GSK2334470 [Ligand Id: 8008] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1765740 (GSK2334470)
  • 3-phosphoinositide dependent protein kinase 1/3-phosphoinositide dependent protein kinase-1 in Human [ChEMBL: CHEMBL2534] [GtoPdb: 1519] [UniProtKB: O15530]
  • This target only has 0 pki data point
  • 0
1 CHEMBL1765740_lig_chart_1 3-phosphoinositide dependent protein kinase-1 Human
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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
  • This target only has 0 pki data point
  • 0
2 CHEMBL1765740_lig_chart_2 Epidermal growth factor receptor erbB1 Human
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  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
  • This target only has 0 pki data point
  • 0
3 CHEMBL1765740_lig_chart_3 Glycogen synthase kinase-3 beta Human
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  • component of inhibitor of nuclear factor kappa B kinase complex/Inhibitor of nuclear factor kappa B kinase alpha subunit in Human [ChEMBL: CHEMBL3476] [GtoPdb: 1989] [UniProtKB: O15111]
  • This target only has 0 pki data point
  • 0
4 CHEMBL1765740_lig_chart_4 Inhibitor of nuclear factor kappa B kinase alpha subunit Human
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  • mitogen-activated protein kinase kinase kinase 5/Mitogen-activated protein kinase kinase kinase 5 in Human [ChEMBL: CHEMBL5285] [GtoPdb: 2080] [UniProtKB: Q99683]
  • This target only has 0 pki data point
  • 0
5 CHEMBL1765740_lig_chart_5 Mitogen-activated protein kinase kinase kinase 5 Human
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/PI3-kinase p110-gamma subunit in Human [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736]
  • This target only has 0 pki data point
  • 0
6 CHEMBL1765740_lig_chart_6 PI3-kinase p110-gamma subunit Human
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  • Rho associated coiled-coil containing protein kinase 1/Rho-associated protein kinase 1 in Human [ChEMBL: CHEMBL3231] [GtoPdb: 1503] [UniProtKB: Q13464]
  • This target only has 0 pki data point
  • 0
7 CHEMBL1765740_lig_chart_7 Rho-associated protein kinase 1 Human
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  • AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
  • This target only has 0 pki data point
  • 0
8 CHEMBL1765740_lig_chart_8 Serine/threonine-protein kinase AKT Human
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  • aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
  • This target only has 0 pki data point
  • 0
9 CHEMBL1765740_lig_chart_9 Serine/threonine-protein kinase Aurora-A Human
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  • aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
  • This target only has 0 pki data point
  • 0
10 CHEMBL1765740_lig_chart_10 Serine/threonine-protein kinase Aurora-B Human
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  • transforming growth factor beta receptor 1/TGF-beta receptor type I in Human [ChEMBL: CHEMBL4439] [GtoPdb: 1788] [UniProtKB: P36897]
  • This target only has 0 pki data point
  • 0
11 CHEMBL1765740_lig_chart_11 TGF-beta receptor type I Human
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  • spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405]
  • This target only has 0 pki data point
  • 0
12 CHEMBL1765740_lig_chart_12 Tyrosine-protein kinase SYK Human
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  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
  • This target only has 0 pki data point
  • 0
13 CHEMBL1765740_lig_chart_13 Vascular endothelial growth factor receptor 2 Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
3-phosphoinositide dependent protein kinase 1/3-phosphoinositide dependent protein kinase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2534] [GtoPdb: 1519] [UniProtKB: O15530]
ChEMBL Inhibition of PDK1-mediated RSK phosphorylation at Ser221 residue in human PC3 cells by ELISA B 6.53 pIC50 293 nM IC50 J. Med. Chem. (2011) 54: 1871-1895 [PMID:21341675]
ChEMBL Inhibition of PDK1-mediated AKT phosphorylation at Thr308 residue in human PC3 cells by ELISA B 6.95 pIC50 113 nM IC50 J. Med. Chem. (2011) 54: 1871-1895 [PMID:21341675]
