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]
ChEMBL Inhibition of CDK1/Cyclin B (unknown origin) in presence of gamma32P-ATP by scintillation counter analysis B 5.7 pIC50 2000 nM IC50 Eur J Med Chem (2021) 220: 113445-113445 [PMID:33901899]
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 2/Cyclin-dependent kinase 2/cyclin A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094128] [GtoPdb: 1973] [UniProtKB: P20248P24941P78396]
ChEMBL Inhibition of CDK2/Cyclin A (unknown origin) B 5.7 pIC50 2000 nM IC50 Eur J Med Chem (2021) 220: 113445-113445 [PMID:33901899]
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]
ChEMBL Inhibition of CDK5/p25 (unknown origin) B 5.38 pIC50 4200 nM IC50 Eur J Med Chem (2021) 220: 113445-113445 [PMID:33901899]
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]
ChEMBL Binding affinity to human C-terminal his tagged GSK3beta (26 to 383 residues) expressed in Escherichia coli at 50 uM by radiometric analysis B 7.46 pKd 34.9 nM Kd J Med Chem (2023) 66: 4009-4024 [PMID:36883902]
ChEMBL Inhibition of human C-terminal his tagged GSK3beta (26 to 383 residues) expressed in Escherichia coli using GYSI(YRRAAVPPSPSLSRHSSPHQ(pS)EDEEE) as peptide substrate incubated for 1 hr in presence of ATP by cook activity assay B 6.82 pIC50 150 nM IC50 J Med Chem (2023) 66: 4009-4024 [PMID:36883902]
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 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]