baricitinib [Ligand Id: 7792] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2105759 (Baricitinib, Baricitinib phosphate, Baricitinib phosphate salt, INCB-028050, INCB028050, Incb-28050, LY-3009104, LY3009104, Olumiant)
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  • protein kinase AMP-activated catalytic subunit alpha 1/5`-AMP-activated protein kinase catalytic subunit alpha-1 in Human [ChEMBL: CHEMBL4045] [GtoPdb: 1541] [UniProtKB: Q13131]
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  • protein kinase AMP-activated non-catalytic subunit gamma 1/5`-AMP-activated protein kinase subunit gamma-1 in Human [ChEMBL: CHEMBL2393] [GtoPdb: 1545] [UniProtKB: P54619]
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  • protein kinase AMP-activated non-catalytic subunit gamma 2/5`-AMP-activated protein kinase subunit gamma-2 in Human [ChEMBL: CHEMBL2453] [GtoPdb: 1546] [UniProtKB: Q9UGJ0]
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  • aarF domain containing kinase 1/AarF domain-containing protein kinase 1 in Human [ChEMBL: CHEMBL4105885] [GtoPdb: 1925] [UniProtKB: Q86TW2]
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  • tyrosine kinase non receptor 2/Activated CDC42 kinase 1 in Human [ChEMBL: CHEMBL4599] [GtoPdb: 2246] [UniProtKB: Q07912]
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  • activin A receptor type 1/Activin receptor type-1 in Human [ChEMBL: CHEMBL5903] [GtoPdb: 1785] [UniProtKB: Q04771]
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  • activin A receptor type 1B/Activin receptor type-1B in Human [ChEMBL: CHEMBL5310] [GtoPdb: 1787] [UniProtKB: P36896]
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  • activin A receptor type IL/Activin receptor type-1-like in Human [ChEMBL: CHEMBL5311] [GtoPdb: 1784] [UniProtKB: P37023]
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  • activin A receptor type 2B/Activin receptor type-2B in Human [ChEMBL: CHEMBL5466] [GtoPdb: 1792] [UniProtKB: Q13705]
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  • Adenylate kinase 2, mitochondrial in Human [ChEMBL: CHEMBL4938] [UniProtKB: P54819]
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  • Mitochondrial adenine nucleotide translocator 2/ADP/ATP translocase 2 in Human [ChEMBL: CHEMBL3709670] [GtoPdb: 1063] [UniProtKB: P05141]
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  • Mitochondrial adenine nucleotide translocator 3/ADP/ATP translocase 3 in Human [ChEMBL: CHEMBL4105854] [GtoPdb: 1064] [UniProtKB: P12236]
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  • AP2 associated kinase 1/AP2-associated protein kinase 1 in Human [ChEMBL: CHEMBL3830] [GtoPdb: 1921] [UniProtKB: Q2M2I8]
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  • ATP-dependent 6-phosphofructokinase, platelet type in Human [ChEMBL: CHEMBL2972] [UniProtKB: Q01813]
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  • ATP-dependent RNA helicase DDX3X in Human [ChEMBL: CHEMBL5553] [UniProtKB: O00571]
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  • coenzyme Q8A/Atypical kinase COQ8A, mitochondrial in Human [ChEMBL: CHEMBL5550] [GtoPdb: 1927] [UniProtKB: Q8NI60]
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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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  • Bifunctional phosphoribosylaminoimidazole carboxylase/phosphoribosylaminoimidazole succinocarboxamide synthetase in Human [ChEMBL: CHEMBL5922] [UniProtKB: P22234]
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  • BMP2 inducible kinase/BMP-2-inducible protein kinase in Human [ChEMBL: CHEMBL4522] [GtoPdb: 1941] [UniProtKB: Q9NSY1]
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  • bone morphogenetic protein receptor type IA/Bone morphogenetic protein receptor type-1A in Human [ChEMBL: CHEMBL5275] [GtoPdb: 1786] [UniProtKB: P36894]
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  • bone morphogenetic protein receptor type IB/Bone morphogenetic protein receptor type-1B in Human [ChEMBL: CHEMBL5476] [GtoPdb: 1789] [UniProtKB: O00238]
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  • bone morphogenetic protein receptor type 2/Bone morphogenetic protein receptor type-2 in Human [ChEMBL: CHEMBL5467] [GtoPdb: 1794] [UniProtKB: Q13873]
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  • BCR activator of RhoGEF and GTPase/Breakpoint cluster region protein in Human [ChEMBL: CHEMBL5146] [GtoPdb: 2755] [UniProtKB: P11274]
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  • calcium/calmodulin dependent protein kinase kinase 2/Calcium/calmodulin-dependent protein kinase kinase 2 in Human [ChEMBL: CHEMBL5284] [GtoPdb: 1957] [UniProtKB: Q96RR4]
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  • calcium/calmodulin dependent protein kinase IG/Calcium/calmodulin-dependent protein kinase type 1G in Human [ChEMBL: CHEMBL5258] [GtoPdb: 1954] [UniProtKB: Q96NX5]
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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 II gamma subunit/Calcium/calmodulin-dependent protein kinase type II subunit gamma in Human [ChEMBL: CHEMBL3829] [GtoPdb: 1557] [UniProtKB: Q13555]
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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, cAMP-dependent, catalytic, beta subunit/cAMP-dependent protein kinase catalytic subunit beta in Human [ChEMBL: CHEMBL2918] [GtoPdb: 1477] [UniProtKB: P22694]
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  • protein kinase, cAMP-dependent, catalytic, gamma subunit/cAMP-dependent protein kinase catalytic subunit gamma in Human [ChEMBL: CHEMBL2743] [GtoPdb: 1478] [UniProtKB: P22612]
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  • protein kinase, cAMP-dependent, regulatory, type II, alpha subunit/cAMP-dependent protein kinase type II-alpha regulatory subunit in Human [ChEMBL: CHEMBL2221] [GtoPdb: 1474] [UniProtKB: P13861]
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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 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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  • Chromodomain-helicase-DNA-binding protein 4 in Human [ChEMBL: CHEMBL4105742] [UniProtKB: Q14839]
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  • citron rho-interacting serine/threonine kinase/Citron Rho-interacting kinase in Human [ChEMBL: CHEMBL5579] [GtoPdb: 1509] [UniProtKB: O14578]
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  • cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493]
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  • cyclin dependent kinase 12/Cyclin-dependent kinase 12 in Human [ChEMBL: CHEMBL3559692] [GtoPdb: 1965] [UniProtKB: Q9NYV4]
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  • cyclin dependent kinase 13/Cyclin-dependent kinase 13 in Human [ChEMBL: CHEMBL1795192] [GtoPdb: 1966] [UniProtKB: Q14004]
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  • cyclin dependent kinase 16/Cyclin-dependent kinase 16 in Human [ChEMBL: CHEMBL4597] [GtoPdb: 1969] [UniProtKB: Q00536]
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  • cyclin dependent kinase 17/Cyclin-dependent kinase 17 in Human [ChEMBL: CHEMBL5790] [GtoPdb: 1970] [UniProtKB: Q00537]
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  • cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
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  • cyclin dependent kinase 3/Cyclin-dependent kinase 3 in Human [ChEMBL: CHEMBL4442] [GtoPdb: 1975] [UniProtKB: Q00526]
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  • cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802]
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  • cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535]
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  • cyclin dependent kinase 6/Cyclin-dependent kinase 6 in Human [ChEMBL: CHEMBL2508] [GtoPdb: 1978] [UniProtKB: Q00534]
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  • cyclin dependent kinase 7/Cyclin-dependent kinase 7 in Human [ChEMBL: CHEMBL3055] [GtoPdb: 1979] [UniProtKB: P50613]
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  • cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750]
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  • cyclin G associated kinase/Cyclin-G-associated kinase in Human [ChEMBL: CHEMBL4355] [GtoPdb: 2027] [UniProtKB: O14976]
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  • Cytochrome c1, heme protein, mitochondrial in Human [ChEMBL: CHEMBL4105975] [UniProtKB: P08574]
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  • discoidin domain receptor tyrosine kinase 2/Discoidin domain-containing receptor 2 in Human [ChEMBL: CHEMBL5122] [GtoPdb: 1844] [UniProtKB: Q16832]
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  • DNA topoisomerase II alpha/DNA topoisomerase 2-alpha in Human [ChEMBL: CHEMBL1806] [GtoPdb: 2637] [UniProtKB: P11388]
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  • mitogen-activated protein kinase kinase 1/Dual specificity mitogen-activated protein kinase kinase 1 in Human [ChEMBL: CHEMBL3587] [GtoPdb: 2062] [UniProtKB: Q02750]
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  • mitogen-activated protein kinase kinase 2/Dual specificity mitogen-activated protein kinase kinase 2 in Human [ChEMBL: CHEMBL2964] [GtoPdb: 2063] [UniProtKB: P36507]
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  • mitogen-activated protein kinase kinase 3/Dual specificity mitogen-activated protein kinase kinase 3 in Human [ChEMBL: CHEMBL2109] [GtoPdb: 2064] [UniProtKB: P46734]
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  • mitogen-activated protein kinase kinase 5/Dual specificity mitogen-activated protein kinase kinase 5 in Human [ChEMBL: CHEMBL4948] [GtoPdb: 2066] [UniProtKB: Q13163]
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  • mitogen-activated protein kinase kinase 6/Dual specificity mitogen-activated protein kinase kinase 6 in Human [ChEMBL: CHEMBL2171] [GtoPdb: 2067] [UniProtKB: P52564]
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  • CDC like kinase 1/Dual specificity protein kinase CLK1 in Human [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759]
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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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  • CDC like kinase 3/Dual specificity protein kinase CLK3 in Human [ChEMBL: CHEMBL4226] [GtoPdb: 1992] [UniProtKB: P49761]
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  • CDC like kinase 4/Dual specificity protein kinase CLK4 in Human [ChEMBL: CHEMBL4203] [GtoPdb: 1993] [UniProtKB: Q9HAZ1]
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  • testis associated actin remodelling kinase 1/Dual specificity testis-specific protein kinase 1 in Human [ChEMBL: CHEMBL5604] [GtoPdb: 2239] [UniProtKB: Q15569]
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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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  • TP53 regulating kinase/EKC/KEOPS complex subunit TP53RK in Human [ChEMBL: CHEMBL1938223] [GtoPdb: 2248] [UniProtKB: Q96S44]
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  • Electron transfer flavoprotein subunit beta in Human [ChEMBL: CHEMBL4105744] [UniProtKB: P38117]
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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 A4/Ephrin type-A receptor 4 in Human [ChEMBL: CHEMBL3988] [GtoPdb: 1824] [UniProtKB: P54764]
