kenpaullone [Ligand Id: 6000] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL296586 (Kenpaullone) |
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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 33:
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]
