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ChEMBL ligand: CHEMBL561708 (WYE-354) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 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]