GSK-3beta inhibitor VIII [Ligand Id: 5979] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL259850 (AR-A014418)
  • cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
  • This target only has 0 pki data point
  • 0
1 CHEMBL259850_lig_chart_1 Cyclin-dependent kinase 2 Human
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  • cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535]
  • This target only has 0 pki data point
  • 0
2 CHEMBL259850_lig_chart_2 Cyclin-dependent kinase 5 Human
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  • Cyclin-dependent kinase 5 regulatory subunit 1 in Human [ChEMBL: CHEMBL2783] [UniProtKB: Q15078]
  • This target only has 0 pki data point
  • 0
3 CHEMBL259850_lig_chart_3 Cyclin-dependent kinase 5 regulatory subunit 1 Human
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  • autophagy related 4B cysteine peptidase/Cysteine protease ATG4B in Human [ChEMBL: CHEMBL1741221] [GtoPdb: 2329] [UniProtKB: Q9Y4P1]
  • This target only has 0 pki data point
  • 0
4 CHEMBL259850_lig_chart_4 Cysteine protease ATG4B Human
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  • glycogen synthase kinase 3 alpha/Glycogen synthase kinase-3 alpha in Human [ChEMBL: CHEMBL2850] [GtoPdb: 2029] [UniProtKB: P49840]
  • This target only has 0 pki data point
  • 0
5 CHEMBL259850_lig_chart_5 Glycogen synthase kinase-3 alpha Human
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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 Mouse [ChEMBL: CHEMBL1075321] [GtoPdb: 2030] [UniProtKB: Q9WV60]
  • 0
6 CHEMBL259850_lig_chart_6 Glycogen synthase kinase-3 beta HumanMouse
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
ChEMBL Inhibition of Cdk2 B 4 pIC50 >100000 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
ChEMBL Inhibition of CDK2 at 10 mM B 4 pIC50 100000 nM IC50 Trends Pharmacol. Sci. (2004) 25: 471-480 [PMID:15559249]
cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535]
ChEMBL Inhibition of CDK5 at 10 mM B 4 pIC50 100000 nM IC50 Trends Pharmacol. Sci. (2004) 25: 471-480 [PMID:15559249]
Cyclin-dependent kinase 5 regulatory subunit 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2783] [UniProtKB: Q15078]
ChEMBL Inhibition of Cdk5 B 4 pIC50 >100000 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
autophagy related 4B cysteine peptidase/Cysteine protease ATG4B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1741221] [GtoPdb: 2329] [UniProtKB: Q9Y4P1]
ChEMBL Inhibition of ATG4B (unknown origin) incubated up to 1 hr in presence of fluorescent protein substrate by FRET-based-LC3 cleavage assay B 5.8 pIC50 1600 nM IC50 WO-2017027984-A1. Compounds and methods for treatment of cancer by inhibiting atg4b and blocking autophagy (null)
glycogen synthase kinase 3 alpha/Glycogen synthase kinase-3 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2850] [GtoPdb: 2029] [UniProtKB: P49840]
ChEMBL Inhibition of human GSK3alpha activity using Ser/Thr 11 peptide as substrate by FRET assay B 4.15 pIC50 70000 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 5610-5615 [PMID:21807510]
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 GSK-3beta using phospho-glycogen synthase peptide-2 as substrate after 10 mins by liquid scintillation counting B 6.11 pKi 770 nM Ki Bioorg. Med. Chem. Lett. (2012) 22: 2099-2101 [PMID:22321216]
GtoPdb - - 7.42 pKi 38 nM Ki J Biol Chem (2003) 278: 45937-45 [PMID:12928438]
ChEMBL Inhibition of GSK3-beta B 7.42 pKi 38 nM Ki Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
ChEMBL Inhibition of human GSK-3beta using biotin-AAEELDSRAGS(PO3H2)PQL as substrate after 20 mins by liquid scintillation counting B 7.42 pKi 38 nM Ki Bioorg. Med. Chem. Lett. (2012) 22: 2099-2101 [PMID:22321216]
ChEMBL Inhibition of human GSK-3beta using YRRAAVPPSPSLSRHSSPHQS(p) EDEEE substrate peptide and [gamma-33P-ATP] incubated for 40 mins by scintillation counting method B 6.66 pIC50 220 nM IC50 Bioorg Med Chem Lett (2018) 28: 160-166 [PMID:29208522]
ChEMBL Inhibition of GSK3-beta B 6.98 pIC50 104 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
ChEMBL Inhibition of GSK3-beta B 6.98 pIC50 104 nM IC50 Trends Pharmacol. Sci. (2004) 25: 471-480 [PMID:15559249]
ChEMBL Inhibition of human recombinant GSK3beta B 6.98 pIC50 104 nM IC50 J. Med. Chem. (2011) 54: 8461-8470 [PMID:22050263]
ChEMBL Inhibition of GSK3beta B 6.98 pIC50 104 nM IC50 J. Med. Chem. (2012) 55: 9107-9119 [PMID:22489897]
ChEMBL Inhibition of recombinant human GSK3beta using biotin-AAEELDSRAGS(PO3H2)PQL as substrate preincubated for 10 to 15 mins followed by [gamma33P]ATP addition after 20 mins by scintillation proximity assay B 7 pIC50 100 nM IC50 Eur J Med Chem (2017) 125: 464-477 [PMID:27689729]
ChEMBL Inhibition of human GSK3-beta B 7 pIC50 100 nM IC50 Eur. J. Med. Chem. (2009) 44: 2361-2371 [PMID:18929433]
ChEMBL Inhibition of recombinant human GSK3beta using prephosphorylated peptide as substrate measured after 30 mins by Kinase-glo luminescence assay B 7.14 pIC50 72 nM IC50 Bioorg Med Chem Lett (2019) 29: 1597-1600 [PMID:31054862]
ChEMBL Inhibition of human GSK3-beta by scintillation counting B 7.38 pIC50 41.8 nM IC50 J. Med. Chem. (2009) 52: 1853-1863 [PMID:19338355]
ChEMBL Inhibition of recombinant full length human His-tagged GSK3beta expressed in baculovirus expression system using ser/thr-9 peptide as substrate measured after 1 hr by Z'-Lyte assay B 8.68 pIC50 2.07 nM IC50 MedChemComm (2018) 9: 1472-1490
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075321] [GtoPdb: 2030] [UniProtKB: Q9WV60]
ChEMBL Inhibition of human GSK-3beta in mouse 3T3 fibroblasts stably expressing four-repeat tau protein assessed as reduction in tau S396 phosphorylation after 4 hrs post dose by Western blot B 7 pIC50 100 nM IC50 Bioorg Med Chem Lett (2018) 28: 160-166 [PMID:29208522]

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]