PLX5622 [Ligand Id: 9105] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3639728 (Plx-5622, PLX-5622, PLX5622)
  • activin A receptor type 1B/Activin receptor type-1B in Human [ChEMBL: CHEMBL5310] [GtoPdb: 1787] [UniProtKB: P36896]
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  • ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
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  • protein kinase AMP-activated non-catalytic subunit gamma 1/protein kinase AMP-activated catalytic subunit alpha 1/protein kinase AMP-activated non-catalytic subunit beta 1/AMP-activated protein kinase (AMPK) alpha-1/beta-1/gamma-1 in Human [ChEMBL: CHEMBL2111345] [GtoPdb: 1545, 1541, 1543] [UniProtKB: P54619, Q13131, Q9Y478]
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  • protein kinase AMP-activated non-catalytic subunit gamma 1/protein kinase AMP-activated catalytic subunit alpha 2/protein kinase AMP-activated non-catalytic subunit beta 1/AMPK alpha2/beta1/gamma1 in Human [ChEMBL: CHEMBL3038455] [GtoPdb: 1545, 1542, 1543] [UniProtKB: P54619, P54646, Q9Y478]
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  • TEK receptor tyrosine kinase/Angiopoietin-1 receptor in Human [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763]
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  • neurotrophic receptor tyrosine kinase 2/BDNF/NT-3 growth factors receptor in Human [ChEMBL: CHEMBL4898] [GtoPdb: 1818] [UniProtKB: Q16620]
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  • beta adrenergic receptor kinase 1/Beta-adrenergic receptor kinase 1 in Human [ChEMBL: CHEMBL4079] [GtoPdb: 1466] [UniProtKB: P25098]
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  • calcium/calmodulin dependent protein kinase I/Calcium/calmodulin-dependent protein kinase type 1 in Human [ChEMBL: CHEMBL2493] [GtoPdb: 1952] [UniProtKB: Q14012]
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  • calcium/calmodulin dependent protein kinase ID/Calcium/calmodulin-dependent protein kinase type 1D in Human [ChEMBL: CHEMBL5073] [GtoPdb: 1953] [UniProtKB: Q8IU85]
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  • calcium/calmodulin-dependent protein kinase II alpha subunit/Calcium/calmodulin-dependent protein kinase type II subunit alpha in Human [ChEMBL: CHEMBL4147] [GtoPdb: 1555] [UniProtKB: Q9UQM7]
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  • calcium/calmodulin-dependent protein kinase II beta subunit/Calcium/calmodulin-dependent protein kinase type II subunit beta in Human [ChEMBL: CHEMBL4121] [GtoPdb: 1556] [UniProtKB: Q13554]
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  • calcium/calmodulin-dependent protein kinase II delta subunit/Calcium/calmodulin-dependent protein kinase type II subunit delta in Human [ChEMBL: CHEMBL2801] [GtoPdb: 1558] [UniProtKB: Q13557]
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  • calcium/calmodulin dependent protein kinase IV/Calcium/calmodulin-dependent protein kinase type IV in Human [ChEMBL: CHEMBL2494] [GtoPdb: 1955] [UniProtKB: Q16566]
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  • protein kinase, cAMP-dependent, catalytic, alpha subunit/cAMP-dependent protein kinase catalytic subunit alpha in Human [ChEMBL: CHEMBL4101] [GtoPdb: 1476] [UniProtKB: P17612]
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  • protein kinase X-linked/cAMP-dependent protein kinase catalytic subunit PRKX in Human [ChEMBL: CHEMBL5818] [GtoPdb: 2175] [UniProtKB: P51817]
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  • casein kinase 1 alpha 1/Casein kinase I isoform alpha in Human [ChEMBL: CHEMBL2793] [GtoPdb: 1995] [UniProtKB: P48729]
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  • casein kinase 1 delta/Casein kinase I isoform delta in Human [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730]
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  • casein kinase 1 epsilon/Casein kinase I isoform epsilon in Human [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674]
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  • casein kinase 1 gamma 1/Casein kinase I isoform gamma-1 in Human [ChEMBL: CHEMBL2426] [GtoPdb: 1999] [UniProtKB: Q9HCP0]
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  • casein kinase 1 gamma 2/Casein kinase I isoform gamma-2 in Human [ChEMBL: CHEMBL2543] [GtoPdb: 2000] [UniProtKB: P78368]
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  • casein kinase 1 gamma 3/Casein kinase I isoform gamma-3 in Human [ChEMBL: CHEMBL5084] [GtoPdb: 2001] [UniProtKB: Q9Y6M4]
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  • casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II subunit alpha in Human [ChEMBL: CHEMBL3629] [GtoPdb: 1549] [UniProtKB: P68400]
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  • casein kinase 2, alpha prime polypeptide subunit/Casein kinase II subunit alpha` in Human [ChEMBL: CHEMBL4070] [GtoPdb: 1550] [UniProtKB: P19784]
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  • Protein kinase G (PKG) 1/cGMP-dependent protein kinase 1 in Human [ChEMBL: CHEMBL4273] [GtoPdb: 1492] [UniProtKB: Q13976]
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  • Protein kinase G (PKG) 2/cGMP-dependent protein kinase 2 in Human [ChEMBL: CHEMBL2896] [GtoPdb: 1493] [UniProtKB: Q13237]
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  • cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078]
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  • BMX non-receptor tyrosine kinase/Cytoplasmic tyrosine-protein kinase BMX in Human [ChEMBL: CHEMBL3834] [GtoPdb: 1942] [UniProtKB: P51813]
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  • death associated protein kinase 1/Death-associated protein kinase 1 in Human [ChEMBL: CHEMBL2558] [GtoPdb: 2002] [UniProtKB: P53355]
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  • death associated protein kinase 3/Death-associated protein kinase 3 in Human [ChEMBL: CHEMBL2468] [GtoPdb: 2004] [UniProtKB: O43293]
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  • CDC like kinase 2/Dual specificity protein kinase CLK2 in Human [ChEMBL: CHEMBL4225] [GtoPdb: 1991] [UniProtKB: P49760]
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  • dual specificity tyrosine phosphorylation regulated kinase 1A/Dual specificity tyrosine-phosphorylation-regulated kinase 1A in Human [ChEMBL: CHEMBL2292] [GtoPdb: 2009] [UniProtKB: Q13627]
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  • dual specificity tyrosine phosphorylation regulated kinase 1B/Dual specificity tyrosine-phosphorylation-regulated kinase 1B in Human [ChEMBL: CHEMBL5543] [GtoPdb: 2010] [UniProtKB: Q9Y463]
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  • dual specificity tyrosine phosphorylation regulated kinase 3/Dual specificity tyrosine-phosphorylation-regulated kinase 3 in Human [ChEMBL: CHEMBL4575] [GtoPdb: 2012] [UniProtKB: O43781]
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  • dual specificity tyrosine phosphorylation regulated kinase 4/Dual specificity tyrosine-phosphorylation-regulated kinase 4 in Human [ChEMBL: CHEMBL1075115] [GtoPdb: 2013] [UniProtKB: Q9NR20]
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  • EPH receptor A1/Ephrin type-A receptor 1 in Human [ChEMBL: CHEMBL5810] [GtoPdb: 1821] [UniProtKB: P21709]
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  • EPH receptor A2/Ephrin type-A receptor 2 in Human [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317]
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  • EPH receptor A3/Ephrin type-A receptor 3 in Human [ChEMBL: CHEMBL4954] [GtoPdb: 1823] [UniProtKB: P29320]
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  • EPH receptor A5/Ephrin type-A receptor 5 in Human [ChEMBL: CHEMBL3987] [GtoPdb: 1825] [UniProtKB: P54756]
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  • EPH receptor A8/Ephrin type-A receptor 8 in Human [ChEMBL: CHEMBL4134] [GtoPdb: 1828] [UniProtKB: P29322]
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  • EPH receptor B1/Ephrin type-B receptor 1 in Human [ChEMBL: CHEMBL5072] [GtoPdb: 1830] [UniProtKB: P54762]
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  • EPH receptor B2/Ephrin type-B receptor 2 in Human [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323]
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  • EPH receptor B3/Ephrin type-B receptor 3 in Human [ChEMBL: CHEMBL4901] [GtoPdb: 1832] [UniProtKB: P54753]
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  • EPH receptor B4/Ephrin type-B receptor 4 in Human [ChEMBL: CHEMBL5147] [GtoPdb: 1833] [UniProtKB: P54760]
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  • epidermal growth factor receptor/Epidermal growth factor receptor in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • eukaryotic elongation factor 2 kinase/Eukaryotic elongation factor 2 kinase in Human [ChEMBL: CHEMBL5026] [GtoPdb: 2014] [UniProtKB: O00418]
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  • fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
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  • fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802]
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  • fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607]
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  • fibroblast growth factor receptor 4/Fibroblast growth factor receptor 4 in Human [ChEMBL: CHEMBL3973] [GtoPdb: 1811] [UniProtKB: P22455]
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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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  • beta adrenergic receptor kinase 2/G protein-coupled receptor kinase 3 in Human [ChEMBL: CHEMBL1075166] [GtoPdb: 1467] [UniProtKB: P35626]
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  • G protein-coupled receptor kinase 4 in Human [ChEMBL: CHEMBL5861] [GtoPdb: 1468] [UniProtKB: P32298]
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  • G protein-coupled receptor kinase 5 in Human [ChEMBL: CHEMBL5678] [GtoPdb: 1469] [UniProtKB: P34947]
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  • G protein-coupled receptor kinase 6 in Human [ChEMBL: CHEMBL6144] [GtoPdb: 1470] [UniProtKB: P43250]
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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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  • homeodomain interacting protein kinase 1/Homeodomain-interacting protein kinase 1 in Human [ChEMBL: CHEMBL5427] [GtoPdb: 2033] [UniProtKB: Q86Z02]
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  • homeodomain interacting protein kinase 2/Homeodomain-interacting protein kinase 2 in Human [ChEMBL: CHEMBL4576] [GtoPdb: 2034] [UniProtKB: Q9H2X6]
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  • homeodomain interacting protein kinase 4/Homeodomain-interacting protein kinase 4 in Human [ChEMBL: CHEMBL1075167] [GtoPdb: 2036] [UniProtKB: Q8NE63]
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  • component of inhibitor of nuclear factor kappa B kinase complex/Inhibitor of nuclear factor kappa-B kinase subunit alpha in Human [ChEMBL: CHEMBL3476] [GtoPdb: 1989] [UniProtKB: O15111]
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  • inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa-B kinase subunit beta in Human [ChEMBL: CHEMBL1991] [GtoPdb: 2039] [UniProtKB: O14920]