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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 A7/Ephrin type-A receptor 7 in Human [ChEMBL: CHEMBL4602] [GtoPdb: 1827] [UniProtKB: Q15375]
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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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  • EPH receptor B6/Ephrin type-B receptor 6 in Human [ChEMBL: CHEMBL5836] [GtoPdb: 1834] [UniProtKB: O15197]
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  • epidermal growth factor receptor/Epidermal growth factor receptor in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • discoidin domain receptor tyrosine kinase 1/Epithelial discoidin domain-containing receptor 1 in Human [ChEMBL: CHEMBL5319] [GtoPdb: 1843] [UniProtKB: Q08345]
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  • Eukaryotic peptide chain release factor GTP-binding subunit ERF3B in Human [ChEMBL: CHEMBL4105974] [UniProtKB: Q8IYD1]
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  • eukaryotic translation initiation factor 2 alpha kinase 1/Eukaryotic translation initiation factor 2-alpha kinase 1 in Human [ChEMBL: CHEMBL6029] [GtoPdb: 2015] [UniProtKB: Q9BQI3]
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  • Eukaryotic translation initiation factor 5B in Human [ChEMBL: CHEMBL4105852] [UniProtKB: O60841]
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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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  • protein tyrosine kinase 2/Focal adhesion kinase 1 in Human [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397]
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  • General transcription and DNA repair factor IIH helicase subunit XPD in Human [ChEMBL: CHEMBL4105743] [UniProtKB: P18074]
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  • Glycogen phosphorylase, brain form in Human [ChEMBL: CHEMBL3856] [UniProtKB: P11216]
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  • Glycogen phosphorylase, liver form in Human [ChEMBL: CHEMBL2568] [UniProtKB: P06737]
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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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  • G protein-coupled receptor kinase 6 in Human [ChEMBL: CHEMBL6144] [GtoPdb: 1470] [UniProtKB: P43250]
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  • Guanine nucleotide-binding protein G(i) subunit alpha-2 in Human [ChEMBL: CHEMBL4105887] [UniProtKB: P04899]
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  • Haem oxygenase 2/Heme oxygenase 2 in Human [ChEMBL: CHEMBL2546] [GtoPdb: 1442] [UniProtKB: P30519]
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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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  • 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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  • inosine monophosphate dehydrogenase 2/Inosine-5`-monophosphate dehydrogenase 2 in Human [ChEMBL: CHEMBL2002] [GtoPdb: 2625] [UniProtKB: P12268]
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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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  • integrin linked kinase/Integrin-linked protein kinase in Human [ChEMBL: CHEMBL5247] [GtoPdb: 2041] [UniProtKB: Q13418]
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  • interleukin 1 receptor associated kinase 1/Interleukin-1 receptor-associated kinase 1 in Human [ChEMBL: CHEMBL3357] [GtoPdb: 2042] [UniProtKB: P51617]
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  • interleukin 1 receptor associated kinase 3/Interleukin-1 receptor-associated kinase 3 in Human [ChEMBL: CHEMBL5081] [GtoPdb: 2044] [UniProtKB: Q9Y616]
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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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  • 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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  • maternal embryonic leucine zipper kinase/Maternal embryonic leucine zipper kinase in Human [ChEMBL: CHEMBL4578] [GtoPdb: 2102] [UniProtKB: Q14680]
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  • Membrane-associated progesterone receptor component 1 in Human [ChEMBL: CHEMBL4105706] [UniProtKB: O00264]
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  • protein kinase, membrane associated tyrosine/threonine 1/Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase in Human [ChEMBL: CHEMBL3984] [GtoPdb: 2167] [UniProtKB: Q99640]
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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 10/Mitogen-activated protein kinase 10 in Human [ChEMBL: CHEMBL2637] [GtoPdb: 1498] [UniProtKB: P53779]
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  • mitogen-activated protein kinase 11/Mitogen-activated protein kinase 11 in Human [ChEMBL: CHEMBL3961] [GtoPdb: 1500] [UniProtKB: Q15759]
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  • mitogen-activated protein kinase 14/Mitogen-activated protein kinase 14 in Human [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
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  • mitogen-activated protein kinase 15/Mitogen-activated protein kinase 15 in Human [ChEMBL: CHEMBL5198] [GtoPdb: 2090] [UniProtKB: Q8TD08]
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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 7/Mitogen-activated protein kinase 7 in Human [ChEMBL: CHEMBL5332] [GtoPdb: 2093] [UniProtKB: Q13164]
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  • mitogen-activated protein kinase 8/Mitogen-activated protein kinase 8 in Human [ChEMBL: CHEMBL2276] [GtoPdb: 1496] [UniProtKB: P45983]
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  • mitogen-activated protein kinase 9/Mitogen-activated protein kinase 9 in Human [ChEMBL: CHEMBL4179] [GtoPdb: 1497] [UniProtKB: P45984]
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  • mitogen-activated protein kinase kinase kinase 1/Mitogen-activated protein kinase kinase kinase 1 in Human [ChEMBL: CHEMBL3956] [GtoPdb: 2069] [UniProtKB: Q13233]
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  • mitogen-activated protein kinase kinase kinase 11/Mitogen-activated protein kinase kinase kinase 11 in Human [ChEMBL: CHEMBL2708] [GtoPdb: 2071] [UniProtKB: Q16584]
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  • mitogen-activated protein kinase kinase kinase 2/Mitogen-activated protein kinase kinase kinase 2 in Human [ChEMBL: CHEMBL5914] [GtoPdb: 2077] [UniProtKB: Q9Y2U5]
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  • ZAK sterile alpha motif and leucine zipper containing kinase AZK/Mitogen-activated protein kinase kinase kinase 20 in Human [ChEMBL: CHEMBL3886] [GtoPdb: 2289] [UniProtKB: Q9NYL2]
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  • mitogen-activated protein kinase kinase kinase 3/Mitogen-activated protein kinase kinase kinase 3 in Human [ChEMBL: CHEMBL5970] [GtoPdb: 2078] [UniProtKB: Q99759]
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  • mitogen-activated protein kinase kinase kinase 4/Mitogen-activated protein kinase kinase kinase 4 in Human [ChEMBL: CHEMBL4853] [GtoPdb: 2079] [UniProtKB: Q9Y6R4]
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  • mitogen-activated protein kinase kinase kinase 5/Mitogen-activated protein kinase kinase kinase 5 in Human [ChEMBL: CHEMBL5285] [GtoPdb: 2080] [UniProtKB: Q99683]
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  • mitogen-activated protein kinase kinase kinase 6/Mitogen-activated protein kinase kinase kinase 6 in Human [ChEMBL: CHEMBL1163123] [GtoPdb: 2081] [UniProtKB: O95382]
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  • mitogen-activated protein kinase kinase kinase kinase 1/Mitogen-activated protein kinase kinase kinase kinase 1 in Human [ChEMBL: CHEMBL5749] [GtoPdb: 2085] [UniProtKB: Q92918]
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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 3/Mitogen-activated protein kinase kinase kinase kinase 3 in Human [ChEMBL: CHEMBL5432] [GtoPdb: 2087] [UniProtKB: Q8IVH8]
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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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There should be some charts here, you may need to enable JavaScript!
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  • myosin light chain kinase 3/Myosin light chain kinase in Human [ChEMBL: CHEMBL4627] [GtoPdb: 2110] [UniProtKB: Q32MK0]
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  • myosin light chain kinase/Myosin light chain kinase, smooth muscle in Human [ChEMBL: CHEMBL2428] [GtoPdb: 1552] [UniProtKB: Q15746]
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  • NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 13 in Human [ChEMBL: CHEMBL4105781] [UniProtKB: Q9P0J0]
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  • tyrosine kinase non receptor 1/Non-receptor tyrosine-protein kinase TNK1 in Human [ChEMBL: CHEMBL5334] [GtoPdb: 2245] [UniProtKB: Q13470]
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  • tyrosine kinase 2/Non-receptor tyrosine-protein kinase TYK2 in Human [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597]
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  • NUAK family, SNF1-like kinase, 2/NUAK family SNF1-like kinase 2 in Human [ChEMBL: CHEMBL5698] [GtoPdb: 2130] [UniProtKB: Q9H093]
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  • PAS domain containing serine/threonine kinase/PAS domain-containing serine/threonine-protein kinase in Human [ChEMBL: CHEMBL6054] [GtoPdb: 2139] [UniProtKB: Q96RG2]
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There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
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  • Phosphatidylethanolamine-binding protein 1 in Human [ChEMBL: CHEMBL4105856] [UniProtKB: P30086]
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  • phosphatidylinositol-5-phosphate 4-kinase type 2 gamma/Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma in Human [ChEMBL: CHEMBL1770034] [GtoPdb: 2163] [UniProtKB: Q8TBX8]
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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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  • platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619]
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  • Probable ATP-dependent RNA helicase DDX6 in Human [ChEMBL: CHEMBL4105783] [UniProtKB: P26196]
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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 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 tyrosine kinase 2 beta/Protein-tyrosine kinase 2-beta in Human [ChEMBL: CHEMBL5469] [GtoPdb: 2181] [UniProtKB: Q14289]
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  • protein tyrosine kinase 6/Protein-tyrosine kinase 6 in Human [ChEMBL: CHEMBL4601] [GtoPdb: 2182] [UniProtKB: Q13882]
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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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  • Putative heat shock protein HSP 90-beta 2 in Human [ChEMBL: CHEMBL4105858] [UniProtKB: Q58FF8]
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There should be some charts here, you may need to enable JavaScript!
