WYE-354 [Ligand Id: 9361] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL561708 (WYE-354)
  • casein kinase 1 gamma 1/Casein kinase I gamma 1 in Human [ChEMBL: CHEMBL2426] [GtoPdb: 1999] [UniProtKB: Q9HCP0]
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  • cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
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  • MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
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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]
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  • MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137]
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  • mitogen-activated protein kinase 1/MAP kinase ERK2 in Human [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
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  • mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
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  • mitogen-activated protein kinase kinase kinase kinase 2/Mitogen-activated protein kinase kinase kinase kinase 2 in Human [ChEMBL: CHEMBL5330] [GtoPdb: 2086] [UniProtKB: Q12851]
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha subunit in Human [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336]
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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]
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  • platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234]
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  • protein kinase C alpha/Protein kinase C alpha in Human [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252]
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  • protein kinase C beta/Protein kinase C beta in Human [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771]
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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]
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  • ribosomal protein S6 kinase A1/Ribosomal protein S6 kinase alpha 1 in Human [ChEMBL: CHEMBL2553] [GtoPdb: 1527] [UniProtKB: Q15418]
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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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  • aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
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  • checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757]
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  • mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345]
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  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
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  • FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
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  • HCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase HCK in Human [ChEMBL: CHEMBL3234] [GtoPdb: 2032] [UniProtKB: P08631]
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  • LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948]
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  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
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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
casein kinase 1 gamma 1/Casein kinase I gamma 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2426] [GtoPdb: 1999] [UniProtKB: Q9HCP0]
ChEMBL Inhibition of CK1gamma1 after 1 hr by mobility shift electrophoresis assay B 4.3 pIC50 >50000 nM IC50 J Med Chem (2009) 52: 5013-5016 [PMID:19645448]
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 CDK1/cyclinB after 1 hr by mobility shift electrophoresis assay B 4.3 pIC50 >50000 nM IC50 J Med Chem (2009) 52: 5013-5016 [PMID:19645448]
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
ChEMBL Inhibition of CDK2/cyclinA after 1 hr by mobility shift electrophoresis assay B 4.3 pIC50 >50000 nM IC50 J Med Chem (2009) 52: 5013-5016 [PMID:19645448]
MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
ChEMBL Inhibition of MET after 1 hr by mobility shift electrophoresis assay B 4.3 pIC50 >50000 nM IC50 J Med Chem (2009) 52: 5013-5016 [PMID:19645448]
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 IKKalpha after 1 hr by mobility shift electrophoresis assay B 4.3 pIC50 >50000 nM IC50 J Med Chem (2009) 52: 5013-5016 [PMID:19645448]
MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137]
ChEMBL Inhibition of MK2 after 1 hr by mobility shift electrophoresis assay B 4.3 pIC50 >50000 nM IC50 J Med Chem (2009) 52: 5013-5016 [PMID:19645448]
mitogen-activated protein kinase 1/MAP kinase ERK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
ChEMBL Inhibition of ERK2 after 1 hr by mobility shift electrophoresis assay B 4.3 pIC50 >50000 nM IC50 J Med Chem (2009) 52: 5013-5016 [PMID:19645448]
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
ChEMBL Inhibition of p38alpha after 1 hr by mobility shift electrophoresis assay B 4.3 pIC50 >50000 nM IC50 J Med Chem (2009) 52: 5013-5016 [PMID:19645448]
mitogen-activated protein kinase kinase kinase kinase 2/Mitogen-activated protein kinase kinase kinase kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5330] [GtoPdb: 2086] [UniProtKB: Q12851]
