kenpaullone [Ligand Id: 6000] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL296586 (Kenpaullone)
  • casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II alpha in Human [ChEMBL: CHEMBL3629] [GtoPdb: 1549] [UniProtKB: P68400]
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  • cyclin dependent kinase 1 in spiny starfish [GtoPdb: 1961]
  • cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493]
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  • cyclin dependent kinase 1 in spiny starfish [GtoPdb: 1961]
  • cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B1 in Human [ChEMBL: CHEMBL1907602] [GtoPdb: 1961] [UniProtKB: P06493, P14635]
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  • cyclin dependent kinase 2 in spiny starfish [GtoPdb: 1973]
  • cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin A in Human [ChEMBL: CHEMBL2094128] [GtoPdb: 1973] [UniProtKB: P20248, P24941, P78396]
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  • cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078]
  • cyclin dependent kinase 5 in Bovine [GtoPdb: 1977]
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  • dual specificity tyrosine phosphorylation regulated kinase 1A/Dual specificity tyrosine-phosphorylation-regulated kinase 1A in Rat [ChEMBL: CHEMBL5508] [GtoPdb: 2009] [UniProtKB: Q63470]
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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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  • Glycogen synthase kinase 3 in Plasmodium falciparum 3D7 [ChEMBL: CHEMBL1781857] [UniProtKB: O77344]
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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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  • mitogen-activated protein kinase 3/MAP kinase ERK1 in Human [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361]
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  • mitogen-activated protein kinase 1/MAP kinase ERK2 in Human [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
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  • sirtuin 2/NAD-dependent deacetylase sirtuin 2 in Human [ChEMBL: CHEMBL4462] [GtoPdb: 2708] [UniProtKB: Q8IXJ6]
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  • Protein kinase Pfmrk in Plasmodium falciparum [ChEMBL: CHEMBL4090] [UniProtKB: P90584]
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  • polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350]
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  • LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
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  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
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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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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3629] [GtoPdb: 1549] [UniProtKB: P68400]
ChEMBL Inhibition of CK2 B 4.7 pIC50 20000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
Casein kinase I isoform alpha in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1781858] [UniProtKB: O19175]
ChEMBL Inhibition of porcine brain CK1 assessed as incorporation of [gamma-33P]-ATP into RRKHAAIGpSAYSITA substrate after 30 mins by scintillation counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2010) 20: 4940-4944 [PMID:20621478]
cyclin dependent kinase 9/CDK9/cyclin T1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111389] [GtoPdb: 1981] [UniProtKB: O60563, P50750]
ChEMBL Inhibition of human recombinant CDK9/cyclin T expressed in insect cells assessed as incorporation of [gamma-33P]-ATP in to pRB fragment (773 to 928) substrate after 30 mins by scintillation counting B 7.19 pIC50 64 nM IC50 Bioorg Med Chem Lett (2010) 20: 4940-4944 [PMID:20621478]
cyclin dependent kinase 1 in spiny starfish [GtoPdb: 1961]
GtoPdb CDK1/cyclin B complex - 6.4 pIC50 400 nM IC50 Cancer Res (1999) 59: 2566-9 [PMID:10363974]
cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493]
ChEMBL In vitro inhibitory activity against cyclin-dependent kinase 1-cyclin B (Cyclin-Dependent Kinase) harvested from starfish oocytes. B 6.4 pIC50 400 nM IC50 J Med Chem (1999) 42: 2909-2919 [PMID:10425100]
cyclin dependent kinase 1 in spiny starfish [GtoPdb: 1961]