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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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There should be some charts here, you may need to enable JavaScript!
  • RAB27A, member RAS oncogene family/Ras-related protein Rab-27A in Human [ChEMBL: CHEMBL4105702] [GtoPdb: 2916] [UniProtKB: P51159]
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There should be some charts here, you may need to enable JavaScript!
  • receptor interacting serine/threonine kinase 2/Receptor-interacting serine/threonine-protein kinase 2 in Human [ChEMBL: CHEMBL5014] [GtoPdb: 2190] [UniProtKB: O43353]
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  • receptor interacting serine/threonine kinase 3/Receptor-interacting serine/threonine-protein kinase 3 in Human [ChEMBL: CHEMBL1795199] [GtoPdb: 2191] [UniProtKB: Q9Y572]
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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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  • 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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  • 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 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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  • Ribosyldihydronicotinamide dehydrogenase [quinone] in Human [ChEMBL: CHEMBL3959] [UniProtKB: P16083]
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There should be some charts here, you may need to enable JavaScript!
  • S-adenosylmethionine synthase isoform type-2 in Human [ChEMBL: CHEMBL3313835] [UniProtKB: P31153]
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There should be some charts here, you may need to enable JavaScript!
  • serine/threonine kinase 10/Serine/threonine-protein kinase 10 in Human [ChEMBL: CHEMBL3981] [GtoPdb: 2211] [UniProtKB: O94804]
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  • serine/threonine kinase 16/Serine/threonine-protein kinase 16 in Human [ChEMBL: CHEMBL3938] [GtoPdb: 2213] [UniProtKB: O75716]
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  • serine/threonine kinase 24/Serine/threonine-protein kinase 24 in Human [ChEMBL: CHEMBL5082] [GtoPdb: 2217] [UniProtKB: Q9Y6E0]
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  • serine/threonine-protein kinase MST4/Serine/threonine-protein kinase 26 in Human [ChEMBL: CHEMBL5941] [GtoPdb: 2287] [UniProtKB: Q9P289]
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  • serine/threonine kinase 3/Serine/threonine-protein kinase 3 in Human [ChEMBL: CHEMBL4708] [GtoPdb: 2219] [UniProtKB: Q13188]
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  • Serine/threonine kinase 38 like/Serine/threonine-protein kinase 38-like in Human [ChEMBL: CHEMBL4851] [GtoPdb: 1518] [UniProtKB: Q9Y2H1]
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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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  • A-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase A-Raf in Human [ChEMBL: CHEMBL1169596] [GtoPdb: 1933] [UniProtKB: P10398]
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  • ATR checkpoint kinase/Serine/threonine-protein kinase ATR in Human [ChEMBL: CHEMBL5024] [GtoPdb: 1935] [UniProtKB: Q13535]
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  • B-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase B-raf in Human [ChEMBL: CHEMBL5145] [GtoPdb: 1943] [UniProtKB: P15056]
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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 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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  • endoplasmic reticulum to nucleus signaling 1/Serine/threonine-protein kinase/endoribonuclease IRE1 in Human [ChEMBL: CHEMBL1163101] [GtoPdb: 2020] [UniProtKB: O75460]
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  • endoplasmic reticulum to nucleus signaling 2/Serine/threonine-protein kinase/endoribonuclease IRE2 in Human [ChEMBL: CHEMBL4105932] [GtoPdb: 2021] [UniProtKB: Q76MJ5]
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  • ciliogenesis associated kinase 1/Serine/threonine-protein kinase ICK in Human [ChEMBL: CHEMBL1163126] [GtoPdb: 2038] [UniProtKB: Q9UPZ9]
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  • large tumor suppressor kinase 1/Serine/threonine-protein kinase LATS1 in Human [ChEMBL: CHEMBL6167] [GtoPdb: 1515] [UniProtKB: O95835]
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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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  • CDC42 binding protein kinase gamma/Serine/threonine-protein kinase MRCK gamma in Human [ChEMBL: CHEMBL5615] [GtoPdb: 1506] [UniProtKB: Q6DT37]
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  • protein kinase N1/Serine/threonine-protein kinase N1 in Human [ChEMBL: CHEMBL3384] [GtoPdb: 1520] [UniProtKB: Q16512]
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  • protein kinase N2/Serine/threonine-protein kinase N2 in Human [ChEMBL: CHEMBL3032] [GtoPdb: 1521] [UniProtKB: Q16513]
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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 3/Serine/threonine-protein kinase Nek3 in Human [ChEMBL: CHEMBL5679] [GtoPdb: 2118] [UniProtKB: P51956]
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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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  • nemo like kinase/Serine/threonine-protein kinase NLK in Human [ChEMBL: CHEMBL5364] [GtoPdb: 2125] [UniProtKB: Q9UBE8]
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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 4/Serine/threonine-protein kinase PAK 4 in Human [ChEMBL: CHEMBL4482] [GtoPdb: 2136] [UniProtKB: O96013]
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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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  • polo like kinase 4/Serine/threonine-protein kinase PLK4 in Human [ChEMBL: CHEMBL3788] [GtoPdb: 2171] [UniProtKB: O00444]
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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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  • SIK family kinase 3/Serine/threonine-protein kinase SIK3 in Human [ChEMBL: CHEMBL6149] [GtoPdb: 2199] [UniProtKB: Q9Y2K2]
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  • serine/threonine kinase 11/Serine/threonine-protein kinase STK11 in Human [ChEMBL: CHEMBL5606] [GtoPdb: 2212] [UniProtKB: Q15831]
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  • TAO kinase 1/Serine/threonine-protein kinase TAO1 in Human [ChEMBL: CHEMBL5261] [GtoPdb: 2233] [UniProtKB: Q7L7X3]
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  • TAO kinase 2/Serine/threonine-protein kinase TAO2 in Human [ChEMBL: CHEMBL1075195] [GtoPdb: 2234] [UniProtKB: Q9UL54]
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  • TAO kinase 3/Serine/threonine-protein kinase TAO3 in Human [ChEMBL: CHEMBL5701] [GtoPdb: 2235] [UniProtKB: Q9H2K8]
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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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  • unc-51 like autophagy activating kinase 1/Serine/threonine-protein kinase ULK1 in Human [ChEMBL: CHEMBL6006] [GtoPdb: 2271] [UniProtKB: O75385]
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  • unc-51 like kinase 3/Serine/threonine-protein kinase ULK3 in Human [ChEMBL: CHEMBL5047] [GtoPdb: 2273] [UniProtKB: Q6PHR2]
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  • Signal recognition particle receptor subunit alpha in Human [ChEMBL: CHEMBL4105934] [UniProtKB: P08240]
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  • signal transducer and activator of transcription 3/Signal transducer and activator of transcription 3 in Human [ChEMBL: CHEMBL4026] [GtoPdb: 2994] [UniProtKB: P40763]
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  • STE20 like kinase/STE20-like serine/threonine-protein kinase in Human [ChEMBL: CHEMBL4202] [GtoPdb: 2200] [UniProtKB: Q9H2G2]
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  • STE20 related adaptor alpha/STE20-related kinase adapter protein alpha in Human [ChEMBL: CHEMBL1795198] [GtoPdb: 2227] [UniProtKB: Q7RTN6]
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  • Structural maintenance of chromosomes protein 1A in Human [ChEMBL: CHEMBL4105747] [UniProtKB: Q14683]
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  • Structural maintenance of chromosomes protein 2 in Human [ChEMBL: CHEMBL4105890] [UniProtKB: O95347]
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  • Succinate--CoA ligase [ADP-forming] subunit beta, mitochondrial in Human [ChEMBL: CHEMBL4105973] [UniProtKB: Q9P2R7]
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  • transforming growth factor beta receptor 1/TGF-beta receptor type-1 in Human [ChEMBL: CHEMBL4439] [GtoPdb: 1788] [UniProtKB: P36897]
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  • transforming growth factor beta receptor 2/TGF-beta receptor type-2 in Human [ChEMBL: CHEMBL4267] [GtoPdb: 1795] [UniProtKB: P37173]
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  • Thyroid hormone receptor-associated protein 3 in Human [ChEMBL: CHEMBL4105820] [UniProtKB: Q9Y2W1]
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  • TRAF2 and NCK interacting kinase/TRAF2 and NCK-interacting protein kinase in Human [ChEMBL: CHEMBL4527] [GtoPdb: 2244] [UniProtKB: Q9UKE5]
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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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  • 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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  • 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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  • Janus kinase 1/Tyrosine-protein kinase JAK1 in Human [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458]
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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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  • spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405]
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  • tec protein tyrosine kinase/Tyrosine-protein kinase Tec in Human [ChEMBL: CHEMBL4246] [GtoPdb: 2238] [UniProtKB: P42680]
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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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  • Tyrosine--tRNA ligase, cytoplasmic in Human [ChEMBL: CHEMBL3179] [UniProtKB: P54577]
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  • U5 small nuclear ribonucleoprotein 200 kDa helicase in Human [ChEMBL: CHEMBL4105972] [UniProtKB: O75643]
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  • aarF domain containing kinase 5/Uncharacterized aarF domain-containing protein kinase 5 in Human [ChEMBL: CHEMBL4105886] [GtoPdb: 1929] [UniProtKB: Q3MIX3]
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  • Very long-chain specific acyl-CoA dehydrogenase, mitochondrial in Human [ChEMBL: CHEMBL4105892] [UniProtKB: P49748]
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  • WEE1 G2 checkpoint kinase/Wee1-like protein kinase in Human [ChEMBL: CHEMBL5491] [GtoPdb: 2278] [UniProtKB: P30291]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
26S proteasome regulatory subunit 6B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3831205] [UniProtKB: P43686]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
protein kinase AMP-activated catalytic subunit alpha 1/5`-AMP-activated protein kinase catalytic subunit alpha-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4045] [GtoPdb: 1541] [UniProtKB: Q13131]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
protein kinase AMP-activated non-catalytic subunit gamma 1/5`-AMP-activated protein kinase subunit gamma-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2393] [GtoPdb: 1545] [UniProtKB: P54619]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
protein kinase AMP-activated non-catalytic subunit gamma 2/5`-AMP-activated protein kinase subunit gamma-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2453] [GtoPdb: 1546] [UniProtKB: Q9UGJ0]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