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  • inhibitor of nuclear factor kappa B kinase subunit epsilon/Inhibitor of nuclear factor kappa-B kinase subunit epsilon in Human [ChEMBL: CHEMBL3529] [GtoPdb: 2040] [UniProtKB: Q14164]
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  • Insulin-like growth factor I receptor/Insulin-like growth factor 1 receptor in Human [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069]
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  • interleukin 1 receptor associated kinase 4/Interleukin-1 receptor-associated kinase 4 in Human [ChEMBL: CHEMBL3778] [GtoPdb: 2045] [UniProtKB: Q9NWZ3]
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  • leucine rich repeat kinase 2/Leucine-rich repeat serine/threonine-protein kinase 2 in Human [ChEMBL: CHEMBL1075104] [GtoPdb: 2059] [UniProtKB: Q5S007]
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  • leukocyte receptor tyrosine kinase/Leukocyte tyrosine kinase receptor in Human [ChEMBL: CHEMBL5627] [GtoPdb: 1838] [UniProtKB: P29376]
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  • colony stimulating factor 1 receptor/Macrophage colony-stimulating factor 1 receptor in Human [ChEMBL: CHEMBL1844] [GtoPdb: 1806] [UniProtKB: P07333]
  • colony stimulating factor 1 receptor/Macrophage colony-stimulating factor 1 receptor in Mouse [ChEMBL: CHEMBL5570] [GtoPdb: 1806] [UniProtKB: P09581]
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  • macrophage stimulating 1 receptor/Macrophage-stimulating protein receptor in Human [ChEMBL: CHEMBL2689] [GtoPdb: 1816] [UniProtKB: Q04912]
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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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  • MAPK activated protein kinase 3/MAP kinase-activated protein kinase 3 in Human [ChEMBL: CHEMBL4670] [GtoPdb: 2095] [UniProtKB: Q16644]
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  • MAPK activated protein kinase 5/MAP kinase-activated protein kinase 5 in Human [ChEMBL: CHEMBL3094] [GtoPdb: 2096] [UniProtKB: Q8IW41]
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  • microtubule affinity regulating kinase 3/MAP/microtubule affinity-regulating kinase 3 in Human [ChEMBL: CHEMBL5600] [GtoPdb: 2099] [UniProtKB: P27448]
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  • microtubule affinity regulating kinase 4/MAP/microtubule affinity-regulating kinase 4 in Human [ChEMBL: CHEMBL5754] [GtoPdb: 2100] [UniProtKB: Q96L34]
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  • KIT proto-oncogene, receptor tyrosine kinase/Mast/stem cell growth factor receptor Kit in Human [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
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  • maternal embryonic leucine zipper kinase/Maternal embryonic leucine zipper kinase in Human [ChEMBL: CHEMBL4578] [GtoPdb: 2102] [UniProtKB: Q14680]
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  • megakaryocyte-associated tyrosine kinase/Megakaryocyte-associated tyrosine-protein kinase in Human [ChEMBL: CHEMBL4175] [GtoPdb: 2101] [UniProtKB: P42679]
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  • misshapen like kinase 1/Misshapen-like kinase 1 in Human [ChEMBL: CHEMBL5518] [GtoPdb: 2103] [UniProtKB: Q8N4C8]
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  • mitogen-activated protein kinase 1/Mitogen-activated protein kinase 1 in Human [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
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  • mitogen-activated protein kinase 12/Mitogen-activated protein kinase 12 in Human [ChEMBL: CHEMBL4674] [GtoPdb: 1501] [UniProtKB: P53778]
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  • mitogen-activated protein kinase 13/Mitogen-activated protein kinase 13 in Human [ChEMBL: CHEMBL2939] [GtoPdb: 1502] [UniProtKB: O15264]
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  • mitogen-activated protein kinase 3/Mitogen-activated protein kinase 3 in Human [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361]
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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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  • mitogen-activated protein kinase kinase kinase kinase 4/Mitogen-activated protein kinase kinase kinase kinase 4 in Human [ChEMBL: CHEMBL6166] [GtoPdb: 2088] [UniProtKB: O95819]
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  • mitogen-activated protein kinase kinase kinase kinase 5/Mitogen-activated protein kinase kinase kinase kinase 5 in Human [ChEMBL: CHEMBL4852] [GtoPdb: 2089] [UniProtKB: Q9Y4K4]
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  • neurotrophic receptor tyrosine kinase 3/NT-3 growth factor receptor in Human [ChEMBL: CHEMBL5608] [GtoPdb: 1819] [UniProtKB: Q16288]
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  • phosphatidylinositol 3-kinase catalytic subunit type 3/Phosphatidylinositol 3-kinase catalytic subunit type 3 in Human [ChEMBL: CHEMBL1075165] [GtoPdb: 2152] [UniProtKB: Q8NEB9]
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform in Human [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736]
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  • phosphatidylinositol 4-kinase beta/Phosphatidylinositol 4-kinase beta in Human [ChEMBL: CHEMBL3268] [GtoPdb: 2149] [UniProtKB: Q9UBF8]
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  • phosphorylase kinase catalytic subunit gamma 2/Phosphorylase b kinase gamma catalytic chain, liver/testis isoform in Human [ChEMBL: CHEMBL2349] [GtoPdb: 2147] [UniProtKB: P15735]
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  • phosphorylase kinase catalytic subunit gamma 1/Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform in Human [ChEMBL: CHEMBL4004] [GtoPdb: 2145] [UniProtKB: Q16816]
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  • phosphoinositide-3-kinase regulatory subunit 1/phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha/p85-alpha in Human [ChEMBL: CHEMBL2111367] [GtoPdb: 2503, 2153] [UniProtKB: P27986, P42336]
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/phosphoinositide-3-kinase regulatory subunit 1/PI3-kinase p110-delta/p85-alpha in Human [ChEMBL: CHEMBL2111432] [GtoPdb: 2155, 2503] [UniProtKB: O00329, P27986]
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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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  • platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619]
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  • protein kinase C alpha/Protein kinase C alpha type in Human [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252]
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  • protein kinase C beta/Protein kinase C beta type in Human [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771]
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  • protein kinase C delta/Protein kinase C delta type in Human [ChEMBL: CHEMBL2996] [GtoPdb: 1485] [UniProtKB: Q05655]
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  • protein kinase C epsilon/Protein kinase C epsilon type in Human [ChEMBL: CHEMBL3582] [GtoPdb: 1486] [UniProtKB: Q02156]
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  • protein kinase C eta/Protein kinase C eta type in Human [ChEMBL: CHEMBL3616] [GtoPdb: 1487] [UniProtKB: P24723]
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  • protein kinase C gamma/Protein kinase C gamma type in Human [ChEMBL: CHEMBL2938] [GtoPdb: 1484] [UniProtKB: P05129]
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  • protein kinase C iota/Protein kinase C iota type in Human [ChEMBL: CHEMBL2598] [GtoPdb: 1490] [UniProtKB: P41743]
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  • protein kinase C theta/Protein kinase C theta type in Human [ChEMBL: CHEMBL3920] [GtoPdb: 1488] [UniProtKB: Q04759]
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  • protein kinase C zeta/Protein kinase C zeta type in Human [ChEMBL: CHEMBL3438] [GtoPdb: 1491] [UniProtKB: Q05513]
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  • protein tyrosine kinase 2 beta/Protein-tyrosine kinase 2-beta in Human [ChEMBL: CHEMBL5469] [GtoPdb: 2181] [UniProtKB: Q14289]
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  • ret proto-oncogene/Proto-oncogene tyrosine-protein kinase receptor Ret in Human [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
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  • SRC proto-oncogene, non-receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase Src in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
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  • AKT serine/threonine kinase 1/RAC-alpha serine/threonine-protein kinase in Human [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
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  • AKT serine/threonine kinase 2/RAC-beta serine/threonine-protein kinase in Human [ChEMBL: CHEMBL2431] [GtoPdb: 1480] [UniProtKB: P31751]
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  • AKT serine/threonine kinase 3/RAC-gamma serine/threonine-protein kinase in Human [ChEMBL: CHEMBL4816] [GtoPdb: 2286] [UniProtKB: Q9Y243]
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  • fms related receptor tyrosine kinase 3/Receptor-type tyrosine-protein kinase FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
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  • erb-b2 receptor tyrosine kinase 2/Receptor tyrosine-protein kinase erbB-2 in Human [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626]
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  • erb-b2 receptor tyrosine kinase 4/Receptor tyrosine-protein kinase erbB-4 in Human [ChEMBL: CHEMBL3009] [GtoPdb: 1799] [UniProtKB: Q15303]
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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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  • Rho associated coiled-coil containing protein kinase 2/Rho-associated protein kinase 2 in Human [ChEMBL: CHEMBL2973] [GtoPdb: 1504] [UniProtKB: O75116]
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  • G protein-coupled receptor kinase 7/Rhodopsin kinase GRK7 in Human [ChEMBL: CHEMBL1075133] [GtoPdb: 1471] [UniProtKB: Q8WTQ7]
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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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  • ribosomal protein S6 kinase A2/Ribosomal protein S6 kinase alpha-2 in Human [ChEMBL: CHEMBL3906] [GtoPdb: 1529] [UniProtKB: Q15349]
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  • ribosomal protein S6 kinase A3/Ribosomal protein S6 kinase alpha-3 in Human [ChEMBL: CHEMBL2345] [GtoPdb: 1528] [UniProtKB: P51812]
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  • ribosomal protein S6 kinase A4/Ribosomal protein S6 kinase alpha-4 in Human [ChEMBL: CHEMBL3125] [GtoPdb: 1524] [UniProtKB: O75676]
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  • ribosomal protein S6 kinase A5/Ribosomal protein S6 kinase alpha-5 in Human [ChEMBL: CHEMBL4237] [GtoPdb: 1523] [UniProtKB: O75582]
