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: P06493, P14635]
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: P42345, Q8N122, Q9BVC4]
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: P42345, Q6R327, Q9BPZ7, Q9BVC4]
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 recombinant FLAG-tagged mTOR (unknown origin) expressed in HEK293 cells assessed as decrease in phosphorylation of S6K level at Thr389 incubated for 2 hrs in presence of ATP and His6-S6K by DELFIA assay B 8.3 pIC50 5 nM IC50 Eur J Med Chem (2020) 208: 112820-112820 [PMID:32966896]
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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]