aarF domain containing kinase 1/AarF domain-containing protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105885] [GtoPdb: 1925] [UniProtKB: Q86TW2]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Actin-related protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6090] [UniProtKB: P61160]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Actin-related protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105857] [UniProtKB: P61158]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
tyrosine kinase non receptor 2/Activated CDC42 kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4599] [GtoPdb: 2246] [UniProtKB: Q07912]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
activin A receptor type 1/Activin receptor type-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5903] [GtoPdb: 1785] [UniProtKB: Q04771]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
activin A receptor type 1B/Activin receptor type-1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5310] [GtoPdb: 1787] [UniProtKB: P36896]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
activin A receptor type IL/Activin receptor type-1-like in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5311] [GtoPdb: 1784] [UniProtKB: P37023]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
activin A receptor type 2B/Activin receptor type-2B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5466] [GtoPdb: 1792] [UniProtKB: Q13705]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Acyl-CoA dehydrogenase family member 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105816] [UniProtKB: Q6JQN1]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Acyl-CoA dehydrogenase family member 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105707] [UniProtKB: Q709F0]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Adenine phosphoribosyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105819] [UniProtKB: P07741]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Adenosine kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3589] [GtoPdb: 1231] [UniProtKB: P55263]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Adenylate kinase 2, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4938] [UniProtKB: P54819]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Mitochondrial adenine nucleotide translocator 2/ADP/ATP translocase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3709670] [GtoPdb: 1063] [UniProtKB: P05141]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Mitochondrial adenine nucleotide translocator 3/ADP/ATP translocase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105854] [GtoPdb: 1064] [UniProtKB: P12236]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
AP2 associated kinase 1/AP2-associated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3830] [GtoPdb: 1921] [UniProtKB: Q2M2I8]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 7.34 pKd 46 nM Kd Science (2017) 358: null-null [PMID:29191878]
GtoPdb Binding affinity determined in a cell-free biochemical assay. - 7.77 pKd 17 nM Kd Lancet Infect Dis (2020) 20: 400-402 [PMID:32113509]
ChEMBL Binding affinity to AAK1 (unknown origin) B 8.09 pKd 8.2 nM Kd J Med Chem (2021) 64: 11090-11128 [PMID:34270254]
ChEMBL Binding affinity to AAK1 (unknown origin) B 8.09 pKd 8.2 nM Kd J Med Chem (2022) 65: 893-921 [PMID:33539089]
ChEMBL Binding affinity to AAK1 (unknown origin) assessed as dissociation constant B 8.09 pKd 8.2 nM Kd J Med Chem (2022) 65: 893-921 [PMID:33539089]
ChEMBL Binding affinity to AAK1 (unknown origin) assessed as dissociation constant B 8.09 pKd 8.2 nM Kd J Med Chem (2022) 65: 935-954 [PMID:33970631]
ChEMBL Binding affinity to AAK1 (unknown origin) B 8.09 pKd 8.2 nM Kd J Med Chem (2022) 65: 4121-4155 [PMID:35171586]
ChEMBL Binding affinity of AAK1 (unknown origin) assessed as dissociation constant B 8.09 pKd 8.2 nM Kd Eur J Med Chem (2023) 248: 115102-115102 [PMID:36640459]
ChEMBL Binding affinity to AAK1 (unknown origin) assessed as dissociation constant B 8.09 pKd 8.2 nM Kd Eur J Med Chem (2024) 263: 115923-115923 [PMID:37981443]
ChEMBL Inhibition of AAK1 (unknown origin) B 7.77 pIC50 17 nM IC50 J Med Chem (2022) 65: 893-921 [PMID:33539089]
ATP-dependent 6-phosphofructokinase, platelet type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2972] [UniProtKB: Q01813]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
ATP-dependent RNA helicase DDX1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2010634] [UniProtKB: Q92499]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
ATP-dependent RNA helicase DDX3X in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5553] [UniProtKB: O00571]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
ATP-dependent RNA helicase DDX42 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105782] [UniProtKB: Q86XP3]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
ATP-dependent RNA helicase DHX30 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105814] [UniProtKB: Q7L2E3]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
coenzyme Q8A/Atypical kinase COQ8A, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5550] [GtoPdb: 1927] [UniProtKB: Q8NI60]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
aurora kinase A/Aurora kinase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
aurora kinase B/Aurora kinase B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
beta adrenergic receptor kinase 1/Beta-adrenergic receptor kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4079] [GtoPdb: 1466] [UniProtKB: P25098]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Bifunctional phosphoribosylaminoimidazole carboxylase/phosphoribosylaminoimidazole succinocarboxamide synthetase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5922] [UniProtKB: P22234]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
BMP2 inducible kinase/BMP-2-inducible protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4522] [GtoPdb: 1941] [UniProtKB: Q9NSY1]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 6.67 pKd 216 nM Kd Science (2017) 358: null-null [PMID:29191878]
GtoPdb Binding affinity determined in a cell-free biochemical assay. - 7.4 pKd 40 nM Kd Lancet Infect Dis (2020) 20: 400-402 [PMID:32113509]
ChEMBL Binding affinity to BIKE (unknown origin) B 7.7 pKd 20 nM Kd J Med Chem (2021) 64: 11090-11128 [PMID:34270254]
ChEMBL Binding affinity to BIKE (unknown origin) B 7.7 pKd 20 nM Kd J Med Chem (2022) 65: 4121-4155 [PMID:35171586]
bone morphogenetic protein receptor type IA/Bone morphogenetic protein receptor type-1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5275] [GtoPdb: 1786] [UniProtKB: P36894]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
bone morphogenetic protein receptor type IB/Bone morphogenetic protein receptor type-1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5476] [GtoPdb: 1789] [UniProtKB: O00238]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
bone morphogenetic protein receptor type 2/Bone morphogenetic protein receptor type-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5467] [GtoPdb: 1794] [UniProtKB: Q13873]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
BCR activator of RhoGEF and GTPase/Breakpoint cluster region protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5146] [GtoPdb: 2755] [UniProtKB: P11274]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
calcium/calmodulin dependent protein kinase kinase 2/Calcium/calmodulin-dependent protein kinase kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5284] [GtoPdb: 1957] [UniProtKB: Q96RR4]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
calcium/calmodulin dependent protein kinase IG/Calcium/calmodulin-dependent protein kinase type 1G in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5258] [GtoPdb: 1954] [UniProtKB: Q96NX5]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
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 Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 6.51 pKd 312 nM Kd Science (2017) 358: null-null [PMID:29191878]
calcium/calmodulin-dependent protein kinase II gamma subunit/Calcium/calmodulin-dependent protein kinase type II subunit gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3829] [GtoPdb: 1557] [UniProtKB: Q13555]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 6.61 pKd 243 nM Kd Science (2017) 358: null-null [PMID:29191878]
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 Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
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 Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 5.44 pKd 3597 nM Kd Science (2017) 358: null-null [PMID:29191878]
protein kinase, cAMP-dependent, catalytic, beta subunit/cAMP-dependent protein kinase catalytic subunit beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2918] [GtoPdb: 1477] [UniProtKB: P22694]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
protein kinase, cAMP-dependent, catalytic, gamma subunit/cAMP-dependent protein kinase catalytic subunit gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2743] [GtoPdb: 1478] [UniProtKB: P22612]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
protein kinase, cAMP-dependent, regulatory, type II, alpha subunit/cAMP-dependent protein kinase type II-alpha regulatory subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2221] [GtoPdb: 1474] [UniProtKB: P13861]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
casein kinase 1 alpha 1/Casein kinase I isoform alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2793] [GtoPdb: 1995] [UniProtKB: P48729]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
casein kinase 1 delta/Casein kinase I isoform delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
casein kinase 1 epsilon/Casein kinase I isoform epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
casein kinase 1 gamma 1/Casein kinase I isoform gamma-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2426] [GtoPdb: 1999] [UniProtKB: Q9HCP0]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 5.76 pKd 1753 nM Kd Science (2017) 358: null-null [PMID:29191878]
casein kinase 1 gamma 2/Casein kinase I isoform gamma-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2543] [GtoPdb: 2000] [UniProtKB: P78368]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 6.58 pKd 265 nM Kd Science (2017) 358: null-null [PMID:29191878]
casein kinase 1 gamma 3/Casein kinase I isoform gamma-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5084] [GtoPdb: 2001] [UniProtKB: Q9Y6M4]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
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 Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Protein kinase G (PKG) 1/cGMP-dependent protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4273] [GtoPdb: 1492] [UniProtKB: Q13976]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Chromodomain-helicase-DNA-binding protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105742] [UniProtKB: Q14839]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
citron rho-interacting serine/threonine kinase/Citron Rho-interacting kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5579] [GtoPdb: 1509] [UniProtKB: O14578]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 5.36 pKd 4361 nM Kd Science (2017) 358: null-null [PMID:29191878]
cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
cyclin dependent kinase 12/Cyclin-dependent kinase 12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3559692] [GtoPdb: 1965] [UniProtKB: Q9NYV4]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
cyclin dependent kinase 13/Cyclin-dependent kinase 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795192] [GtoPdb: 1966] [UniProtKB: Q14004]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
cyclin dependent kinase 16/Cyclin-dependent kinase 16 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4597] [GtoPdb: 1969] [UniProtKB: Q00536]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
cyclin dependent kinase 17/Cyclin-dependent kinase 17 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5790] [GtoPdb: 1970] [UniProtKB: Q00537]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
cyclin dependent kinase 3/Cyclin-dependent kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4442] [GtoPdb: 1975] [UniProtKB: Q00526]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
cyclin dependent kinase 6/Cyclin-dependent kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2508] [GtoPdb: 1978] [UniProtKB: Q00534]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
cyclin dependent kinase 7/Cyclin-dependent kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3055] [GtoPdb: 1979] [UniProtKB: P50613]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
cyclin G associated kinase/Cyclin-G-associated kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4355] [GtoPdb: 2027] [UniProtKB: O14976]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 5.31 pKd 4862 nM Kd Science (2017) 358: null-null [PMID:29191878]