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  • ribosomal protein S6 kinase A6/Ribosomal protein S6 kinase alpha-6 in Human [ChEMBL: CHEMBL4924] [GtoPdb: 1530] [UniProtKB: Q9UK32]
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  • ribosomal protein S6 kinase B1/Ribosomal protein S6 kinase beta-1 in Human [ChEMBL: CHEMBL4501] [GtoPdb: 1525] [UniProtKB: P23443]
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  • serine/threonine kinase 25/Serine/threonine-protein kinase 25 in Human [ChEMBL: CHEMBL5552] [GtoPdb: 2218] [UniProtKB: O00506]
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  • serine/threonine kinase 4/Serine/threonine-protein kinase 4 in Human [ChEMBL: CHEMBL4598] [GtoPdb: 2225] [UniProtKB: Q13043]
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  • BR serine/threonine kinase 1/Serine/threonine-protein kinase BRSK1 in Human [ChEMBL: CHEMBL5650] [GtoPdb: 1946] [UniProtKB: Q8TDC3]
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  • checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757]
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  • protein kinase D1/Serine/threonine-protein kinase D1 in Human [ChEMBL: CHEMBL3863] [GtoPdb: 1489] [UniProtKB: Q15139]
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  • protein kinase D2/Serine/threonine-protein kinase D2 in Human [ChEMBL: CHEMBL4900] [GtoPdb: 2173] [UniProtKB: Q9BZL6]
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  • protein kinase D3/Serine/threonine-protein kinase D3 in Human [ChEMBL: CHEMBL2595] [GtoPdb: 2174] [UniProtKB: O94806]
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  • microtubule affinity regulating kinase 1/Serine/threonine-protein kinase MARK1 in Human [ChEMBL: CHEMBL5940] [GtoPdb: 2097] [UniProtKB: Q9P0L2]
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  • microtubule affinity regulating kinase 2/Serine/threonine-protein kinase MARK2 in Human [ChEMBL: CHEMBL3831] [GtoPdb: 2098] [UniProtKB: Q7KZI7]
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  • CDC42 binding protein kinase alpha/Serine/threonine-protein kinase MRCK alpha in Human [ChEMBL: CHEMBL4516] [GtoPdb: 1507] [UniProtKB: Q5VT25]
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  • CDC42 binding protein kinase beta/Serine/threonine-protein kinase MRCK beta in Human [ChEMBL: CHEMBL5052] [GtoPdb: 1508] [UniProtKB: Q9Y5S2]
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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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  • protein kinase N1/Serine/threonine-protein kinase N1 in Human [ChEMBL: CHEMBL3384] [GtoPdb: 1520] [UniProtKB: Q16512]
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  • NIMA related kinase 1/Serine/threonine-protein kinase Nek1 in Human [ChEMBL: CHEMBL5855] [GtoPdb: 2114] [UniProtKB: Q96PY6]
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  • NIMA related kinase 2/Serine/threonine-protein kinase Nek2 in Human [ChEMBL: CHEMBL3835] [GtoPdb: 2117] [UniProtKB: P51955]
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  • NIMA related kinase 6/Serine/threonine-protein kinase Nek6 in Human [ChEMBL: CHEMBL4309] [GtoPdb: 2121] [UniProtKB: Q9HC98]
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  • NIMA related kinase 9/Serine/threonine-protein kinase Nek9 in Human [ChEMBL: CHEMBL5257] [GtoPdb: 2124] [UniProtKB: Q8TD19]
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  • p21 (RAC1) activated kinase 2/Serine/threonine-protein kinase PAK 2 in Human [ChEMBL: CHEMBL4487] [GtoPdb: 2134] [UniProtKB: Q13177]
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  • p21 (RAC1) activated kinase 3/Serine/threonine-protein kinase PAK 3 in Human [ChEMBL: CHEMBL2999] [GtoPdb: 2135] [UniProtKB: O75914]
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  • p21 (RAC1) activated kinase 4/Serine/threonine-protein kinase PAK 4 in Human [ChEMBL: CHEMBL4482] [GtoPdb: 2136] [UniProtKB: O96013]
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  • p21 (RAC1) activated kinase 5/Serine/threonine-protein kinase PAK 5 in Human [ChEMBL: CHEMBL4524] [GtoPdb: 2138] [UniProtKB: Q9P286]
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  • p21 (RAC1) activated kinase 6/Serine/threonine-protein kinase PAK 6 in Human [ChEMBL: CHEMBL4311] [GtoPdb: 2137] [UniProtKB: Q9NQU5]
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  • Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-1 in Human [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309]
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  • Pim-2 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-2 in Human [ChEMBL: CHEMBL4523] [GtoPdb: 2159] [UniProtKB: Q9P1W9]
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  • polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350]
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  • polo like kinase 2/Serine/threonine-protein kinase PLK2 in Human [ChEMBL: CHEMBL5938] [GtoPdb: 2169] [UniProtKB: Q9NYY3]
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  • polo like kinase 3/Serine/threonine-protein kinase PLK3 in Human [ChEMBL: CHEMBL4897] [GtoPdb: 2170] [UniProtKB: Q9H4B4]
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  • serum/glucocorticoid regulated kinase 1/Serine/threonine-protein kinase Sgk1 in Human [ChEMBL: CHEMBL2343] [GtoPdb: 1534] [UniProtKB: O00141]
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  • serum/glucocorticoid regulated kinase 2/Serine/threonine-protein kinase Sgk2 in Human [ChEMBL: CHEMBL5794] [GtoPdb: 1535] [UniProtKB: Q9HBY8]
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  • serum/glucocorticoid regulated kinase family member 3/Serine/threonine-protein kinase Sgk3 in Human [ChEMBL: CHEMBL6186] [GtoPdb: 1536] [UniProtKB: Q96BR1]
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  • salt inducible kinase 2/Serine/threonine-protein kinase SIK2 in Human [ChEMBL: CHEMBL5699] [GtoPdb: 2198] [UniProtKB: Q9H0K1]
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  • TANK binding kinase 1/Serine/threonine-protein kinase TBK1 in Human [ChEMBL: CHEMBL5408] [GtoPdb: 2237] [UniProtKB: Q9UHD2]
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  • sphingosine kinase 1/Sphingosine kinase 1 in Human [ChEMBL: CHEMBL4394] [GtoPdb: 2204] [UniProtKB: Q9NYA1]
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  • testis specific serine kinase 1B/Testis-specific serine/threonine-protein kinase 1 in Human [ChEMBL: CHEMBL6003] [GtoPdb: 2257] [UniProtKB: Q9BXA7]
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  • testis specific serine kinase 2/Testis-specific serine/threonine-protein kinase 2 in Human [ChEMBL: CHEMBL6014] [GtoPdb: 2258] [UniProtKB: Q96PF2]
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  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL1 in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
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  • ABL proto-oncogene 2, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL2 in Human [ChEMBL: CHEMBL4014] [GtoPdb: 1924] [UniProtKB: P42684]
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  • BLK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Blk in Human [ChEMBL: CHEMBL2250] [GtoPdb: 1940] [UniProtKB: P51451]
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  • Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187]
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  • C-terminal Src kinase/Tyrosine-protein kinase CSK in Human [ChEMBL: CHEMBL2634] [GtoPdb: 1994] [UniProtKB: P41240]
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  • FER tyrosine kinase/Tyrosine-protein kinase Fer in Human [ChEMBL: CHEMBL3982] [GtoPdb: 2022] [UniProtKB: P16591]
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  • FES proto-oncogene, tyrosine kinase/Tyrosine-protein kinase Fes/Fps in Human [ChEMBL: CHEMBL5455] [GtoPdb: 2023] [UniProtKB: P07332]
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  • FGR proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Fgr in Human [ChEMBL: CHEMBL4454] [GtoPdb: 2024] [UniProtKB: P09769]
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  • fyn related Src family tyrosine kinase/Tyrosine-protein kinase FRK in Human [ChEMBL: CHEMBL4223] [GtoPdb: 2025] [UniProtKB: P42685]
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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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  • IL2 inducible T cell kinase/Tyrosine-protein kinase ITK/TSK in Human [ChEMBL: CHEMBL2959] [GtoPdb: 2046] [UniProtKB: Q08881]
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  • Janus kinase 2/Tyrosine-protein kinase JAK2 in Human [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
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  • Janus kinase 3/Tyrosine-protein kinase JAK3 in Human [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
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  • LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lck in Human [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
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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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  • MER proto-oncogene, tyrosine kinase/Tyrosine-protein kinase Mer in Human [ChEMBL: CHEMBL5331] [GtoPdb: 1837] [UniProtKB: Q12866]
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  • TYRO3 protein tyrosine kinase/Tyrosine-protein kinase receptor TYRO3 in Human [ChEMBL: CHEMBL5314] [GtoPdb: 1836] [UniProtKB: Q06418]
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  • AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530]
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  • spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405]
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  • YES proto-oncogene 1, Src family tyrosine kinase/Tyrosine-protein kinase Yes in Human [ChEMBL: CHEMBL2073] [GtoPdb: 2284] [UniProtKB: P07947]
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  • zeta chain of T cell receptor associated protein kinase 70/Tyrosine-protein kinase ZAP-70 in Human [ChEMBL: CHEMBL2803] [GtoPdb: 2285] [UniProtKB: P43403]
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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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  • fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
activin A receptor type 1B/Activin receptor type-1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5310] [GtoPdb: 1787] [UniProtKB: P36896]
ChEMBL Inhibition of ACVR1B (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
ChEMBL Inhibition of ALK (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
protein kinase AMP-activated non-catalytic subunit gamma 1/protein kinase AMP-activated catalytic subunit alpha 1/protein kinase AMP-activated non-catalytic subunit beta 1/AMP-activated protein kinase (AMPK) alpha-1/beta-1/gamma-1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111345] [GtoPdb: 1545, 1541, 1543] [UniProtKB: P54619, Q13131, Q9Y478]
ChEMBL Inhibition of AMPK_A1/B1/G1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
protein kinase AMP-activated non-catalytic subunit gamma 1/protein kinase AMP-activated catalytic subunit alpha 2/protein kinase AMP-activated non-catalytic subunit beta 1/AMPK alpha2/beta1/gamma1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038455] [GtoPdb: 1545, 1542, 1543] [UniProtKB: P54619, P54646, Q9Y478]