GtoPdb CDK1/cyclin B complex - 6.4 pIC50 400 nM IC50 Cancer Res (1999) 59: 2566-9 [PMID:10363974]
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094127] [GtoPdb: 1961] [UniProtKB: O95067, P06493, P14635, Q8WWL7]
ChEMBL Inhibition of Cyclin-dependent kinase 1-cyclin B from Starfish oocytes B 6.4 pIC50 400 nM IC50 Bioorg Med Chem Lett (2000) 10: 567-569 [PMID:10741555]
ChEMBL Inhibition of Cyclin-dependent kinase 1-cyclin B from M phase starfish (Marthasterias glacialis) oocytes B 6.4 pIC50 400 nM IC50 J Med Chem (2003) 46: 876-879 [PMID:12593668]
ChEMBL Inhibition of human cyclin-dependent kinase 1-cyclin B B 6.4 pIC50 400 nM IC50 Bioorg Med Chem Lett (2004) 14: 413-416 [PMID:14698171]
ChEMBL Inhibition of CDK1/cyclin B expressed in M phase starfish oocyte B 6.4 pIC50 400 nM IC50 Eur J Med Chem (2010) 45: 335-342 [PMID:19906467]
ChEMBL Inhibition of CDK1/cyclinB B 6.4 pIC50 400 nM IC50 Trends Pharmacol Sci (2004) 25: 471-480 [PMID:15559249]
ChEMBL Inhibitory activity against cyclin dependent kinase 1-cyclinB extracted from M phase starfish (Marthasterias glacialis) oocytes B 6.4 pIC50 399.94 nM IC50 J Med Chem (2004) 47: 22-36 [PMID:14695817]
cyclin dependent kinase 1 in spiny starfish [GtoPdb: 1961]
GtoPdb CDK1/cyclin B complex - 6.4 pIC50 400 nM IC50 Cancer Res (1999) 59: 2566-9 [PMID:10363974]
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907602] [GtoPdb: 1961] [UniProtKB: P06493, P14635]
ChEMBL Inhibition of human GST-CDK1/cyclin B1 expressed in baculovirus using [gamma-33P]ATP after 45 mins by liquid scintillation counting B 6.4 pIC50 400 nM IC50 Eur J Med Chem (2010) 45: 4316-4330 [PMID:20638755]
ChEMBL Inhibition of CDK1/cyclin B B 6.4 pIC50 400 nM IC50 Bioorg Med Chem Lett (2010) 20: 4940-4944 [PMID:20621478]
ChEMBL Inhibition of GST-tagged CDK1/cyclin B (unknown origin) expressed in Escherichia coli B 6.4 pIC50 400 nM IC50 Eur J Med Chem (2017) 142: 244-265 [PMID:28803677]
cyclin dependent kinase 2 in spiny starfish [GtoPdb: 1973]
GtoPdb CDK2/cyclin A complex - 6.17 pIC50 680 nM IC50 Cancer Res (1999) 59: 2566-9 [PMID:10363974]
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094128] [GtoPdb: 1973] [UniProtKB: P20248, P24941, P78396]
ChEMBL Inhibition of human recombinant CDK2/cyclin A assessed as incorporation of [gamma-33P]-ATP into histone H1 substrate after 30 mins by scintillation counting B 6.11 pIC50 780 nM IC50 Bioorg Med Chem Lett (2010) 20: 4940-4944 [PMID:20621478]
ChEMBL Inhibition of CDK2/cyclin A B 6.17 pIC50 680 nM IC50 Eur J Med Chem (2012) 56: 246-253 [PMID:22995819]
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 human recombinant CDK5/p25 assessed as incorporation of [gamma-33P]-ATP into histone H1 substrate after 30 mins by scintillation counting B 6 pIC50 1000 nM IC50 Bioorg Med Chem Lett (2010) 20: 4940-4944 [PMID:20621478]
ChEMBL Inhibition of Cyclin-dependent kinase 5 (CDK5) B 6.07 pIC50 850 nM IC50 J Med Chem (2003) 46: 876-879 [PMID:12593668]
ChEMBL Inhibition of human Cyclin-dependent kinase 5-p35nck5a B 6.07 pIC50 850 nM IC50 Bioorg Med Chem Lett (2004) 14: 413-416 [PMID:14698171]
ChEMBL Inhibition of recombinant CDK5/p25 expressed in Escherichia coli B 6.07 pIC50 850 nM IC50 J Med Chem (2008) 51: 2196-2207 [PMID:18345612]
ChEMBL Inhibition of Cyclin-dependent kinase 5-p35nck5a B 6.07 pIC50 849.18 nM IC50 J Med Chem (2004) 47: 22-36 [PMID:14695817]
cyclin dependent kinase 5 in Bovine [GtoPdb: 1977]
GtoPdb CDK5/p25 complex - 6.07 pIC50 850 nM IC50 Cancer Res (1999) 59: 2566-9 [PMID:10363974]
dual specificity tyrosine phosphorylation regulated kinase 1A/Dual specificity tyrosine-phosphorylation-regulated kinase 1A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5508] [GtoPdb: 2009] [UniProtKB: Q63470]
ChEMBL Inhibition of rat recombinant GST-fused DYRK1A expressed in Escherichia coli assessed as assessed as incorporation of [gamma-33P]-ATP into myelin basic protein after 30 mins by scintillation counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2010) 20: 4940-4944 [PMID:20621478]
CDC like kinase 1/Dual specificty protein kinase CLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759]
ChEMBL Inhibition of CLK1 B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2010) 20: 4940-4944 [PMID:20621478]
Glycogen synthase kinase 3 in Plasmodium falciparum 3D7 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1781857] [UniProtKB: O77344]