GtoPdb Binding affinity determined in a cell-free biochemical assay. - 6.87 pKd 136 nM Kd Lancet Infect Dis (2020) 20: 400-402 [PMID:32113509]
ChEMBL Binding affinity to GAK (unknown origin) B 6.92 pKd 120 nM Kd J Med Chem (2021) 64: 11090-11128 [PMID:34270254]
ChEMBL Binding affinity to GAK (unknown origin) assessed as dissociation constant B 6.92 pKd 120 nM Kd J Med Chem (2022) 65: 893-921 [PMID:33539089]
ChEMBL Binding affinity to GAK (unknown origin) assessed as dissociation constant B 6.92 pKd 120 nM Kd J Med Chem (2022) 65: 935-954 [PMID:33970631]
ChEMBL Binding affinity to GAK (unknown origin) B 6.92 pKd 120 nM Kd J Med Chem (2022) 65: 4121-4155 [PMID:35171586]
ChEMBL Inhibition of GAK (unknown origin) B 6.87 pIC50 136 nM IC50 J Med Chem (2022) 65: 893-921 [PMID:33539089]
Cysteine--tRNA ligase, cytoplasmic in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105937] [UniProtKB: P49589]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Cytochrome c1, heme protein, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105975] [UniProtKB: P08574]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
dCTP pyrophosphatase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3769292] [UniProtKB: Q9H773]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Delta(24)-sterol reductase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2331059] [UniProtKB: Q15392]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Deoxycytidine kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2447] [UniProtKB: P27707]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
discoidin domain receptor tyrosine kinase 2/Discoidin domain-containing receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5122] [GtoPdb: 1844] [UniProtKB: Q16832]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
DnaJ homolog subfamily A member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189122] [UniProtKB: P31689]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
DNA replication licensing factor MCM4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105745] [UniProtKB: P33991]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
DNA topoisomerase II alpha/DNA topoisomerase 2-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1806] [GtoPdb: 2637] [UniProtKB: P11388]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
DNA topoisomerase 2-beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3396] [UniProtKB: Q02880]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase kinase 1/Dual specificity mitogen-activated protein kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3587] [GtoPdb: 2062] [UniProtKB: Q02750]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase kinase 2/Dual specificity mitogen-activated protein kinase kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2964] [GtoPdb: 2063] [UniProtKB: P36507]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase kinase 3/Dual specificity mitogen-activated protein kinase kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2109] [GtoPdb: 2064] [UniProtKB: P46734]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase kinase 5/Dual specificity mitogen-activated protein kinase kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4948] [GtoPdb: 2066] [UniProtKB: Q13163]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase kinase 6/Dual specificity mitogen-activated protein kinase kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2171] [GtoPdb: 2067] [UniProtKB: P52564]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
CDC like kinase 1/Dual specificity protein kinase CLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 6.11 pKd 778 nM Kd Science (2017) 358: null-null [PMID:29191878]
CDC like kinase 2/Dual specificity protein kinase CLK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4225] [GtoPdb: 1991] [UniProtKB: P49760]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
CDC like kinase 3/Dual specificity protein kinase CLK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4226] [GtoPdb: 1992] [UniProtKB: P49761]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
CDC like kinase 4/Dual specificity protein kinase CLK4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4203] [GtoPdb: 1993] [UniProtKB: Q9HAZ1]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
testis associated actin remodelling kinase 1/Dual specificity testis-specific protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5604] [GtoPdb: 2239] [UniProtKB: Q15569]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
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 Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Dynamin-like GTPase OPA1, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105705] [UniProtKB: O60313]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
TP53 regulating kinase/EKC/KEOPS complex subunit TP53RK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1938223] [GtoPdb: 2248] [UniProtKB: Q96S44]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Electron transfer flavoprotein subunit beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105744] [UniProtKB: P38117]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Elongation factor Tu, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105970] [UniProtKB: P49411]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
EPH receptor A1/Ephrin type-A receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5810] [GtoPdb: 1821] [UniProtKB: P21709]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
EPH receptor A2/Ephrin type-A receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
EPH receptor A4/Ephrin type-A receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3988] [GtoPdb: 1824] [UniProtKB: P54764]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
EPH receptor A5/Ephrin type-A receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3987] [GtoPdb: 1825] [UniProtKB: P54756]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
EPH receptor A7/Ephrin type-A receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4602] [GtoPdb: 1827] [UniProtKB: Q15375]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
EPH receptor B2/Ephrin type-B receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
EPH receptor B3/Ephrin type-B receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4901] [GtoPdb: 1832] [UniProtKB: P54753]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
EPH receptor B4/Ephrin type-B receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5147] [GtoPdb: 1833] [UniProtKB: P54760]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
EPH receptor B6/Ephrin type-B receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5836] [GtoPdb: 1834] [UniProtKB: O15197]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
epidermal growth factor receptor/Epidermal growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
discoidin domain receptor tyrosine kinase 1/Epithelial discoidin domain-containing receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5319] [GtoPdb: 1843] [UniProtKB: Q08345]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Eukaryotic peptide chain release factor GTP-binding subunit ERF3B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105974] [UniProtKB: Q8IYD1]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
eukaryotic translation initiation factor 2 alpha kinase 1/Eukaryotic translation initiation factor 2-alpha kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6029] [GtoPdb: 2015] [UniProtKB: Q9BQI3]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 6.47 pKd 335 nM Kd Science (2017) 358: null-null [PMID:29191878]
Eukaryotic translation initiation factor 5B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105852] [UniProtKB: O60841]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Exosome RNA helicase MTR4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105889] [UniProtKB: P42285]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Ferrochelatase, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3879831] [UniProtKB: P22830]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
protein tyrosine kinase 2/Focal adhesion kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
General transcription and DNA repair factor IIH helicase subunit XPD in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105743] [UniProtKB: P18074]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Glycine--tRNA ligase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105815] [UniProtKB: P41250]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Glycogen phosphorylase, brain form in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3856] [UniProtKB: P11216]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Glycogen phosphorylase, liver form in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2568] [UniProtKB: P06737]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
glycogen synthase kinase 3 alpha/Glycogen synthase kinase-3 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2850] [GtoPdb: 2029] [UniProtKB: P49840]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
G protein-coupled receptor kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6144] [GtoPdb: 1470] [UniProtKB: P43250]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
GTP-binding nuclear protein Ran in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1741190] [UniProtKB: P62826]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
GTP-binding protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105780] [UniProtKB: Q9BZE4]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Guanine nucleotide-binding protein G(i) subunit alpha-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105887] [UniProtKB: P04899]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Haem oxygenase 2/Heme oxygenase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2546] [GtoPdb: 1442] [UniProtKB: P30519]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
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 Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
inosine monophosphate dehydrogenase 2/Inosine-5`-monophosphate dehydrogenase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2002] [GtoPdb: 2625] [UniProtKB: P12268]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
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 Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
integrin linked kinase/Integrin-linked protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5247] [GtoPdb: 2041] [UniProtKB: Q13418]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
interleukin 1 receptor associated kinase 1/Interleukin-1 receptor-associated kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3357] [GtoPdb: 2042] [UniProtKB: P51617]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
interleukin 1 receptor associated kinase 3/Interleukin-1 receptor-associated kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5081] [GtoPdb: 2044] [UniProtKB: Q9Y616]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
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 Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Isoleucine--tRNA ligase, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105821] [UniProtKB: Q9NSE4]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Janus kinase 2/Janus kinase 1/tyrosine kinase 2/JAK1/JAK2/TYK2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3301390] [GtoPdb: 204820472269] [UniProtKB: O60674P23458P29597]
GtoPdb - - 7.21 pIC50 61 nM IC50 J Med Chem (2014) 57: 5023-38 [PMID:24417533]
ChEMBL Inhibition of JAK1/JAK2/TYK2 in human whole blood assessed as inhibition of IL-6-induced STAT-1 phosphorylation preincubated for 45 mins followed by IL-6 addition measured after 15 mins by FACS analysis B 7.68 pIC50 21.1 nM IC50 J Med Chem (2014) 57: 5023-5038 [PMID:24417533]
ChEMBL Inhibition of JAK1/JAK2/TYK2 in human PBMC assessed as reduction in IL-6-induced STAT1 phosphorylation preincubated for 5 mins followed by IL-6 stimulation for 15 to 60 mins by flow cytometry analysis B 7.8 pIC50 16 nM IC50 J Med Chem (2016) 59: 733-749 [PMID:26701356]
GtoPdb - - 8.15 pIC50 7 nM IC50 J Med Chem (2014) 57: 5023-38 [PMID:24417533]
GtoPdb - - 8.23 pIC50 5.9 nM IC50 J Immunol (2010) 184: 5298-307 [PMID:20363976]
GtoPdb - - 8.24 pIC50 5.7 nM IC50 J Immunol (2010) 184: 5298-307 [PMID:20363976]
GtoPdb - - 8.4 pIC50 4 nM IC50 J Med Chem (2014) 57: 5023-38 [PMID:24417533]
Janus kinase 1/tyrosine kinase 2/JAK1/TYK2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3301391] [GtoPdb: 20472269] [UniProtKB: P23458P29597]