ChEMBL Inhibition of AMPK_A2/B1/G1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
TEK receptor tyrosine kinase/Angiopoietin-1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763]
ChEMBL Inhibition of TEK (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
aurora kinase A/Aurora kinase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
ChEMBL Inhibition of AURKA (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
aurora kinase B/Aurora kinase B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
ChEMBL Inhibition of AURKB (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
aurora kinase C/Aurora kinase C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3935] [GtoPdb: 1938] [UniProtKB: Q9UQB9]
ChEMBL Selectivity interaction (SelectScreen (Invitrogen, enzymatic assay with 100 µM ATP)) EUB0000697a AURKC B 6 pIC50 1000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of AURKC (unknown origin) B 6 pIC50 1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
neurotrophic receptor tyrosine kinase 2/BDNF/NT-3 growth factors receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4898] [GtoPdb: 1818] [UniProtKB: Q16620]
ChEMBL Inhibition of NTRK2 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
beta adrenergic receptor kinase 1/Beta-adrenergic receptor kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4079] [GtoPdb: 1466] [UniProtKB: P25098]
ChEMBL Inhibition of ADRBK1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
calcium/calmodulin dependent protein kinase I/Calcium/calmodulin-dependent protein kinase type 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2493] [GtoPdb: 1952] [UniProtKB: Q14012]
ChEMBL Inhibition of CAMK1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
calcium/calmodulin dependent protein kinase ID/Calcium/calmodulin-dependent protein kinase type 1D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5073] [GtoPdb: 1953] [UniProtKB: Q8IU85]
ChEMBL Inhibition of CAMK1D (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
calcium/calmodulin-dependent protein kinase II alpha subunit/Calcium/calmodulin-dependent protein kinase type II subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4147] [GtoPdb: 1555] [UniProtKB: Q9UQM7]
ChEMBL Inhibition of CAMK2A (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
calcium/calmodulin-dependent protein kinase II beta subunit/Calcium/calmodulin-dependent protein kinase type II subunit beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4121] [GtoPdb: 1556] [UniProtKB: Q13554]
ChEMBL Inhibition of CAMK2B (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
calcium/calmodulin-dependent protein kinase II delta subunit/Calcium/calmodulin-dependent protein kinase type II subunit delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2801] [GtoPdb: 1558] [UniProtKB: Q13557]
ChEMBL Inhibition of CAMK2D (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
calcium/calmodulin dependent protein kinase IV/Calcium/calmodulin-dependent protein kinase type IV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2494] [GtoPdb: 1955] [UniProtKB: Q16566]
ChEMBL Inhibition of CAMK4 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
protein kinase, cAMP-dependent, catalytic, alpha subunit/cAMP-dependent protein kinase catalytic subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4101] [GtoPdb: 1476] [UniProtKB: P17612]
ChEMBL Inhibition of PRKACA (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
protein kinase X-linked/cAMP-dependent protein kinase catalytic subunit PRKX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5818] [GtoPdb: 2175] [UniProtKB: P51817]
ChEMBL Inhibition of PRKX (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
casein kinase 1 alpha 1/Casein kinase I isoform alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2793] [GtoPdb: 1995] [UniProtKB: P48729]
ChEMBL Inhibition of CSNK1A1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
casein kinase 1 delta/Casein kinase I isoform delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730]
ChEMBL Inhibition of CSNK1D (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
casein kinase 1 epsilon/Casein kinase I isoform epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674]
ChEMBL Inhibition of CSNK1E (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
casein kinase 1 gamma 1/Casein kinase I isoform gamma-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2426] [GtoPdb: 1999] [UniProtKB: Q9HCP0]
ChEMBL Inhibition of CSNK1G1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
casein kinase 1 gamma 2/Casein kinase I isoform gamma-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2543] [GtoPdb: 2000] [UniProtKB: P78368]
ChEMBL Inhibition of CSNK1G2 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
casein kinase 1 gamma 3/Casein kinase I isoform gamma-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5084] [GtoPdb: 2001] [UniProtKB: Q9Y6M4]
ChEMBL Inhibition of CSNK1G3 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3629] [GtoPdb: 1549] [UniProtKB: P68400]
ChEMBL Inhibition of CSNK2A1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
casein kinase 2, alpha prime polypeptide subunit/Casein kinase II subunit alpha` in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4070] [GtoPdb: 1550] [UniProtKB: P19784]
ChEMBL Inhibition of CSNK2A2 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
cyclin dependent kinase 7/CDK7/Cyclin H/MNAT1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038473] [GtoPdb: 1979] [UniProtKB: P50613, P51946, P51948]
ChEMBL Inhibition of CDK7/CyclinH/MNAT1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
cyclin dependent kinase 9/CDK9/cyclin T1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111389] [GtoPdb: 1981] [UniProtKB: O60563, P50750]
ChEMBL Inhibition of CDK9/CyclinT1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
Protein kinase G (PKG) 1/cGMP-dependent protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4273] [GtoPdb: 1492] [UniProtKB: Q13976]
ChEMBL Inhibition of PRKG1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
Protein kinase G (PKG) 2/cGMP-dependent protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2896] [GtoPdb: 1493] [UniProtKB: Q13237]
ChEMBL Inhibition of PRKG2 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
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 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078]
ChEMBL Inhibition of CDK5_p25 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
ChEMBL Inhibition of CDK5_p35 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
CYP1A2/Cytochrome P450 1A2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3356] [GtoPdb: 1319] [UniProtKB: P05177]
ChEMBL Inhibition Enzyme Assay: CYP (Cytochrome P450) enzymes are the major drug metabolizing enzymes present in the liver. The inhibition of CYP enzyme activity (IC50) for each of CYP1A2, CYP2C19, CYP2C9, CYP2D6, CYP3A4(BFC) and CYP3A4(BQ) is determined for compounds, where inhibition of metabolism of a known substrate leads to a decrease in the fluorescence of the metabolized product. The fluorescence of the product is monitored as a function of compound concentration.Compounds are dissolved in DMSO to a concentration of 100 mM. These are diluted 1 uL into 82 uL of acetonitrile. An 11 uL aliquot of this solution is then added to 204 uL of cofactor mix (1.3% NADPH Regeneration system Solution A, 1.04% NADPH Regeneration system Solution B from BD Biosciences, 5% acetonitrile and 0.05% DMSO). These are then serially diluted 1:1 (160 uL to 160 uL co-factor mix) for a total of 10 points. A 10 uL aliquot of this final mixture is dispensed into 384 well assay plates. B 5 pIC50 >10000 nM IC50 US-9096593-B2. Compounds and methods for kinase modulation, and indications therefor (2015)
CYP2C19/Cytochrome P450 2C19 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3622] [GtoPdb: 1328] [UniProtKB: P33261]
ChEMBL Inhibition Enzyme Assay: CYP (Cytochrome P450) enzymes are the major drug metabolizing enzymes present in the liver. The inhibition of CYP enzyme activity (IC50) for each of CYP1A2, CYP2C19, CYP2C9, CYP2D6, CYP3A4(BFC) and CYP3A4(BQ) is determined for compounds, where inhibition of metabolism of a known substrate leads to a decrease in the fluorescence of the metabolized product. The fluorescence of the product is monitored as a function of compound concentration.Compounds are dissolved in DMSO to a concentration of 100 mM. These are diluted 1 uL into 82 uL of acetonitrile. An 11 uL aliquot of this solution is then added to 204 uL of cofactor mix (1.3% NADPH Regeneration system Solution A, 1.04% NADPH Regeneration system Solution B from BD Biosciences, 5% acetonitrile and 0.05% DMSO). These are then serially diluted 1:1 (160 uL to 160 uL co-factor mix) for a total of 10 points. A 10 uL aliquot of this final mixture is dispensed into 384 well assay plates. B 5.3 pIC50 5000 nM IC50 US-9096593-B2. Compounds and methods for kinase modulation, and indications therefor (2015)
CYP2C9/Cytochrome P450 2C9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3397] [GtoPdb: 1326] [UniProtKB: P11712]
ChEMBL Inhibition Enzyme Assay: CYP (Cytochrome P450) enzymes are the major drug metabolizing enzymes present in the liver. The inhibition of CYP enzyme activity (IC50) for each of CYP1A2, CYP2C19, CYP2C9, CYP2D6, CYP3A4(BFC) and CYP3A4(BQ) is determined for compounds, where inhibition of metabolism of a known substrate leads to a decrease in the fluorescence of the metabolized product. The fluorescence of the product is monitored as a function of compound concentration.Compounds are dissolved in DMSO to a concentration of 100 mM. These are diluted 1 uL into 82 uL of acetonitrile. An 11 uL aliquot of this solution is then added to 204 uL of cofactor mix (1.3% NADPH Regeneration system Solution A, 1.04% NADPH Regeneration system Solution B from BD Biosciences, 5% acetonitrile and 0.05% DMSO). These are then serially diluted 1:1 (160 uL to 160 uL co-factor mix) for a total of 10 points. A 10 uL aliquot of this final mixture is dispensed into 384 well assay plates. B 5.3 pIC50 5000 nM IC50 US-9096593-B2. Compounds and methods for kinase modulation, and indications therefor (2015)
CYP2D6/Cytochrome P450 2D6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL289] [GtoPdb: 1329] [UniProtKB: P10635]
ChEMBL Inhibition Enzyme Assay: CYP (Cytochrome P450) enzymes are the major drug metabolizing enzymes present in the liver. The inhibition of CYP enzyme activity (IC50) for each of CYP1A2, CYP2C19, CYP2C9, CYP2D6, CYP3A4(BFC) and CYP3A4(BQ) is determined for compounds, where inhibition of metabolism of a known substrate leads to a decrease in the fluorescence of the metabolized product. The fluorescence of the product is monitored as a function of compound concentration.Compounds are dissolved in DMSO to a concentration of 100 mM. These are diluted 1 uL into 82 uL of acetonitrile. An 11 uL aliquot of this solution is then added to 204 uL of cofactor mix (1.3% NADPH Regeneration system Solution A, 1.04% NADPH Regeneration system Solution B from BD Biosciences, 5% acetonitrile and 0.05% DMSO). These are then serially diluted 1:1 (160 uL to 160 uL co-factor mix) for a total of 10 points. A 10 uL aliquot of this final mixture is dispensed into 384 well assay plates. B 5 pIC50 >10000 nM IC50 US-9096593-B2. Compounds and methods for kinase modulation, and indications therefor (2015)
