chem (2005) 48: 4208-11 [PMID:15974571]
ChEMBL Inhibition of Cyclin B-cyclin-dependent kinase 1 B 9.22 pIC50 0.6 nM IC50 J. Med. Chem. (2005) 48: 4208-4211 [PMID:15974571]
ChEMBL Inhibition of Cyclin B-cyclin-dependent kinase 1 B 9.22 pIC50 0.6 nM IC50 J. Med. Chem. (2005) 48: 4208-4211 [PMID:15974571]
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907602] [GtoPdb: 1961] [UniProtKB: P06493P14635]
ChEMBL Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay B 8.7 pIC50 2 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
GtoPdb CDK1/cyclin B complex - 9.22 pIC50 0.6 nM IC50 J Med Chem (2005) 48: 4208-11 [PMID:15974571]
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094128] [GtoPdb: 1973] [UniProtKB: P20248P24941P78396]
GtoPdb CDK2/cyclin A complex - 9.3 pIC50 0.5 nM IC50 J Med Chem (2005) 48: 4208-11 [PMID:15974571]
ChEMBL Inhibition of Cyclin-dependent kinase 2-cyclin A B 9.3 pIC50 0.5 nM IC50 J. Med. Chem. (2005) 48: 4208-4211 [PMID:15974571]
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907605] [GtoPdb: 1973] [UniProtKB: P24864P24941]
ChEMBL Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay B 8.52 pIC50 3 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
GtoPdb CDK2/cyclin A complex - 9.3 pIC50 0.5 nM IC50 J Med Chem (2005) 48: 4208-11 [PMID:15974571]
cyclin dependent kinase 4/Cyclin-dependent kinase 4/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907601] [GtoPdb: 1976] [UniProtKB: P11802P24385]
ChEMBL Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay B 7.23 pIC50 59 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535Q15078]
ChEMBL Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay B 9.7 pIC50 0.2 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
CDC like kinase 3/Dual specificity protein kinase CLK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4226] [GtoPdb: 1992] [UniProtKB: P49761]
ChEMBL Inhibition of human CLK3 (275 to 632 residues) expressed in Escherichia coli BL21(DE3) preincubated for 10 mins followed by substrate addition by pyruvate kinase and lactate dehydrogenase coupled enzyme assay B 7.53 pIC50 29.2 nM IC50 Eur J Med Chem (2017) 126: 754-761 [PMID:27940419]
CDC like kinase 1/Dual specificty protein kinase CLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759]
ChEMBL Inhibition of human CLK1 (148 to 484 residues) expressed in Escherichia coli BL21(DE3) preincubated for 10 mins followed by AFRREWSPGKEAKK substrate addition by pyruvate kinase and lactate dehydrogenase coupled enzyme assay B 8.05 pIC50 8.9 nM IC50 Eur J Med Chem (2017) 126: 754-761 [PMID:27940419]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibition of Epidermal growth factor receptor B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2005) 48: 4208-4211 [PMID:15974571]
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
ChEMBL Inhibition of human GSK3beta using Biotin-labeled GSP-2 peptide substrate after 90 mins in presence of [gamma33-P]ATP by scintillation proximity assay B 6.68 pIC50 210 nM IC50 Eur J Med Chem (2017) 126: 754-761 [PMID:27940419]
ChEMBL Inhibition of GSK3-beta B 6.85 pIC50 140 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213]
ChEMBL Inhibition of Insulin kinase-beta activity B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2005) 48: 4208-4211 [PMID:15974571]
eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525]
ChEMBL Inhibition of human recombinant PKR autophosphorylation using poly[I:C] after 10 mins by luminescent assay B 5.8 pIC50 1600 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 4108-4114 [PMID:21632247]
Plasmodium berghei (target type: ORGANISM) [ChEMBL: CHEMBL612653]
ChEMBL HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells F 6.33 pIC50 472 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2012) 109: 8511-8516 [PMID:22586124]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL HARVARD: Inhibition of blood stage Plasmodium falciparum Dd2 infection F 6.59 pIC50 258 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2012) 109: 8511-8516 [PMID:22586124]
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
ChEMBL Inhibition of Vascular endothelial growth factor receptor 2 B 7.49 pIC50 32 nM IC50 J. Med. Chem. (2005) 48: 4208-4211 [PMID:15974571]
ChEMBL Inhibition of VEGFR2 B 7.49 pIC50 32 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
fms related receptor tyrosine kinase 1 in Human [GtoPdb: 1812] [UniProtKB: P17948]
GtoPdb - - 7.49 pIC50 32 nM IC50 J Med Chem (2005) 48: 4208-11 [PMID:15974571]

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]