ChEMBL Inhibition of Plasmodium falciparum GSK3 B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2010) 20: 4940-4944 [PMID:20621478]
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 GSK3-beta B 6.64 pIC50 230 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
ChEMBL Inhibition of GSK3beta (unknown origin) B 6.7 pIC50 200 nM IC50 J Med Chem (2017) 60: 8482-8514 [PMID:29016121]
ChEMBL Inhibition of Glycogen synthase kinase-3 beta purified from insect sf9 cells B 7.64 pIC50 23.01 nM IC50 J Med Chem (2004) 47: 22-36 [PMID:14695817]
ChEMBL Inhibition of GSK3-beta B 7.64 pIC50 23 nM IC50 Trends Pharmacol Sci (2004) 25: 471-480 [PMID:15559249]
ChEMBL Inhibition of GSK3beta (unknown origin) expressed in sf9 cells after 30 mins by scintillation counting analysis in presence of [gamma-32P]ATP B 7.64 pIC50 23 nM IC50 Bioorg Med Chem Lett (2014) 24: 1532-1537 [PMID:24560539]
ChEMBL Inhibition of GSK3beta (unknown origin) B 7.64 pIC50 23 nM IC50 Eur J Med Chem (2021) 210: 112949-112949 [PMID:33097303]
ChEMBL Inhibition of human glycogen synthase kinase-3 beta B 7.64 pIC50 23 nM IC50 Bioorg Med Chem Lett (2004) 14: 413-416 [PMID:14698171]
ChEMBL Inhibition of GSK3-beta expressed in insect Sf9 cells B 7.64 pIC50 23 nM IC50 Eur J Med Chem (2010) 45: 335-342 [PMID:19906467]
GtoPdb - - 7.64 pIC50 23 nM IC50 J Biol Chem (2001) 276: 251-60 [PMID:11013232]
Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213]
ChEMBL Inhibition of INSR assessed as [33Pi] incorporation by microplate scintillation counting in presence of 0.1 uM ATP B 4 pIC50 >100000 nM IC50 J Med Chem (2010) 53: 2433-2442 [PMID:20170163]
mitogen-activated protein kinase 3/MAP kinase ERK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361]
ChEMBL Inhibition of ERK1 B 4.7 pIC50 20000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
mitogen-activated protein kinase 1/MAP kinase ERK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
ChEMBL Inhibition of ERK2 B 5.05 pIC50 9000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
sirtuin 2/NAD-dependent deacetylase sirtuin 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4462] [GtoPdb: 2708] [UniProtKB: Q8IXJ6]
ChEMBL Inhibition of human recombinant SIRT2 B 4 pIC50 >100000 nM IC50 J Med Chem (2006) 49: 7307-7316 [PMID:17149860]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 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 Dd2 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 D10 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 5 pIC50 10000 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 5 pIC50 10000 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5.1 pIC50 7943.28 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antimicrobial activity against Plasmodium falciparum F 5.4 pIC50 4000 nM IC50 Bioorg Med Chem (2010) 18: 2225-2231 [PMID:20185316]
ChEMBL Inhibitory activity against Plasmodium falciparum W2 F 5.42 pIC50 3800 nM IC50 J Med Chem (2003) 46: 3877-3882 [PMID:12930149]
ChEMBL Inhibitory activity against Plasmodium falciparum D6 F 5.42 pIC50 3800 nM IC50 J Med Chem (2003) 46: 3877-3882 [PMID:12930149]
Protein kinase Pfmrk in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4090] [UniProtKB: P90584]
ChEMBL Inhibitory activity against Plasmodium falciparum cyclin dependent protein kinase, Pfmrk B 4.82 pIC50 15000 nM IC50 J Med Chem (2003) 46: 3877-3882 [PMID:12930149]
ChEMBL Inhibition of Plasmodium falciparum cyclin-dependent kinase B 4.82 pIC50 15000 nM IC50 J Med Chem (2004) 47: 5418-5426 [PMID:15481979]
polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350]
ChEMBL Inhibition of PLK1 assessed as [33Pi] incorporation by microplate scintillation counting in presence of 0.1 uM ATP B 4 pIC50 >100000 nM IC50 J Med Chem (2010) 53: 2433-2442 [PMID:20170163]
LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
ChEMBL Inhibition of Lck B 6.33 pIC50 470 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
ChEMBL Inhibition of c-Src B 4.82 pIC50 15000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
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 VEGFR2 assessed as [33Pi] incorporation by microplate scintillation counting in presence of 0.1 uM ATP B 4 pIC50 >100000 nM IC50 J Med Chem (2010) 53: 2433-2442 [PMID:20170163]

ChEMBL data shown on this page come from version 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]