ChEMBL Inhibition Enzyme Assay: CYP (Cytochrome P450) enzymes are the major drug metabolizing enzymes present in the liver. The inhibition of CYP enzyme activity (IC50) for each of CYP1A2, CYP2C19, CYP2C9, CYP2D6, CYP3A4(BFC) and CYP3A4(BQ) is determined for compounds, where inhibition of metabolism of a known substrate leads to a decrease in the fluorescence of the metabolized product. The fluorescence of the product is monitored as a function of compound concentration.Compounds are dissolved in DMSO to a concentration of 100 mM. These are diluted 1 uL into 82 uL of acetonitrile. An 11 uL aliquot of this solution is then added to 204 uL of cofactor mix (1.3% NADPH Regeneration system Solution A, 1.04% NADPH Regeneration system Solution B from BD Biosciences, 5% acetonitrile and 0.05% DMSO). These are then serially diluted 1:1 (160 uL to 160 uL co-factor mix) for a total of 10 points. A 10 uL aliquot of this final mixture is dispensed into 384 well assay plates. B 5 pIC50 >10000 nM IC50 US-9096593-B2. Compounds and methods for kinase modulation, and indications therefor (2015)
CYP3A4/Cytochrome P450 3A4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL340] [GtoPdb: 1337] [UniProtKB: P08684]
ChEMBL Inhibition Enzyme Assay: CYP (Cytochrome P450) enzymes are the major drug metabolizing enzymes present in the liver. The inhibition of CYP enzyme activity (IC50) for each of CYP1A2, CYP2C19, CYP2C9, CYP2D6, CYP3A4(BFC) and CYP3A4(BQ) is determined for compounds, where inhibition of metabolism of a known substrate leads to a decrease in the fluorescence of the metabolized product. The fluorescence of the product is monitored as a function of compound concentration.Compounds are dissolved in DMSO to a concentration of 100 mM. These are diluted 1 uL into 82 uL of acetonitrile. An 11 uL aliquot of this solution is then added to 204 uL of cofactor mix (1.3% NADPH Regeneration system Solution A, 1.04% NADPH Regeneration system Solution B from BD Biosciences, 5% acetonitrile and 0.05% DMSO). These are then serially diluted 1:1 (160 uL to 160 uL co-factor mix) for a total of 10 points. A 10 uL aliquot of this final mixture is dispensed into 384 well assay plates. B 5 pIC50 >10000 nM IC50 US-9096593-B2. Compounds and methods for kinase modulation, and indications therefor (2015)
ChEMBL Inhibition Enzyme Assay: CYP (Cytochrome P450) enzymes are the major drug metabolizing enzymes present in the liver. The inhibition of CYP enzyme activity (IC50) for each of CYP1A2, CYP2C19, CYP2C9, CYP2D6, CYP3A4(BFC) and CYP3A4(BQ) is determined for compounds, where inhibition of metabolism of a known substrate leads to a decrease in the fluorescence of the metabolized product. The fluorescence of the product is monitored as a function of compound concentration.Compounds are dissolved in DMSO to a concentration of 100 mM. These are diluted 1 uL into 82 uL of acetonitrile. An 11 uL aliquot of this solution is then added to 204 uL of cofactor mix (1.3% NADPH Regeneration system Solution A, 1.04% NADPH Regeneration system Solution B from BD Biosciences, 5% acetonitrile and 0.05% DMSO). These are then serially diluted 1:1 (160 uL to 160 uL co-factor mix) for a total of 10 points. A 10 uL aliquot of this final mixture is dispensed into 384 well assay plates. B 5.3 pIC50 5000 nM IC50 US-9096593-B2. Compounds and methods for kinase modulation, and indications therefor (2015)
BMX non-receptor tyrosine kinase/Cytoplasmic tyrosine-protein kinase BMX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3834] [GtoPdb: 1942] [UniProtKB: P51813]
ChEMBL Inhibition of BMX (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
death associated protein kinase 1/Death-associated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2558] [GtoPdb: 2002] [UniProtKB: P53355]
ChEMBL Inhibition of DAPK1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
death associated protein kinase 3/Death-associated protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2468] [GtoPdb: 2004] [UniProtKB: O43293]
ChEMBL Inhibition of DAPK3 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
CDC like kinase 2/Dual specificity protein kinase CLK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4225] [GtoPdb: 1991] [UniProtKB: P49760]
ChEMBL Inhibition of CLK2 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
dual specificity tyrosine phosphorylation regulated kinase 1A/Dual specificity tyrosine-phosphorylation-regulated kinase 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2292] [GtoPdb: 2009] [UniProtKB: Q13627]
ChEMBL Inhibition of DYRK1A (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
dual specificity tyrosine phosphorylation regulated kinase 1B/Dual specificity tyrosine-phosphorylation-regulated kinase 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5543] [GtoPdb: 2010] [UniProtKB: Q9Y463]
ChEMBL Inhibition of DYRK1B (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
dual specificity tyrosine phosphorylation regulated kinase 3/Dual specificity tyrosine-phosphorylation-regulated kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4575] [GtoPdb: 2012] [UniProtKB: O43781]
ChEMBL Inhibition of DYRK3 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
dual specificity tyrosine phosphorylation regulated kinase 4/Dual specificity tyrosine-phosphorylation-regulated kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075115] [GtoPdb: 2013] [UniProtKB: Q9NR20]
ChEMBL Inhibition of DYRK4 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
EPH receptor A1/Ephrin type-A receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5810] [GtoPdb: 1821] [UniProtKB: P21709]
ChEMBL Inhibition of EPHA1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
EPH receptor A2/Ephrin type-A receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317]
ChEMBL Inhibition of EPHA2 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
EPH receptor A3/Ephrin type-A receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4954] [GtoPdb: 1823] [UniProtKB: P29320]
ChEMBL Inhibition of EPHA3 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
EPH receptor A5/Ephrin type-A receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3987] [GtoPdb: 1825] [UniProtKB: P54756]
ChEMBL Inhibition of EPHA5 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
EPH receptor A8/Ephrin type-A receptor 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4134] [GtoPdb: 1828] [UniProtKB: P29322]
ChEMBL Inhibition of EPHA8 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
EPH receptor B1/Ephrin type-B receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5072] [GtoPdb: 1830] [UniProtKB: P54762]
ChEMBL Inhibition of EPHB1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
EPH receptor B2/Ephrin type-B receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323]
ChEMBL Inhibition of EPHB2 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
EPH receptor B3/Ephrin type-B receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4901] [GtoPdb: 1832] [UniProtKB: P54753]
ChEMBL Inhibition of EPHB3 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
EPH receptor B4/Ephrin type-B receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5147] [GtoPdb: 1833] [UniProtKB: P54760]
ChEMBL Inhibition of EPHB4 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
epidermal growth factor receptor/Epidermal growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibition of EGFR (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
eukaryotic elongation factor 2 kinase/Eukaryotic elongation factor 2 kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5026] [GtoPdb: 2014] [UniProtKB: O00418]
ChEMBL Inhibition of EEF2K (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
ChEMBL Inhibition of FGFR1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802]
ChEMBL Inhibition of FGFR2 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607]
ChEMBL Inhibition of FGFR3 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
fibroblast growth factor receptor 4/Fibroblast growth factor receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3973] [GtoPdb: 1811] [UniProtKB: P22455]
ChEMBL Inhibition of FGFR4 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
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 GSK3A (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
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 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
beta adrenergic receptor kinase 2/G protein-coupled receptor kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075166] [GtoPdb: 1467] [UniProtKB: P35626]
ChEMBL Inhibition of ADRBK2 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
G protein-coupled receptor kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5861] [GtoPdb: 1468] [UniProtKB: P32298]
ChEMBL Inhibition of GRK4 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
G protein-coupled receptor kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5678] [GtoPdb: 1469] [UniProtKB: P34947]
ChEMBL Inhibition of GRK5 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
G protein-coupled receptor kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6144] [GtoPdb: 1470] [UniProtKB: P43250]
ChEMBL Inhibition of GRK6 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
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 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
homeodomain interacting protein kinase 1/Homeodomain-interacting protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5427] [GtoPdb: 2033] [UniProtKB: Q86Z02]
ChEMBL Inhibition of HIPK1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
homeodomain interacting protein kinase 2/Homeodomain-interacting protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4576] [GtoPdb: 2034] [UniProtKB: Q9H2X6]
ChEMBL Inhibition of HIPK2 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
homeodomain interacting protein kinase 4/Homeodomain-interacting protein kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075167] [GtoPdb: 2036] [UniProtKB: Q8NE63]
ChEMBL Inhibition of HIPK4 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
component of inhibitor of nuclear factor kappa B kinase complex/Inhibitor of nuclear factor kappa-B kinase subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3476] [GtoPdb: 1989] [UniProtKB: O15111]
ChEMBL Inhibition of CHUK (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa-B kinase subunit beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1991] [GtoPdb: 2039] [UniProtKB: O14920]
ChEMBL Inhibition of IKBKB (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
inhibitor of nuclear factor kappa B kinase subunit epsilon/Inhibitor of nuclear factor kappa-B kinase subunit epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3529] [GtoPdb: 2040] [UniProtKB: Q14164]
ChEMBL Inhibition of IKBKE (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
Insulin-like growth factor I receptor/Insulin-like growth factor 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069]
ChEMBL Inhibition of IGF1R (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213]
ChEMBL Inhibition of INSR (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