GtoPdb - - 7.21 pIC50 61 nM IC50 J Med Chem (2014) 57: 5023-38 [PMID:24417533]
ChEMBL Inhibition of JAK1/TYK2 in human whole blood assessed as reduction in IFNalpha induced STAT3 phosphorylation preincubated for 45 mins followed by IFNalpha addition measured after 15 mins by flow cytometric analysis B 7.54 pIC50 29 nM IC50 J Med Chem (2018) 61: 1130-1152 [PMID:29298069]
ChEMBL Inhibition of JAK1/TYK2 in human whole blood assessed as inhibition of IFN-alpha-induced STAT-3 phosphorylation preincubated for 45 mins followed by IFN-alpha addition measured after 15 mins by FACS analysis B 7.54 pIC50 28.7 nM IC50 J Med Chem (2014) 57: 5023-5038 [PMID:24417533]
ChEMBL Inhibition of TYK2/JAK1 in human PBMC assessed as reduction in IFNalpha-induced STAT1 phosphorylation preincubated for 5 mins followed by IFNalpha stimulation for 15 to 60 mins by flow cytometry analysis B 7.82 pIC50 15 nM IC50 J Med Chem (2016) 59: 733-749 [PMID:26701356]
ChEMBL Inhibition of JAK1/TYK2 in human M07E cells assessed as reduction of IFN alpha stimulated STAT phosphorylation preincubated for 30 mins followed by IFN alpha stimulation and measured after 15 mins by flow cytometry method B 7.89 pIC50 13 nM IC50 J Med Chem (2023) 66: 2161-2168 [PMID:36657024]
GtoPdb - - 8.23 pIC50 5.9 nM IC50 J Immunol (2010) 184: 5298-307 [PMID:20363976]
GtoPdb - - 8.4 pIC50 4 nM IC50 J Med Chem (2014) 57: 5023-38 [PMID:24417533]
Janus kinase 2/tyrosine kinase 2/JAK2/TYK2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3301392] [GtoPdb: 20482269] [UniProtKB: O60674P29597]
ChEMBL Inhibition of TYK2/JAK2 in human PBMC assessed as reduction in IL-23-induced STAT4 phosphorylation preincubated for 5 mins followed by IL-23 stimulation for 15 to 60 mins by flow cytometry analysis B 6.7 pIC50 200 nM IC50 J Med Chem (2016) 59: 733-749 [PMID:26701356]
ChEMBL Inhibition of JAK2/TYK2 in human whole blood assessed as inhibition of IL-12-induced STAT-4 phosphorylation preincubated for 45 mins followed by IL-12 addition measured after 15 mins by FACS analysis B 6.83 pIC50 149 nM IC50 J Med Chem (2014) 57: 5023-5038 [PMID:24417533]
ChEMBL Inhibition of JAK2/TYK2 in human whole blood assessed as inhibition of IL-23-induced STAT-3 phosphorylation preincubated for 45 mins followed by IL-23 addition measured after 15 mins by FACS analysis B 7.09 pIC50 81.9 nM IC50 J Med Chem (2014) 57: 5023-5038 [PMID:24417533]
GtoPdb - - 7.21 pIC50 61 nM IC50 J Med Chem (2014) 57: 5023-38 [PMID:24417533]
GtoPdb - - 8.15 pIC50 7 nM IC50 J Med Chem (2014) 57: 5023-38 [PMID:24417533]
GtoPdb - - 8.24 pIC50 5.7 nM IC50 J Immunol (2010) 184: 5298-307 [PMID:20363976]
Janus kinase 1/Janus kinase 3/JAK3/JAK1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038491] [GtoPdb: 20472049] [UniProtKB: P23458P52333]
GtoPdb - - 6.1 pIC50 787 nM IC50 J Med Chem (2014) 57: 5023-38 [PMID:24417533]
ChEMBL Inhibition of JAK1/JAK3 signaling pathway in human THP-1 cells assessed as reduction in IL-4 induced STAT6 phosphorylation preincubated for 2 hrs followed by IL-4 addition and measured after 10 mins by HTRF method B 6.25 pIC50 562 nM IC50 Eur J Med Chem (2021) 218: 113394-113394 [PMID:33813153]
ChEMBL Inhibition of JAK1/JAK3 in human whole blood assessed as inhibition of IL-15-induced STAT-5 phosphorylation preincubated for 45 mins followed by IL-15 addition measured after 15 mins by FACS analysis B 6.59 pIC50 259 nM IC50 J Med Chem (2014) 57: 5023-5038 [PMID:24417533]
ChEMBL Inhibition of JAK1/JAK3 in human PBMC assessed as reduction in IL-21-induced STAT3 phosphorylation preincubated for 5 mins followed by IL-21 stimulation for 15 to 60 mins by flow cytometry analysis B 7.17 pIC50 67 nM IC50 J Med Chem (2016) 59: 733-749 [PMID:26701356]
ChEMBL Inhibition of JAK1/JAK3 in human blood assessed as reduction of IL-2 stimulated STAT phosphorylation preincubated for 30 mins followed by IL-2 stimulation and measured after 15 mins by flow cytometry method B 7.46 pIC50 35 nM IC50 J Med Chem (2023) 66: 2161-2168 [PMID:36657024]
GtoPdb - - 8.23 pIC50 5.9 nM IC50 J Immunol (2010) 184: 5298-307 [PMID:20363976]
ChEMBL Inhibition of JAK1/JAK3 in human M07E cells assessed as reduction of IL-15 stimulated STAT phosphorylation preincubated for 30 mins followed by IL-15 stimulation and measured after 15 mins by flow cytometry analysis B 8.3 pIC50 5 nM IC50 J Med Chem (2023) 66: 2161-2168 [PMID:36657024]
GtoPdb - - 8.4 pIC50 4 nM IC50 J Med Chem (2014) 57: 5023-38 [PMID:24417533]
LIM domain kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3836] [GtoPdb: 2054] [UniProtKB: P53667]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
LIM domain kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5932] [GtoPdb: 2055] [UniProtKB: P53671]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Long-chain-fatty-acid--CoA ligase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105818] [UniProtKB: Q9ULC5]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
macrophage stimulating 1 receptor/Macrophage-stimulating protein receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2689] [GtoPdb: 1816] [UniProtKB: Q04912]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
MAPK activated protein kinase 3/MAP kinase-activated protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4670] [GtoPdb: 2095] [UniProtKB: Q16644]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
MAPK activated protein kinase 5/MAP kinase-activated protein kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3094] [GtoPdb: 2096] [UniProtKB: Q8IW41]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
microtubule affinity regulating kinase 3/MAP/microtubule affinity-regulating kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5600] [GtoPdb: 2099] [UniProtKB: P27448]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 6.98 pKd 104 nM Kd Science (2017) 358: null-null [PMID:29191878]
maternal embryonic leucine zipper kinase/Maternal embryonic leucine zipper kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4578] [GtoPdb: 2102] [UniProtKB: Q14680]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Membrane-associated progesterone receptor component 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105706] [UniProtKB: O00264]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
protein kinase, membrane associated tyrosine/threonine 1/Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3984] [GtoPdb: 2167] [UniProtKB: Q99640]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Midasin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105779] [UniProtKB: Q9NU22]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
misshapen like kinase 1/Misshapen-like kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5518] [GtoPdb: 2103] [UniProtKB: Q8N4C8]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase 1/Mitogen-activated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase 10/Mitogen-activated protein kinase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2637] [GtoPdb: 1498] [UniProtKB: P53779]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase 11/Mitogen-activated protein kinase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3961] [GtoPdb: 1500] [UniProtKB: Q15759]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase 14/Mitogen-activated protein kinase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase 15/Mitogen-activated protein kinase 15 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5198] [GtoPdb: 2090] [UniProtKB: Q8TD08]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase 3/Mitogen-activated protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase 7/Mitogen-activated protein kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5332] [GtoPdb: 2093] [UniProtKB: Q13164]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase 8/Mitogen-activated protein kinase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2276] [GtoPdb: 1496] [UniProtKB: P45983]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase 9/Mitogen-activated protein kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4179] [GtoPdb: 1497] [UniProtKB: P45984]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase kinase kinase 1/Mitogen-activated protein kinase kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3956] [GtoPdb: 2069] [UniProtKB: Q13233]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 5.72 pKd 1891 nM Kd Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase kinase kinase 11/Mitogen-activated protein kinase kinase kinase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2708] [GtoPdb: 2071] [UniProtKB: Q16584]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase kinase kinase 2/Mitogen-activated protein kinase kinase kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5914] [GtoPdb: 2077] [UniProtKB: Q9Y2U5]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
ZAK sterile alpha motif and leucine zipper containing kinase AZK/Mitogen-activated protein kinase kinase kinase 20 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3886] [GtoPdb: 2289] [UniProtKB: Q9NYL2]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase kinase kinase 3/Mitogen-activated protein kinase kinase kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5970] [GtoPdb: 2078] [UniProtKB: Q99759]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase kinase kinase 4/Mitogen-activated protein kinase kinase kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4853] [GtoPdb: 2079] [UniProtKB: Q9Y6R4]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase kinase kinase 5/Mitogen-activated protein kinase kinase kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5285] [GtoPdb: 2080] [UniProtKB: Q99683]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase kinase kinase 6/Mitogen-activated protein kinase kinase kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163123] [GtoPdb: 2081] [UniProtKB: O95382]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase kinase kinase kinase 1/Mitogen-activated protein kinase kinase kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5749] [GtoPdb: 2085] [UniProtKB: Q92918]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
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 Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase kinase kinase kinase 3/Mitogen-activated protein kinase kinase kinase kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5432] [GtoPdb: 2087] [UniProtKB: Q8IVH8]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
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 Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
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 Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Myosin-10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105746] [UniProtKB: P35580]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Myosin-14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105888] [UniProtKB: Q7Z406]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
myosin light chain kinase 3/Myosin light chain kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4627] [GtoPdb: 2110] [UniProtKB: Q32MK0]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
myosin light chain kinase/Myosin light chain kinase, smooth muscle in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2428] [GtoPdb: 1552] [UniProtKB: Q15746]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105781] [UniProtKB: Q9P0J0]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
tyrosine kinase non receptor 1/Non-receptor tyrosine-protein kinase TNK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5334] [GtoPdb: 2245] [UniProtKB: Q13470]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 6.21 pKd 622 nM Kd Science (2017) 358: null-null [PMID:29191878]
tyrosine kinase 2/Non-receptor tyrosine-protein kinase TYK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
GtoPdb - - 7.21 pIC50 61 nM IC50 J Med Chem (2014) 57: 5023-38 [PMID:24417533]
ChEMBL Inhibition of TYK2 (unknown origin) B 7.21 pIC50 61 nM IC50 J Med Chem (2014) 57: 5023-5038 [PMID:24417533]
ChEMBL Inhibition of recombinant human N-terminal GST-tagged TYK2 (871 to 1187 residues) expressed in baculovirus expression system B 7.21 pIC50 61 nM IC50 Eur J Med Chem (2021) 218: 113394-113394 [PMID:33813153]
ChEMBL Inhibition of recombinant epitope tagged Tyk2 kinase domain (873 to 1187 residues) (unknown origin) using peptide substrate by fluorescence based assay B 7.28 pIC50 53 nM IC50 Bioorg Med Chem (2019) 27: 2592-2597 [PMID:30926315]
ChEMBL Inhibition of Tyk2 (unknown origin) B 7.28 pIC50 53 nM IC50 Bioorg Med Chem (2019) 27: 2592-2597 [PMID:30926315]
