LY2090314 [Ligand Id: 7958] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL362558 (Ly 2090314, Ly-2090314, LY2090314, LY-2090314)
  • protein kinase, cAMP-dependent, catalytic, beta subunit/cAMP-dependent protein kinase beta-1 catalytic subunit in Human [ChEMBL: CHEMBL2918] [GtoPdb: 1477] [UniProtKB: P22694]
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  • cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
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  • cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802]
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  • glycogen synthase kinase 3 alpha/Glycogen synthase kinase-3 alpha in Human [ChEMBL: CHEMBL2850] [GtoPdb: 2029] [UniProtKB: P49840]
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  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
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  • ZAK sterile alpha motif and leucine zipper containing kinase AZK/Mixed lineage kinase 7 in Human [ChEMBL: CHEMBL3886] [GtoPdb: 2289] [UniProtKB: Q9NYL2]
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  • protein kinase C beta/Protein kinase C beta in Human [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771]
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  • pyruvate dehydrogenase kinase 1/Pyruvate dehydrogenase kinase isoform 1 in Human [ChEMBL: CHEMBL4766] [GtoPdb: 2915] [UniProtKB: Q15118]
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  • AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
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  • transforming growth factor beta receptor 2/TGF-beta receptor type II in Human [ChEMBL: CHEMBL4267] [GtoPdb: 1795] [UniProtKB: P37173]
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  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
protein kinase, cAMP-dependent, catalytic, beta subunit/cAMP-dependent protein kinase beta-1 catalytic subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2918] [GtoPdb: 1477] [UniProtKB: P22694]
ChEMBL Inhibition of human Protein kinase A beta B 4.7 pIC50 >20000 nM IC50 J. Med. Chem. (2004) 47: 3934-3937 [PMID:15267232]
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
ChEMBL Inhibition of human Cyclin-dependent kinase 2 B 5.55 pIC50 2800 nM IC50 J. Med. Chem. (2004) 47: 3934-3937 [PMID:15267232]
cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802]
ChEMBL Inhibition of human Cyclin-dependent kinase 4 B 5.74 pIC50 1800 nM IC50 J. Med. Chem. (2004) 47: 3934-3937 [PMID:15267232]
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 GSK3alpha (unknown origin) B 8.82 pIC50 1.5 nM IC50 Drug Metab. Dispos. (2013) 41: 714-726 [PMID:23305709]
ChEMBL Inhibition of human GSK-3alpha using YRRAAVPPSPSLSRHSSPHQ(pS)EDEEE as substrate measured in presence of [gamma-33P]ATP by radiometric assay B 8.82 pIC50 1.5 nM IC50 Eur J Med Chem (2019) 171: 221-234 [PMID:30925338]
ChEMBL Inhibition of human GSK-3alpha S449A mutant (2 to end residues) using phospho GS2 peptide as substrate after 40 mins in presence of [gamma-33ATP] by scintillation counting method B 8.99 pIC50 1.02 nM IC50 Eur J Med Chem (2019) 171: 221-234 [PMID:30925338]
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 human Glycogen synthase kinase-3 beta B 8.96 pIC50 1.1 nM IC50 J. Med. Chem. (2004) 47: 3934-3937 [PMID:15267232]
ChEMBL Inhibition of human GSK3-beta B 8.96 pIC50 1.1 nM IC50 Eur. J. Med. Chem. (2009) 44: 2361-2371 [PMID:18929433]
GtoPdb Inhibition of GSK-3β-mediated phosphoryaltion of phosph0-CREB - 8.96 pIC50 1.1 nM IC50 J Med Chem (2004) 47: 3934-7 [PMID:15267232]
ChEMBL Inhibition of GSK3beta (unknown origin) B 9.05 pIC50 0.9 nM IC50 Drug Metab. Dispos. (2013) 41: 714-726 [PMID:23305709]
ChEMBL Inhibition of Glycogen synthase kinase-3 beta dependent Tau protein serine-396 phosphorylation in human SY5Y cells F 9.15 pIC50 0.7 nM IC50 J. Med. Chem. (2004) 47: 3934-3937 [PMID:15267232]
ZAK sterile alpha motif and leucine zipper containing kinase AZK/Mixed lineage kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3886] [GtoPdb: 2289] [UniProtKB: Q9NYL2]
ChEMBL Inhibition of human MLK7 B 4.7 pIC50 >20000 nM IC50 J. Med. Chem. (2004) 47: 3934-3937 [PMID:15267232]
protein kinase C beta/Protein kinase C beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771]
ChEMBL Inhibition of human Protein kinase C beta 2 B 6.38 pIC50 420 nM IC50 J. Med. Chem. (2004) 47: 3934-3937 [PMID:15267232]
pyruvate dehydrogenase kinase 1/Pyruvate dehydrogenase kinase isoform 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4766] [GtoPdb: 2915] [UniProtKB: Q15118]
ChEMBL Inhibition of human PDK-1 B 5.21 pIC50 6200 nM IC50 J. Med. Chem. (2004) 47: 3934-3937 [PMID:15267232]
AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
ChEMBL Inhibition of human Akt1 B 4.7 pIC50 >20000 nM IC50 J. Med. Chem. (2004) 47: 3934-3937 [PMID:15267232]
transforming growth factor beta receptor 2/TGF-beta receptor type II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4267] [GtoPdb: 1795] [UniProtKB: P37173]
ChEMBL Inhibition of human TGF-beta type II receptor B 5.92 pIC50 >1200 nM IC50 J. Med. Chem. (2004) 47: 3934-3937 [PMID:15267232]
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 human Vascular endothelial growth factor receptor 2 B 4.7 pIC50 >20000 nM IC50 J. Med. Chem. (2004) 47: 3934-3937 [PMID:15267232]

ChEMBL data shown on this page come from version 31:

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]