interleukin 1 receptor associated kinase 4/Interleukin-1 receptor-associated kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3778] [GtoPdb: 2045] [UniProtKB: Q9NWZ3]
ChEMBL Inhibition of IRAK4 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
leucine rich repeat kinase 2/Leucine-rich repeat serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075104] [GtoPdb: 2059] [UniProtKB: Q5S007]
ChEMBL Inhibition of LRRK2 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
leukocyte receptor tyrosine kinase/Leukocyte tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5627] [GtoPdb: 1838] [UniProtKB: P29376]
ChEMBL Inhibition of LTK (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
colony stimulating factor 1 receptor/Macrophage colony-stimulating factor 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1844] [GtoPdb: 1806] [UniProtKB: P07333]
ChEMBL Inhibition of CSF1R (unknown origin) expressed in mouse NFS-60 cells assessed as inhibition of CSF1-CSF1R dependent cell proliferation incubated for 3 days by ATPlite 1step Luminescence Assay reagent based assay B 6.59 pIC50 260 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
ChEMBL Inhibition of CSF1R (unknown origin) expressed in mouse EOC 20 cells assessed as inhibition of CSF1-CSF1R dependent cell proliferation incubated for 3 days by ATPlite 1step Luminescence Assay reagent based assay B 6.96 pIC50 110 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
ChEMBL Biochemical Assay: In one assay the biochemical activity IC50 values are determined with respect to inhibition of Fms kinase activity, where inhibition of phosphorylation of a peptide substrate is measured as a function of compound concentration. Compounds to be tested, dissolved in DMSO (1 uL), are added to a white 384-well plate (Costar #3705). Working stocks of Fms kinase (Invitrogen #PV3249), biotin-(E4Y)10 substrate (Upstate Biotech, Cat#12-440), and ATP (Sigma, Cat#A-3377) are prepared in 25 mM Hepes pH 7.5, 0.5 mM MgCl2, 2 mM MnCl2, 2 mM DTT, 0.01% BSA, and 0.01% Tween-20. All components are added to the 384-well plate for a final concentration of 1 ng/well Fms, 30 nM biotin-(E4Y)10 (Upstate Biotechnology) and 100 uM ATP in a volume of 20 uL. Each sample is at 5% DMSO. The plate is then incubated for 20 minutes at 30 C. Just before use, working stocks of donor and acceptor beads from the AlphaScreen PY20 Detection Kit (PerkinElmer, Cat#676601M) are prepared in 25 mM Hepes pH 7.5. B 7 pIC50 <100 nM IC50 US-9096593-B2. Compounds and methods for kinase modulation, and indications therefor (2015)
ChEMBL Biochemical Assay: In one assay the biochemical activity IC50 values are determined with respect to inhibition of Fms kinase activity, where inhibition of phosphorylation of a peptide substrate is measured as a function of compound concentration. Compounds to be tested, dissolved in DMSO (1 uL), are added to a white 384-well plate (Costar #3705). Working stocks of Fms kinase (Invitrogen #PV3249), biotin-(E4Y)10 substrate (Upstate Biotech, Cat#12-440), and ATP (Sigma, Cat#A-3377) are prepared in 25 mM Hepes pH 7.5, 0.5 mM MgCl2, 2 mM MnCl2, 2 mM DTT, 0.01% BSA, and 0.01% Tween-20. All components are added to the 384-well plate for a final concentration of 1 ng/well Fms, 30 nM biotin-(E4Y)10 (Upstate Biotechnology) and 100 uM ATP in a volume of 20 uL. Each sample is at 5% DMSO. The plate is then incubated for 20 minutes at 30 C. Just before use, working stocks of donor and acceptor beads from the AlphaScreen PY20 Detection Kit (PerkinElmer, Cat#676601M) are prepared in 25 mM Hepes pH 7.5. B 7 pIC50 <100 nM IC50 US-9096593-B2. Compounds and methods for kinase modulation, and indications therefor (2015)
ChEMBL Affinity Phenotypic Cellular interaction (THP-1 CSF1R phosphor-Tyr assay (CSF1R autophosphorylation in human acute monocytic leukemia cell line THP-1)) EUB0000697a CSF1R B 7.24 pIC50 58 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of CSF1R autophosphorylation in human THP-1 cells B 7.24 pIC50 58 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
ChEMBL Inhibition of CSF1R (unknown origin) B 7.8 pIC50 16 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
ChEMBL Inhibition of CSF1R (unknown origin) in presence of 100 uM ATP by enzymatic assay B 7.8 pIC50 16 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
ChEMBL Affinity Biochemical interaction (Enzymatic inhibition assay (100 µM ATP)) EUB0000697a CSF1R B 7.8 pIC50 16 nM IC50 Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of human CSF1R by discoverX kinome scan assay B 7.8 pIC50 16 nM IC50 Eur J Med Chem (2023) 245: 114884-114884 [PMID:36335744]
colony stimulating factor 1 receptor/Macrophage colony-stimulating factor 1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5570] [GtoPdb: 1806] [UniProtKB: P09581]
ChEMBL Inhibition of CSF1R autophosphorylation in mouse RAW264.7 cells measured after 4 hrs by Western blot analysis B 7.59 pIC50 26 nM IC50 Eur J Med Chem (2023) 245: 114884-114884 [PMID:36335744]
macrophage stimulating 1 receptor/Macrophage-stimulating protein receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2689] [GtoPdb: 1816] [UniProtKB: Q04912]
ChEMBL Inhibition of MST1R (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
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 MAPKAPK2 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
MAPK activated protein kinase 3/MAP kinase-activated protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4670] [GtoPdb: 2095] [UniProtKB: Q16644]
ChEMBL Inhibition of MAPKAPK3 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
MAPK activated protein kinase 5/MAP kinase-activated protein kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3094] [GtoPdb: 2096] [UniProtKB: Q8IW41]
ChEMBL Inhibition of MAPKAPK5 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
microtubule affinity regulating kinase 3/MAP/microtubule affinity-regulating kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5600] [GtoPdb: 2099] [UniProtKB: P27448]
ChEMBL Inhibition of MARK3 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
microtubule affinity regulating kinase 4/MAP/microtubule affinity-regulating kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5754] [GtoPdb: 2100] [UniProtKB: Q96L34]
ChEMBL Inhibition of MARK4 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
KIT proto-oncogene, receptor tyrosine kinase/Mast/stem cell growth factor receptor Kit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
ChEMBL Inhibition of endogenous KIT in human M-07e cells assessed as inhibition of SCF-KIT dependent cell proliferation incubated for 3 days by ATPlite 1step Luminescence Assay reagent based assay B 5.34 pIC50 4600 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
ChEMBL Selectivity interaction (BCR-KIT fusion dependent proliferation of Ba/F3 cells) EUB0000697a KIT B 5.57 pIC50 2700 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of KIT (unknown origin) in presence of ATP by enzymatic assay B 6.07 pIC50 860 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
ChEMBL Inhibition of KIT (unknown origin) B 6.07 pIC50 860 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
ChEMBL Selectivity interaction (SelectScreen (Invitrogen, enzymatic assay with 100 µM ATP)) EUB0000697a KIT B 6.07 pIC50 860 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
GtoPdb Binned IC50 value from patent data - 7 pIC50 >100 nM IC50 US9096593B2. Compounds and methods for kinase modulation, and indications therefor (2015)
ChEMBL Biochemical Assay: In one assay the biochemical activity IC50 values are determined with respect to inhibition of c-Kit kinase activity, where inhibition of phosphorylation of a peptide substrate is measured as a function of compound concentration. Compounds to be tested are dissolved in DMSO to a concentration of 20 mM. These are diluted 30 uL into 120 uL of DMSO (4 mM) and 1 uL is added to an assay plate. These are then serially diluted 1:2 (50 uL to 100 uL DMSO) for a total of 8 points. Plates are prepared such that each kinase reaction is 20 uL in 1x kinase buffer (25 mM HEPES, pH 7.5, 2 mM MgCl2, 2 mM MnCl2, 0.01% Tween-20, 1 mM DTT, 0.01% BSA), 5% DMSO and 100 uM ATP. Substrate is 30 nM biotin-(E4Y)10 (Millipore). C-kit kinase (obtained from Millipore (#14-559) or is prepared as described in U.S. Patent Application Publication Number 2009/0076046, the disclosure of which is hereby incorporated by reference as it relates to this assay) is at 0.75 ng per sample. B 7 pIC50 >100 nM IC50 US-9096593-B2. Compounds and methods for kinase modulation, and indications therefor (2015)
ChEMBL Biochemical Assay: In one assay the biochemical activity IC50 values are determined with respect to inhibition of c-Kit kinase activity, where inhibition of phosphorylation of a peptide substrate is measured as a function of compound concentration. Compounds to be tested are dissolved in DMSO to a concentration of 20 mM. These are diluted 30 uL into 120 uL of DMSO (4 mM) and 1 uL is added to an assay plate. These are then serially diluted 1:2 (50 uL to 100 uL DMSO) for a total of 8 points. Plates are prepared such that each kinase reaction is 20 uL in 1x kinase buffer (25 mM HEPES, pH 7.5, 2 mM MgCl2, 2 mM MnCl2, 0.01% Tween-20, 1 mM DTT, 0.01% BSA), 5% DMSO and 100 uM ATP. Substrate is 30 nM biotin-(E4Y)10 (Millipore). C-kit kinase (obtained from Millipore (#14-559) or is prepared as described in U.S. Patent Application Publication Number 2009/0076046, the disclosure of which is hereby incorporated by reference as it relates to this assay) is at 0.75 ng per sample. B 7 pIC50 >100 nM IC50 US-9096593-B2. Compounds and methods for kinase modulation, and indications therefor (2015)
maternal embryonic leucine zipper kinase/Maternal embryonic leucine zipper kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4578] [GtoPdb: 2102] [UniProtKB: Q14680]
ChEMBL Inhibition of MELK (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
megakaryocyte-associated tyrosine kinase/Megakaryocyte-associated tyrosine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4175] [GtoPdb: 2101] [UniProtKB: P42679]
ChEMBL Inhibition of MATK (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
misshapen like kinase 1/Misshapen-like kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5518] [GtoPdb: 2103] [UniProtKB: Q8N4C8]
ChEMBL Inhibition of MINK1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
mitogen-activated protein kinase 1/Mitogen-activated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
ChEMBL Inhibition of MAPK1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
mitogen-activated protein kinase 12/Mitogen-activated protein kinase 12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4674] [GtoPdb: 1501] [UniProtKB: P53778]
ChEMBL Inhibition of MAPK12 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
mitogen-activated protein kinase 13/Mitogen-activated protein kinase 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2939] [GtoPdb: 1502] [UniProtKB: O15264]
ChEMBL Inhibition of MAPK13 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
mitogen-activated protein kinase 3/Mitogen-activated protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361]
ChEMBL Inhibition of MAPK3 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
