1-azakenpaullone [Ligand Id: 8018] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL336961 (Azakenpaullone)
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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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  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Rat [ChEMBL: CHEMBL3669] [GtoPdb: 2030] [UniProtKB: P18266]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094127] [GtoPdb: 1961] [UniProtKB: O95067P06493P14635Q8WWL7]
ChEMBL Inhibition of human cyclin-dependent kinase 1-cyclin B B 5.7 pIC50 2000 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 413-416 [PMID:14698171]
ChEMBL Inhibition of CDK1/cyclinB B 5.7 pIC50 2000 nM IC50 Trends Pharmacol. Sci. (2004) 25: 471-480 [PMID:15559249]
GtoPdb CDK1/cyclin B complex in assay - 5.7 pIC50 2000 nM IC50 Bioorg Med Chem Lett (2004) 14: 413-6 [PMID:14698171]
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 GST-tagged CDK1/cyclin B (unknown origin) expressed in Escherichia coli B 5.7 pIC50 2000 nM IC50 Eur J Med Chem (2017) 142: 244-265 [PMID:28803677]
GtoPdb CDK1/cyclin B complex in assay - 5.7 pIC50 2000 nM IC50 Bioorg Med Chem Lett (2004) 14: 413-6 [PMID:14698171]
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 human Cyclin-dependent kinase 5-p35nck5a B 5.38 pIC50 4200 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 413-416 [PMID:14698171]
ChEMBL Inhibition of recombinant CDK5/p25 expressed in Escherichia coli B 5.38 pIC50 4200 nM IC50 J. Med. Chem. (2008) 51: 2196-2207 [PMID:18345612]
GtoPdb CDK5/p25 complex in assay - 5.38 pIC50 4200 nM IC50 Bioorg Med Chem Lett (2004) 14: 413-6 [PMID:14698171]
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
GtoPdb - - 7.74 pIC50 18 nM IC50 Bioorg Med Chem Lett (2004) 14: 413-6 [PMID:14698171]
ChEMBL Inhibition of human glycogen synthase kinase-3 beta B 7.74 pIC50 18 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 413-416 [PMID:14698171]
ChEMBL Inhibition of GSK3-beta B 7.74 pIC50 18 nM IC50 Trends Pharmacol. Sci. (2004) 25: 471-480 [PMID:15559249]
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3669] [GtoPdb: 2030] [UniProtKB: P18266]
ChEMBL Inhibition of rat GSK3beta expressed in Sf9 cells incubated for 30 mins using GS-1 peptide substrate and [gamma-32P]ATP by scintillation counting method B 7.74 pIC50 18 nM IC50 Eur J Med Chem (2017) 142: 244-265 [PMID:28803677]

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]