ChEMBL Inhibition of recombinant TYK2 (unknown origin) (873 to 1187 residues) in presence of ATP by homogeneous time-resolved fluorescence assay B 7.28 pIC50 53 nM IC50 Eur J Med Chem (2024) 267: 116210-116210 [PMID:38359535]
ChEMBL Inhibition of recombinant epitope tagged TYK2 (unknown origin) (873 to 1187 residues) using peptide as substrate in presence of ATP by homogeneous time-resolved fluorescence assay B 7.28 pIC50 53 nM IC50 Eur J Med Chem (2022) 239: 114551-114551 [PMID:35749986]
ChEMBL Inhibition of recombinant epitope tagged TYK2 (unknown origin) (873 to 1187 residues) using peptide substrate in presence of ATP by time-resolved fluorescence assay B 7.28 pIC50 53 nM IC50 J Med Chem (2023) 66: 6725-6742 [PMID:37163463]
ChEMBL Inhibition of Tyk2 (unknown origin) B 7.28 pIC50 53 nM IC50 J Med Chem (2015) 58: 7596-7602 [PMID:26351728]
ChEMBL Biochemical Activity Assay: The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ��-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35. B 7.52 pIC50 30 nM IC50 US-11203595-B2. Aza-indazole compounds for use in tendon and/or ligament injuries (2021)
ChEMBL Kinase Assay: A kinase selectivity panel which measures substrate peptide phosphorylation was set-up for recombinant human Jak1 (aa 866-1154), Jak2 (aa808-1132), Jak3 (aa811-1124) and Tyk2 (aa888-1187). The technology used for the described assay is based on the separation and quantification of substrate and product in an electrical field. In the course of the kinase reaction the peptide substrate is phosphorylated by a kinase. The transfer of a phosphate residue also causes the introduction of two additional negative charges and hence to a change in the net charge of the phospho-peptide compared to the unphosphorylated peptide. Due to this difference in charge the phosphorylated und unphosphorylated peptides migrate with different velocities in an electrical field.In the applied method, this separation takes place inside a chip that contains a complex capillary system for simultaneous analysis of 12 samples (12-sipper chip, Caliper Technologies Corp., Mountain View, USA). In order to allow the detection and quantification of the peptides in the capillary system, the peptides carry a fluorescent label (fluorescein). With this label the peptides can be quantified by fluorescence intensity through the instruments laser and detection system (LC3000, Caliper Life Sciences).The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ß-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35.Plates with terminated kinase reactions were transferred to the Caliper LC3000 workstation (Caliper Technologies Corp., Mountain View, USA) for reading. The relative amount of phosphorylated peptide r, was calculated using the heights of the substrate peak, s, and the product peak, p: r=p/(p+s). B 7.52 pIC50 30 nM IC50 US-10112907-B2. Substituted indazoles for treating tendon and/or ligament injuries (2018)
ChEMBL Biochemical Activity Assay: The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ß-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35. B 7.52 pIC50 30 nM IC50 US-10766894-B2. Aza-indazole compounds for use in tendon and/or ligament injuries (2020)
ChEMBL Inhibition of TYK2 (unknown origin) by caliper technology B 7.64 pIC50 23 nM IC50 J Med Chem (2023) 66: 2161-2168 [PMID:36657024]
ChEMBL Inhibition of recombinant human TYK2 kinase domain (885-1176 residues) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent substrate phosphorylation after 45 mins by TR-FRET assay B 8.06 pIC50 8.7 nM IC50 J Med Chem (2016) 59: 733-749 [PMID:26701356]
NUAK family, SNF1-like kinase, 2/NUAK family SNF1-like kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5698] [GtoPdb: 2130] [UniProtKB: Q9H093]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Obg-like ATPase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105704] [UniProtKB: Q9NTK5]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
PAS domain containing serine/threonine kinase/PAS domain-containing serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6054] [GtoPdb: 2139] [UniProtKB: Q96RG2]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Peroxisomal acyl-coenzyme A oxidase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105748] [UniProtKB: Q15067]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Peroxisomal acyl-coenzyme A oxidase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105817] [UniProtKB: O15254]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Phenylalanine--tRNA ligase beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105969] [UniProtKB: Q9NSD9]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Phosphatidylethanolamine-binding protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105856] [UniProtKB: P30086]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
phosphatidylinositol-5-phosphate 4-kinase type 2 gamma/Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1770034] [GtoPdb: 2163] [UniProtKB: Q8TBX8]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
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 Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
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 Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Probable ATP-dependent RNA helicase DDX6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105783] [UniProtKB: P26196]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
protein kinase C alpha/Protein kinase C alpha type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 5.68 pKd 2071 nM Kd Science (2017) 358: null-null [PMID:29191878]
protein kinase C beta/Protein kinase C beta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.58 pKd 26324 nM Kd Science (2017) 358: null-null [PMID:29191878]
protein kinase C delta/Protein kinase C delta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2996] [GtoPdb: 1485] [UniProtKB: Q05655]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 5.97 pKd 1075 nM Kd Science (2017) 358: null-null [PMID:29191878]
protein kinase C iota/Protein kinase C iota type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2598] [GtoPdb: 1490] [UniProtKB: P41743]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
protein kinase C theta/Protein kinase C theta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3920] [GtoPdb: 1488] [UniProtKB: Q04759]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
protein tyrosine kinase 2 beta/Protein-tyrosine kinase 2-beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5469] [GtoPdb: 2181] [UniProtKB: Q14289]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
protein tyrosine kinase 6/Protein-tyrosine kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4601] [GtoPdb: 2182] [UniProtKB: Q13882]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
ret proto-oncogene/Proto-oncogene tyrosine-protein kinase receptor Ret in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 6.01 pKd 973 nM Kd Science (2017) 358: null-null [PMID:29191878]
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 Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Putative heat shock protein HSP 90-beta 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105858] [UniProtKB: Q58FF8]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Pyridoxal kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075181] [UniProtKB: O00764]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Rab-like protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105853] [UniProtKB: Q5HYI8]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
AKT serine/threonine kinase 1/RAC-alpha serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
AKT serine/threonine kinase 2/RAC-beta serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2431] [GtoPdb: 1480] [UniProtKB: P31751]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
AKT serine/threonine kinase 3/RAC-gamma serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4816] [GtoPdb: 2286] [UniProtKB: Q9Y243]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Ras-related protein Rab-10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105971] [UniProtKB: P61026]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
RAB27A, member RAS oncogene family/Ras-related protein Rab-27A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105702] [GtoPdb: 2916] [UniProtKB: P51159]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Ras-related protein Rab-6A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105703] [UniProtKB: P20340]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
receptor interacting serine/threonine kinase 2/Receptor-interacting serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5014] [GtoPdb: 2190] [UniProtKB: O43353]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
receptor interacting serine/threonine kinase 3/Receptor-interacting serine/threonine-protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795199] [GtoPdb: 2191] [UniProtKB: Q9Y572]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
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 Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
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 Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 6.32 pKd 482 nM Kd Science (2017) 358: null-null [PMID:29191878]
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 Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 6.12 pKd 756 nM Kd Science (2017) 358: null-null [PMID:29191878]
ribosomal protein S6 kinase A1/Ribosomal protein S6 kinase alpha-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2553] [GtoPdb: 1527] [UniProtKB: Q15418]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
ribosomal protein S6 kinase A3/Ribosomal protein S6 kinase alpha-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2345] [GtoPdb: 1528] [UniProtKB: P51812]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
ribosomal protein S6 kinase A4/Ribosomal protein S6 kinase alpha-4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3125] [GtoPdb: 1524] [UniProtKB: O75676]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
ribosomal protein S6 kinase A5/Ribosomal protein S6 kinase alpha-5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4237] [GtoPdb: 1523] [UniProtKB: O75582]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
ribosomal protein S6 kinase A6/Ribosomal protein S6 kinase alpha-6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4924] [GtoPdb: 1530] [UniProtKB: Q9UK32]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
ribosomal protein S6 kinase B1/Ribosomal protein S6 kinase beta-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4501] [GtoPdb: 1525] [UniProtKB: P23443]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Ribosyldihydronicotinamide dehydrogenase [quinone] in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3959] [UniProtKB: P16083]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
RNA cytidine acetyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105935] [UniProtKB: Q9H0A0]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
S-adenosylmethionine synthase isoform type-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3313835] [UniProtKB: P31153]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Septin-9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105891] [UniProtKB: Q9UHD8]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 7.08 pKd 84 nM Kd Science (2017) 358: null-null [PMID:29191878]
serine/threonine kinase 10/Serine/threonine-protein kinase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3981] [GtoPdb: 2211] [UniProtKB: O94804]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
serine/threonine kinase 16/Serine/threonine-protein kinase 16 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3938] [GtoPdb: 2213] [UniProtKB: O75716]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
serine/threonine kinase 24/Serine/threonine-protein kinase 24 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5082] [GtoPdb: 2217] [UniProtKB: Q9Y6E0]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
serine/threonine-protein kinase MST4/Serine/threonine-protein kinase 26 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5941] [GtoPdb: 2287] [UniProtKB: Q9P289]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
serine/threonine kinase 3/Serine/threonine-protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4708] [GtoPdb: 2219] [UniProtKB: Q13188]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Serine/threonine kinase 38 like/Serine/threonine-protein kinase 38-like in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4851] [GtoPdb: 1518] [UniProtKB: Q9Y2H1]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