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 MAP4K2 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
mitogen-activated protein kinase kinase kinase kinase 4/Mitogen-activated protein kinase kinase kinase kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6166] [GtoPdb: 2088] [UniProtKB: O95819]
ChEMBL Inhibition of MAP4K4 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
mitogen-activated protein kinase kinase kinase kinase 5/Mitogen-activated protein kinase kinase kinase kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4852] [GtoPdb: 2089] [UniProtKB: Q9Y4K4]
ChEMBL Inhibition of MAP4K5 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
neurotrophic receptor tyrosine kinase 3/NT-3 growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5608] [GtoPdb: 1819] [UniProtKB: Q16288]
ChEMBL Inhibition of NTRK3 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
phosphatidylinositol 3-kinase catalytic subunit type 3/Phosphatidylinositol 3-kinase catalytic subunit type 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075165] [GtoPdb: 2152] [UniProtKB: Q8NEB9]
ChEMBL Inhibition of PIK3C3 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736]
ChEMBL Inhibition of PIK3CG (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
phosphatidylinositol 4-kinase beta/Phosphatidylinositol 4-kinase beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3268] [GtoPdb: 2149] [UniProtKB: Q9UBF8]
ChEMBL Inhibition of PI4KB (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
phosphorylase kinase catalytic subunit gamma 2/Phosphorylase b kinase gamma catalytic chain, liver/testis isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2349] [GtoPdb: 2147] [UniProtKB: P15735]
ChEMBL Inhibition of PHKG2 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
phosphorylase kinase catalytic subunit gamma 1/Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4004] [GtoPdb: 2145] [UniProtKB: Q16816]
ChEMBL Inhibition of PHKG1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
phosphoinositide-3-kinase regulatory subunit 1/phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha/p85-alpha in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111367] [GtoPdb: 2503, 2153] [UniProtKB: P27986, P42336]
ChEMBL Inhibition of PIK3CA/PIK3R1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/phosphoinositide-3-kinase regulatory subunit 1/PI3-kinase p110-delta/p85-alpha in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111432] [GtoPdb: 2155, 2503] [UniProtKB: O00329, P27986]
ChEMBL Inhibition of PIK3CD/PIK3R1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
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 PDGFRA (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619]
ChEMBL Inhibition of PDGFRB (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
protein kinase C alpha/Protein kinase C alpha type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252]
ChEMBL Inhibition of PRKCA (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
protein kinase C beta/Protein kinase C beta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771]
ChEMBL Inhibition of PRKCB1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
ChEMBL Inhibition of PRKCB2 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
protein kinase C delta/Protein kinase C delta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2996] [GtoPdb: 1485] [UniProtKB: Q05655]
ChEMBL Inhibition of PRKCD (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
protein kinase C epsilon/Protein kinase C epsilon type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3582] [GtoPdb: 1486] [UniProtKB: Q02156]
ChEMBL Inhibition of PRKCE (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
protein kinase C eta/Protein kinase C eta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3616] [GtoPdb: 1487] [UniProtKB: P24723]
ChEMBL Inhibition of PRKCH (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
protein kinase C gamma/Protein kinase C gamma type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2938] [GtoPdb: 1484] [UniProtKB: P05129]
ChEMBL Inhibition of PRKCG (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
protein kinase C iota/Protein kinase C iota type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2598] [GtoPdb: 1490] [UniProtKB: P41743]
ChEMBL Inhibition of PRKCI (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
protein kinase C theta/Protein kinase C theta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3920] [GtoPdb: 1488] [UniProtKB: Q04759]
ChEMBL Inhibition of PRKCQ (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
protein kinase C zeta/Protein kinase C zeta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3438] [GtoPdb: 1491] [UniProtKB: Q05513]
ChEMBL Inhibition of PRKCZ (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
protein tyrosine kinase 2 beta/Protein-tyrosine kinase 2-beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5469] [GtoPdb: 2181] [UniProtKB: Q14289]
ChEMBL Inhibition of PTK2B (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
ret proto-oncogene/Proto-oncogene tyrosine-protein kinase receptor Ret in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
ChEMBL Inhibition of RET (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
ChEMBL Inhibition of RET V804L mutant (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
ChEMBL Inhibition of RET Y791F mutant (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
SRC proto-oncogene, non-receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase Src in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
ChEMBL Inhibition of SRC (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
AKT serine/threonine kinase 1/RAC-alpha serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
ChEMBL Inhibition of AKT1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
AKT serine/threonine kinase 2/RAC-beta serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2431] [GtoPdb: 1480] [UniProtKB: P31751]
ChEMBL Inhibition of AKT2 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
AKT serine/threonine kinase 3/RAC-gamma serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4816] [GtoPdb: 2286] [UniProtKB: Q9Y243]
ChEMBL Inhibition of AKT3 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
fms related receptor tyrosine kinase 3/Receptor-type tyrosine-protein kinase FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
ChEMBL Selectivity interaction (FLT3-ITD dependent proliferation of Ba/F3 cells) EUB0000697a FLT3 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of FLT3-ITD (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of FLT3-ITD dependent cell proliferation incubated for 3 days by ATPlite 1step Luminescence Assay reagent based assay B 5 pIC50 >10000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
ChEMBL Inhibition of FLT3 (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of FLT3 ligand-FLT3 dependent cell proliferation incubated for 3 days by ATPlite 1step Luminescence Assay reagent based assay B 5 pIC50 >10000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
ChEMBL Selectivity interaction (SelectScreen (Invitrogen, enzymatic assay with 100 µM ATP)) EUB0000697a FLT3 B 6.41 pIC50 390 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of FLT3 (unknown origin) B 6.41 pIC50 390 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
ChEMBL Inhibition of FLT3 (unknown origin) in presence of ATP by enzymatic assay B 6.41 pIC50 390 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
erb-b2 receptor tyrosine kinase 2/Receptor tyrosine-protein kinase erbB-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626]
ChEMBL Inhibition of ERBB2 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
erb-b2 receptor tyrosine kinase 4/Receptor tyrosine-protein kinase erbB-4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3009] [GtoPdb: 1799] [UniProtKB: Q15303]
ChEMBL Inhibition of ERBB4 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
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 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
Rho associated coiled-coil containing protein kinase 2/Rho-associated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2973] [GtoPdb: 1504] [UniProtKB: O75116]
ChEMBL Inhibition of ROCK2 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
G protein-coupled receptor kinase 7/Rhodopsin kinase GRK7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075133] [GtoPdb: 1471] [UniProtKB: Q8WTQ7]
ChEMBL Inhibition of GRK7 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
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 RPS6KA1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
ribosomal protein S6 kinase A2/Ribosomal protein S6 kinase alpha-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3906] [GtoPdb: 1529] [UniProtKB: Q15349]
ChEMBL Inhibition of RPS6KA2 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
ribosomal protein S6 kinase A3/Ribosomal protein S6 kinase alpha-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2345] [GtoPdb: 1528] [UniProtKB: P51812]
ChEMBL Inhibition of RPS6KA3 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
ribosomal protein S6 kinase A4/Ribosomal protein S6 kinase alpha-4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3125] [GtoPdb: 1524] [UniProtKB: O75676]
ChEMBL Inhibition of RPS6KA4 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
ribosomal protein S6 kinase A5/Ribosomal protein S6 kinase alpha-5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4237] [GtoPdb: 1523] [UniProtKB: O75582]
ChEMBL Inhibition of RPS6KA5 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
ribosomal protein S6 kinase A6/Ribosomal protein S6 kinase alpha-6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4924] [GtoPdb: 1530] [UniProtKB: Q9UK32]
ChEMBL Inhibition of RPS6KA6 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
ribosomal protein S6 kinase B1/Ribosomal protein S6 kinase beta-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4501] [GtoPdb: 1525] [UniProtKB: P23443]
ChEMBL Inhibition of RPS6KB1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
serine/threonine kinase 25/Serine/threonine-protein kinase 25 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5552] [GtoPdb: 2218] [UniProtKB: O00506]
ChEMBL Inhibition of STK25 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
serine/threonine kinase 4/Serine/threonine-protein kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4598] [GtoPdb: 2225] [UniProtKB: Q13043]
ChEMBL Inhibition of STK4 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
BR serine/threonine kinase 1/Serine/threonine-protein kinase BRSK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5650] [GtoPdb: 1946] [UniProtKB: Q8TDC3]
ChEMBL Inhibition of BRSK1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757]
ChEMBL Inhibition of CHEK1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
protein kinase D1/Serine/threonine-protein kinase D1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3863] [GtoPdb: 1489] [UniProtKB: Q15139]
ChEMBL Inhibition of PRKD1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
protein kinase D2/Serine/threonine-protein kinase D2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4900] [GtoPdb: 2173] [UniProtKB: Q9BZL6]
ChEMBL Inhibition of PRKD2 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