ChEMBL Inhibition of GCK after 1 hr by mobility shift electrophoresis assay B 4.3 pIC50 >50000 nM IC50 J Med Chem (2009) 52: 5013-5016 [PMID:19645448]
mechanistic target of rapamycin kinase/mTORC1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4296661] [GtoPdb: 2109] [UniProtKB: P42345Q8N122Q9BVC4]
GtoPdb DELFIA assay measuring His6-S6K1 T389 phosphorylation. - 8.3 pIC50 5 nM IC50 Cancer Res (2009) 69: 6232-40 [PMID:19584280]
ChEMBL Inhibition of mTORC1 (unknown origin) B 8.3 pIC50 5 nM IC50 J Med Chem (2018) 61: 4656-4687 [PMID:29211480]
mechanistic target of rapamycin kinase/mTORC2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4523999] [GtoPdb: 2109] [UniProtKB: P42345Q6R327Q9BPZ7Q9BVC4]
GtoPdb DELFIA assay measuring His6-S6K1 T389 phosphorylation. - 8.3 pIC50 5 nM IC50 Cancer Res (2009) 69: 6232-40 [PMID:19584280]
ChEMBL Inhibition of mTORC2 (unknown origin) B 8.3 pIC50 5 nM IC50 J Med Chem (2018) 61: 4656-4687 [PMID:29211480]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336]
ChEMBL Inhibition of PI3Kalpha expressed in Escherichia coli by microtiter plate-based fluorescence polarization assay B 5.99 pIC50 1026 nM IC50 J Med Chem (2009) 52: 5013-5016 [PMID:19645448]
ChEMBL Inhibition of p100alpha B 5.99 pIC50 1026 nM IC50 Bioorg Med Chem Lett (2010) 20: 4308-4312 [PMID:20561789]
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 5.2 pIC50 6315 nM IC50 J Med Chem (2009) 52: 5013-5016 [PMID:19645448]
platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234]
ChEMBL Inhibition of PDGFRalpha after 1 hr by mobility shift electrophoresis assay B 4.3 pIC50 >50000 nM IC50 J Med Chem (2009) 52: 5013-5016 [PMID:19645448]
protein kinase C alpha/Protein kinase C alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252]
ChEMBL Inhibition of PKCalpha after 1 hr by mobility shift electrophoresis assay B 4.3 pIC50 >50000 nM IC50 J Med Chem (2009) 52: 5013-5016 [PMID:19645448]
protein kinase C beta/Protein kinase C beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771]
ChEMBL Inhibition of PKCbeta after 1 hr by mobility shift electrophoresis assay B 4.3 pIC50 >50000 nM IC50 J Med Chem (2009) 52: 5013-5016 [PMID:19645448]
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 after 1 hr by mobility shift electrophoresis assay B 4.3 pIC50 >50000 nM IC50 J Med Chem (2009) 52: 5013-5016 [PMID:19645448]
ribosomal protein S6 kinase A1/Ribosomal protein S6 kinase alpha 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2553] [GtoPdb: 1527] [UniProtKB: Q15418]
ChEMBL Inhibition of RSK1 after 1 hr by mobility shift electrophoresis assay B 4.3 pIC50 >50000 nM IC50 J Med Chem (2009) 52: 5013-5016 [PMID:19645448]
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 PKBalpha after 1 hr by mobility shift electrophoresis assay B 4.3 pIC50 >50000 nM IC50 J Med Chem (2009) 52: 5013-5016 [PMID:19645448]
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 after 1 hr by mobility shift electrophoresis assay B 4.3 pIC50 >50000 nM IC50 J Med Chem (2009) 52: 5013-5016 [PMID:19645448]
checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757]
ChEMBL Inhibition of CHK1 after 1 hr by mobility shift electrophoresis assay B 4.3 pIC50 >50000 nM IC50 J Med Chem (2009) 52: 5013-5016 [PMID:19645448]
mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345]
GtoPdb DELFIA assay measuring His6-S6K1 T389 phosphorylation. - 8.3 pIC50 5 nM IC50 Cancer Res (2009) 69: 6232-40 [PMID:19584280]
ChEMBL Inhibition of recombinant mTOR assessed as inhibition of S6K T389 phosphorylation by DELFIA assay B 8.3 pIC50 5 nM IC50 Bioorg Med Chem Lett (2010) 20: 4308-4312 [PMID:20561789]
ChEMBL Inhibition of flag-tagged truncated human mTOR (1360-2549) expressed in HEK293 cells by DELFIA assay B 8.37 pIC50 4.3 nM IC50 J Med Chem (2009) 52: 5013-5016 [PMID:19645448]
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
ChEMBL Inhibition of ABL1 after 1 hr by mobility shift electrophoresis assay B 4.3 pIC50 >50000 nM IC50 J Med Chem (2009) 52: 5013-5016 [PMID:19645448]
FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
ChEMBL Inhibition of FYN after 1 hr by mobility shift electrophoresis assay B 4.3 pIC50 >50000 nM IC50 J Med Chem (2009) 52: 5013-5016 [PMID:19645448]
HCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase HCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3234] [GtoPdb: 2032] [UniProtKB: P08631]
ChEMBL Inhibition of HCK after 1 hr by mobility shift electrophoresis assay B 4.3 pIC50 >50000 nM IC50 J Med Chem (2009) 52: 5013-5016 [PMID:19645448]
LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948]
ChEMBL Inhibition of LYN after 1 hr by mobility shift electrophoresis assay B 4.3 pIC50 >50000 nM IC50 J Med Chem (2009) 52: 5013-5016 [PMID:19645448]
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
ChEMBL Inhibition of SRC after 1 hr by mobility shift electrophoresis assay B 4.3 pIC50 >50000 nM IC50 J Med Chem (2009) 52: 5013-5016 [PMID:19645448]
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 after 1 hr by mobility shift electrophoresis assay B 4.3 pIC50 >50000 nM IC50 J Med Chem (2009) 52: 5013-5016 [PMID:19645448]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]