ChEMBL Inhibition of recombinant full length PDK1 (unknown origin) expressed in insect cells assessed as inhibition of Akt activation measured for 30 mins in presence of [gamma32P-ATP] B 8 pIC50 10 nM IC50 J. Med. Chem. (2013) 56: 2726-2737 [PMID:23448267]
ChEMBL Inhibition of recombinant human His-tagged PDK1 catalytic domain using Ac-Sox-PKTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIAD-NH2 as substrate by fluorescence-based spectrophotometry B 8 pIC50 10 nM IC50 J. Med. Chem. (2011) 54: 8490-8500 [PMID:22040023]
ChEMBL Inhibition of PDK1 B 8.6 pIC50 2.51 nM IC50 J. Med. Chem. (2011) 54: 1871-1895 [PMID:21341675]
GtoPdb - - 8.6 pIC50 2.51 nM IC50 J Med Chem (2011) 54: 1871-95 [PMID:21341675]
ChEMBL Inhibition of PDK1 B 8.6 pIC50 2.5 nM IC50 J. Med. Chem. (2011) 54: 1871-1895 [PMID:21341675]
ChEMBL Inhibition of PDK1 (unknown origin) B 8.6 pIC50 2.5 nM IC50 Eur. J. Med. Chem. (2016) 118: 47-63 [PMID:27123901]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibition of EGFR B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2011) 54: 1871-1895 [PMID:21341675]
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 GSK3B B 4.6 pIC50 >25118 nM IC50 J. Med. Chem. (2011) 54: 1871-1895 [PMID:21341675]
component of inhibitor of nuclear factor kappa B kinase complex/Inhibitor of nuclear factor kappa B kinase alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3476] [GtoPdb: 1989] [UniProtKB: O15111]
ChEMBL Inhibition of IKK1 B 4.6 pIC50 >25118 nM IC50 J. Med. Chem. (2011) 54: 1871-1895 [PMID:21341675]
mitogen-activated protein kinase kinase kinase 5/Mitogen-activated protein kinase kinase kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5285] [GtoPdb: 2080] [UniProtKB: Q99683]
ChEMBL Inhibition of ASK1 B 4.56 pIC50 >27542 nM IC50 J. Med. Chem. (2011) 54: 1871-1895 [PMID:21341675]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/PI3-kinase p110-gamma subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736]
ChEMBL Inhibition of PI3Kgamma B 4.6 pIC50 25118 nM IC50 J. Med. Chem. (2011) 54: 1871-1895 [PMID:21341675]
Rho associated coiled-coil containing protein kinase 1/Rho-associated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3231] [GtoPdb: 1503] [UniProtKB: Q13464]
ChEMBL Inhibition of ROCK1 B 5.1 pIC50 7943.28 nM IC50 J. Med. Chem. (2011) 54: 1871-1895 [PMID:21341675]
ChEMBL Inhibition of ROCK1 B 5.1 pIC50 7943 nM IC50 J. Med. Chem. (2011) 54: 1871-1895 [PMID:21341675]
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 AKT1 B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2011) 54: 1871-1895 [PMID:21341675]
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 B 4.4 pIC50 39810 nM IC50 J. Med. Chem. (2011) 54: 1871-1895 [PMID:21341675]
GtoPdb - - 5 pIC50 >10000 nM IC50 J Med Chem (2011) 54: 1871-95 [PMID:21341675]
ChEMBL Inhibition of aurora A B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2011) 54: 1871-1895 [PMID:21341675]
aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
ChEMBL Inhibition of aurora B B 5.5 pIC50 3162.28 nM IC50 J. Med. Chem. (2011) 54: 1871-1895 [PMID:21341675]
GtoPdb - - 5.5 pIC50 3160 nM IC50 J Med Chem (2011) 54: 1871-95 [PMID:21341675]
ChEMBL Inhibition of aurora B B 5.5 pIC50 3162 nM IC50 J. Med. Chem. (2011) 54: 1871-1895 [PMID:21341675]
transforming growth factor beta receptor 1/TGF-beta receptor type I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4439] [GtoPdb: 1788] [UniProtKB: P36897]
ChEMBL Inhibition of ALK5 B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2011) 54: 1871-1895 [PMID:21341675]
ChEMBL Inhibition of ALK5 B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2011) 54: 1871-1895 [PMID:21341675]
spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405]
ChEMBL Inhibition of SYK B 4.6 pIC50 >25118 nM IC50 J. Med. Chem. (2011) 54: 1871-1895 [PMID:21341675]
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 VEGFR2 B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2011) 54: 1871-1895 [PMID:21341675]

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, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]