protein kinase D3/Serine/threonine-protein kinase D3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2595] [GtoPdb: 2174] [UniProtKB: O94806]
ChEMBL Inhibition of PRKCN (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
microtubule affinity regulating kinase 1/Serine/threonine-protein kinase MARK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5940] [GtoPdb: 2097] [UniProtKB: Q9P0L2]
ChEMBL Inhibition of MARK1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
microtubule affinity regulating kinase 2/Serine/threonine-protein kinase MARK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3831] [GtoPdb: 2098] [UniProtKB: Q7KZI7]
ChEMBL Inhibition of MARK2 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
CDC42 binding protein kinase alpha/Serine/threonine-protein kinase MRCK alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4516] [GtoPdb: 1507] [UniProtKB: Q5VT25]
ChEMBL Inhibition of CDC42_BPA (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
CDC42 binding protein kinase beta/Serine/threonine-protein kinase MRCK beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5052] [GtoPdb: 1508] [UniProtKB: Q9Y5S2]
ChEMBL Inhibition of CDC42_BPB (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345]
ChEMBL Inhibition of FRAP1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
protein kinase N1/Serine/threonine-protein kinase N1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3384] [GtoPdb: 1520] [UniProtKB: Q16512]
ChEMBL Inhibition of PKN1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
NIMA related kinase 1/Serine/threonine-protein kinase Nek1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5855] [GtoPdb: 2114] [UniProtKB: Q96PY6]
ChEMBL Inhibition of NEK1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
NIMA related kinase 2/Serine/threonine-protein kinase Nek2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3835] [GtoPdb: 2117] [UniProtKB: P51955]
ChEMBL Inhibition of NEK2 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
NIMA related kinase 6/Serine/threonine-protein kinase Nek6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4309] [GtoPdb: 2121] [UniProtKB: Q9HC98]
ChEMBL Inhibition of NEK6 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
NIMA related kinase 9/Serine/threonine-protein kinase Nek9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5257] [GtoPdb: 2124] [UniProtKB: Q8TD19]
ChEMBL Inhibition of NEK9 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
p21 (RAC1) activated kinase 2/Serine/threonine-protein kinase PAK 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4487] [GtoPdb: 2134] [UniProtKB: Q13177]
ChEMBL Inhibition of PAK2 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
p21 (RAC1) activated kinase 3/Serine/threonine-protein kinase PAK 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2999] [GtoPdb: 2135] [UniProtKB: O75914]
ChEMBL Inhibition of PAK3 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
p21 (RAC1) activated kinase 4/Serine/threonine-protein kinase PAK 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4482] [GtoPdb: 2136] [UniProtKB: O96013]
ChEMBL Inhibition of PAK4 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
p21 (RAC1) activated kinase 5/Serine/threonine-protein kinase PAK 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4524] [GtoPdb: 2138] [UniProtKB: Q9P286]
ChEMBL Inhibition of PAK7 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
p21 (RAC1) activated kinase 6/Serine/threonine-protein kinase PAK 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4311] [GtoPdb: 2137] [UniProtKB: Q9NQU5]
ChEMBL Inhibition of PAK6 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309]
ChEMBL Inhibition of PIM1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
Pim-2 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523] [GtoPdb: 2159] [UniProtKB: Q9P1W9]
ChEMBL Inhibition of PIM2 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350]
ChEMBL Inhibition of PLK1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
polo like kinase 2/Serine/threonine-protein kinase PLK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5938] [GtoPdb: 2169] [UniProtKB: Q9NYY3]
ChEMBL Inhibition of PLK2 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
polo like kinase 3/Serine/threonine-protein kinase PLK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4897] [GtoPdb: 2170] [UniProtKB: Q9H4B4]
ChEMBL Inhibition of PLK3 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
serum/glucocorticoid regulated kinase 1/Serine/threonine-protein kinase Sgk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2343] [GtoPdb: 1534] [UniProtKB: O00141]
ChEMBL Inhibition of SGK (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
serum/glucocorticoid regulated kinase 2/Serine/threonine-protein kinase Sgk2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5794] [GtoPdb: 1535] [UniProtKB: Q9HBY8]
ChEMBL Inhibition of SGK2 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
serum/glucocorticoid regulated kinase family member 3/Serine/threonine-protein kinase Sgk3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6186] [GtoPdb: 1536] [UniProtKB: Q96BR1]
ChEMBL Inhibition of SGKL (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
salt inducible kinase 2/Serine/threonine-protein kinase SIK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5699] [GtoPdb: 2198] [UniProtKB: Q9H0K1]
ChEMBL Inhibition of SNF1LK2 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
TANK binding kinase 1/Serine/threonine-protein kinase TBK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5408] [GtoPdb: 2237] [UniProtKB: Q9UHD2]
ChEMBL Inhibition of TBK1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
sphingosine kinase 1/Sphingosine kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4394] [GtoPdb: 2204] [UniProtKB: Q9NYA1]
ChEMBL Inhibition of SPHK1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
SRC kinase signaling inhibitor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2150836] [UniProtKB: Q9C0H9]
ChEMBL Inhibition of SRCN1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
SRSF protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4375] [GtoPdb: 2208] [UniProtKB: Q96SB4]
ChEMBL Inhibition of SRPK1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
SRSF protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5668] [GtoPdb: 2209] [UniProtKB: P78362]
ChEMBL Inhibition of SRPK2 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
testis specific serine kinase 1B/Testis-specific serine/threonine-protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6003] [GtoPdb: 2257] [UniProtKB: Q9BXA7]
ChEMBL Inhibition of STK22D (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
testis specific serine kinase 2/Testis-specific serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6014] [GtoPdb: 2258] [UniProtKB: Q96PF2]
ChEMBL Inhibition of STK22B (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
ChEMBL Inhibition of ABL1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
ABL proto-oncogene 2, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4014] [GtoPdb: 1924] [UniProtKB: P42684]
ChEMBL Inhibition of ABL2 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
BLK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Blk in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2250] [GtoPdb: 1940] [UniProtKB: P51451]
ChEMBL Inhibition of BLK (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187]
ChEMBL Inhibition of BTK (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
C-terminal Src kinase/Tyrosine-protein kinase CSK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2634] [GtoPdb: 1994] [UniProtKB: P41240]
ChEMBL Inhibition of CSK (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
FER tyrosine kinase/Tyrosine-protein kinase Fer in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3982] [GtoPdb: 2022] [UniProtKB: P16591]
ChEMBL Inhibition of FER (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
FES proto-oncogene, tyrosine kinase/Tyrosine-protein kinase Fes/Fps in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5455] [GtoPdb: 2023] [UniProtKB: P07332]
ChEMBL Inhibition of FES (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
FGR proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Fgr in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4454] [GtoPdb: 2024] [UniProtKB: P09769]
ChEMBL Inhibition of FGR (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
fyn related Src family tyrosine kinase/Tyrosine-protein kinase FRK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4223] [GtoPdb: 2025] [UniProtKB: P42685]
ChEMBL Inhibition of FRK (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
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 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
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 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
IL2 inducible T cell kinase/Tyrosine-protein kinase ITK/TSK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2959] [GtoPdb: 2046] [UniProtKB: Q08881]
ChEMBL Inhibition of ITK (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
ChEMBL Inhibition of JAK2 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
ChEMBL Inhibition of JAK3 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lck in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
ChEMBL Inhibition of LCK (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
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_A (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
ChEMBL Inhibition of LYN_B (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
MER proto-oncogene, tyrosine kinase/Tyrosine-protein kinase Mer in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5331] [GtoPdb: 1837] [UniProtKB: Q12866]
ChEMBL Inhibition of MERTK (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
TYRO3 protein tyrosine kinase/Tyrosine-protein kinase receptor TYRO3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5314] [GtoPdb: 1836] [UniProtKB: Q06418]
ChEMBL Inhibition of TYRO3 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530]
ChEMBL Inhibition of AXL (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405]
ChEMBL Inhibition of SYK (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
YES proto-oncogene 1, Src family tyrosine kinase/Tyrosine-protein kinase Yes in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073] [GtoPdb: 2284] [UniProtKB: P07947]
ChEMBL Inhibition of YES1 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
zeta chain of T cell receptor associated protein kinase 70/Tyrosine-protein kinase ZAP-70 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2803] [GtoPdb: 2285] [UniProtKB: P43403]
ChEMBL Inhibition of ZAP70 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
ChEMBL Selectivity interaction (SelectScreen (Invitrogen, enzymatic assay with 100 µM ATP)) EUB0000697a KDR B 5.96 pIC50 1100 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of KDR (unknown origin) B 5.96 pIC50 1100 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]
fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916]
ChEMBL Inhibition of FLT4 (unknown origin) B 6 pIC50 >1000 nM IC50 Nat Commun (2019) 10: 3758-3758 [PMID:31434879]

ChEMBL data shown on this page come from version 36:

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]