GSK-3 inhibitor XIII [Ligand Id: 5976] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL359482
  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
1 CHEMBL359482_lig_chart_1 Glycogen synthase kinase-3 beta Human
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  • eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525]
  • This target only has 0 pki data point
2 CHEMBL359482_lig_chart_2 Interferon-induced, double-stranded RNA-activated protein kinase Human
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  • aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
3 CHEMBL359482_lig_chart_3 Serine/threonine-protein kinase Aurora-A Human
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  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
4 CHEMBL359482_lig_chart_4 Tyrosine-protein kinase SRC Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 Gsk3beta B 7.66 pKi 22 nM Ki J. Med. Chem. (2009) 52: 2629-2651 [PMID:19320489]
ChEMBL Inhibition of GSK3-beta B 7.66 pKi 22 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 3586-3592 [PMID:19447622]
GtoPdb - - 7.66 pKi 22 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 3586-92 [PMID:19447622]
eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525]
ChEMBL Inhibition of human recombinant PKR autophosphorylation using poly[I:C] after 10 mins by luminescent assay B 4.82 pIC50 15000 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 4108-4114 [PMID:21632247]
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
ChEMBL Inhibition of aurora A kinase B 7.24 pKi 58 nM Ki J. Med. Chem. (2009) 52: 2629-2651 [PMID:19320489]
ChEMBL Inhibition of Aurora-A by coupled assay B 7.24 pKi 58 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 3586-3592 [PMID:19447622]
GtoPdb - - 7.24 pKi 58 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 3586-92 [PMID:19447622]
ChEMBL Inhibition of Aurora A (unknown origin) using FAM-labelled peptide as substrate pretreated for 10 mins followed by substrate addition and measured after 60 mins by fluorescence assay B 7.55 pIC50 28 nM IC50 Eur J Med Chem (2018) 157: 1361-1375 [PMID:30196060]
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
GtoPdb - - 7.09 pKi 81 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 3586-92 [PMID:19447622]
ChEMBL Inhibition of Src B 7.09 pKi 81 nM Ki J. Med. Chem. (2009) 52: 2629-2651 [PMID:19320489]
ChEMBL Inhibition of Src B 7.09 pKi 81 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 3586-3592 [PMID:19447622]

ChEMBL data shown on this page come from version 27:

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]