serine/threonine kinase 4/Serine/threonine-protein kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4598] [GtoPdb: 2225] [UniProtKB: Q13043]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
A-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase A-Raf in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1169596] [GtoPdb: 1933] [UniProtKB: P10398]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
ATR checkpoint kinase/Serine/threonine-protein kinase ATR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5024] [GtoPdb: 1935] [UniProtKB: Q13535]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
B-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase B-raf in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5145] [GtoPdb: 1943] [UniProtKB: P15056]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
protein kinase D2/Serine/threonine-protein kinase D2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4900] [GtoPdb: 2173] [UniProtKB: Q9BZL6]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
protein kinase D3/Serine/threonine-protein kinase D3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2595] [GtoPdb: 2174] [UniProtKB: O94806]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
endoplasmic reticulum to nucleus signaling 1/Serine/threonine-protein kinase/endoribonuclease IRE1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163101] [GtoPdb: 2020] [UniProtKB: O75460]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
endoplasmic reticulum to nucleus signaling 2/Serine/threonine-protein kinase/endoribonuclease IRE2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105932] [GtoPdb: 2021] [UniProtKB: Q76MJ5]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
ciliogenesis associated kinase 1/Serine/threonine-protein kinase ICK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163126] [GtoPdb: 2038] [UniProtKB: Q9UPZ9]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
large tumor suppressor kinase 1/Serine/threonine-protein kinase LATS1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6167] [GtoPdb: 1515] [UniProtKB: O95835]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
microtubule affinity regulating kinase 2/Serine/threonine-protein kinase MARK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3831] [GtoPdb: 2098] [UniProtKB: Q7KZI7]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 6.9 pKd 125 nM Kd Science (2017) 358: null-null [PMID:29191878]
CDC42 binding protein kinase alpha/Serine/threonine-protein kinase MRCK alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4516] [GtoPdb: 1507] [UniProtKB: Q5VT25]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
CDC42 binding protein kinase beta/Serine/threonine-protein kinase MRCK beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5052] [GtoPdb: 1508] [UniProtKB: Q9Y5S2]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
CDC42 binding protein kinase gamma/Serine/threonine-protein kinase MRCK gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5615] [GtoPdb: 1506] [UniProtKB: Q6DT37]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
protein kinase N1/Serine/threonine-protein kinase N1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3384] [GtoPdb: 1520] [UniProtKB: Q16512]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 6.98 pKd 104 nM Kd Science (2017) 358: null-null [PMID:29191878]
protein kinase N2/Serine/threonine-protein kinase N2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3032] [GtoPdb: 1521] [UniProtKB: Q16513]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 6.57 pKd 269 nM Kd Science (2017) 358: null-null [PMID:29191878]
NIMA related kinase 1/Serine/threonine-protein kinase Nek1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5855] [GtoPdb: 2114] [UniProtKB: Q96PY6]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
NIMA related kinase 2/Serine/threonine-protein kinase Nek2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3835] [GtoPdb: 2117] [UniProtKB: P51955]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
NIMA related kinase 3/Serine/threonine-protein kinase Nek3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5679] [GtoPdb: 2118] [UniProtKB: P51956]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
NIMA related kinase 9/Serine/threonine-protein kinase Nek9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5257] [GtoPdb: 2124] [UniProtKB: Q8TD19]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
nemo like kinase/Serine/threonine-protein kinase NLK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5364] [GtoPdb: 2125] [UniProtKB: Q9UBE8]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
p21 (RAC1) activated kinase 2/Serine/threonine-protein kinase PAK 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4487] [GtoPdb: 2134] [UniProtKB: Q13177]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
p21 (RAC1) activated kinase 4/Serine/threonine-protein kinase PAK 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4482] [GtoPdb: 2136] [UniProtKB: O96013]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
p21 (RAC1) activated kinase 6/Serine/threonine-protein kinase PAK 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4311] [GtoPdb: 2137] [UniProtKB: Q9NQU5]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
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 Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
polo like kinase 4/Serine/threonine-protein kinase PLK4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3788] [GtoPdb: 2171] [UniProtKB: O00444]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
salt inducible kinase 2/Serine/threonine-protein kinase SIK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5699] [GtoPdb: 2198] [UniProtKB: Q9H0K1]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
SIK family kinase 3/Serine/threonine-protein kinase SIK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6149] [GtoPdb: 2199] [UniProtKB: Q9Y2K2]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
serine/threonine kinase 11/Serine/threonine-protein kinase STK11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5606] [GtoPdb: 2212] [UniProtKB: Q15831]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
TAO kinase 1/Serine/threonine-protein kinase TAO1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5261] [GtoPdb: 2233] [UniProtKB: Q7L7X3]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
TAO kinase 2/Serine/threonine-protein kinase TAO2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075195] [GtoPdb: 2234] [UniProtKB: Q9UL54]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
TAO kinase 3/Serine/threonine-protein kinase TAO3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5701] [GtoPdb: 2235] [UniProtKB: Q9H2K8]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
TANK binding kinase 1/Serine/threonine-protein kinase TBK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5408] [GtoPdb: 2237] [UniProtKB: Q9UHD2]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
unc-51 like autophagy activating kinase 1/Serine/threonine-protein kinase ULK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6006] [GtoPdb: 2271] [UniProtKB: O75385]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 6.09 pKd 810 nM Kd Science (2017) 358: null-null [PMID:29191878]
unc-51 like kinase 3/Serine/threonine-protein kinase ULK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5047] [GtoPdb: 2273] [UniProtKB: Q6PHR2]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Signal recognition particle receptor subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105934] [UniProtKB: P08240]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
signal transducer and activator of transcription 3/Signal transducer and activator of transcription 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4026] [GtoPdb: 2994] [UniProtKB: P40763]
ChEMBL Inhibition of IL-6 stimulated STAT3 phosphorylation in human PBMC preincubated with compound for 10 to 15 mins followed by IL-6 stimulation and measured after 15 mins by ELISA analysis B 7.36 pIC50 44 nM IC50 Eur J Med Chem (2020) 192: 112155-112155 [PMID:32120325]
ChEMBL Inhibition of IL-23 stimulated STAT3 production in human naive T cell preincubated with compound for 10 to 15 mins followed by IL-23 stimulation and measured after 15 mins by ELISA analysis B 7.7 pIC50 20 nM IC50 Eur J Med Chem (2020) 192: 112155-112155 [PMID:32120325]
STE20 like kinase/STE20-like serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4202] [GtoPdb: 2200] [UniProtKB: Q9H2G2]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
STE20 related adaptor alpha/STE20-related kinase adapter protein alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795198] [GtoPdb: 2227] [UniProtKB: Q7RTN6]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Structural maintenance of chromosomes protein 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105747] [UniProtKB: Q14683]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Structural maintenance of chromosomes protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105890] [UniProtKB: O95347]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Succinate--CoA ligase [ADP-forming] subunit beta, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105973] [UniProtKB: Q9P2R7]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
transforming growth factor beta receptor 1/TGF-beta receptor type-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4439] [GtoPdb: 1788] [UniProtKB: P36897]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
transforming growth factor beta receptor 2/TGF-beta receptor type-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4267] [GtoPdb: 1795] [UniProtKB: P37173]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Thyroid hormone receptor-associated protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105820] [UniProtKB: Q9Y2W1]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
TRAF2 and NCK interacting kinase/TRAF2 and NCK-interacting protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4527] [GtoPdb: 2244] [UniProtKB: Q9UKE5]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
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 Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
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 Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
C-terminal Src kinase/Tyrosine-protein kinase CSK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2634] [GtoPdb: 1994] [UniProtKB: P41240]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
FER tyrosine kinase/Tyrosine-protein kinase Fer in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3982] [GtoPdb: 2022] [UniProtKB: P16591]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
FES proto-oncogene, tyrosine kinase/Tyrosine-protein kinase Fes/Fps in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5455] [GtoPdb: 2023] [UniProtKB: P07332]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
fyn related Src family tyrosine kinase/Tyrosine-protein kinase FRK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4223] [GtoPdb: 2025] [UniProtKB: P42685]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Fyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
HCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase HCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3234] [GtoPdb: 2032] [UniProtKB: P08631]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
ChEMBL Inhibition of JAK1 in human whole blood assessed as reduction in IL6-induced STAT1 phosphorylation in CD4+ T cells preincubated with compound for 30 mins followed by IL-6 addition and measured after 20 mins by flow cytometry analysis B 6.63 pIC50 234 nM IC50 J Immunol (2013) 191: 3568-3577 [PMID:24006460]
ChEMBL Inhibition of JAK1 in human whole blood assessed as reduction in IL6-induced STAT1 phosphorylation in CD4+ T cells preincubated with compound for 30 mins followed by IL-6 addition and measured after 20 mins by flow cytometry analysis B 7.63 pIC50 23.39 nM IC50 J Immunol (2013) 191: 3568-3577 [PMID:24006460]
ChEMBL Inhibition of JAK1 (unknown origin) B 8.22 pIC50 6 nM IC50 J Med Chem (2015) 58: 7596-7602 [PMID:26351728]
ChEMBL Inhibition of JAK1 (unknown origin) B 8.23 pIC50 5.9 nM IC50 Eur J Med Chem (2024) 275: 116540-116540 [PMID:38852338]
ChEMBL Inhibition of recombinant epitope tagged JAK1 kinase domain (837 to 1142 residues) (unknown origin) using peptide substrate by fluorescence based assay B 8.23 pIC50 5.9 nM IC50 Bioorg Med Chem (2019) 27: 2592-2597 [PMID:30926315]
ChEMBL Inhibition of JAK1 (unknown origin) using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition and measured by 30 mins by HTRF assay B 8.23 pIC50 5.9 nM IC50 Bioorg Med Chem (2019) 27: 2592-2597 [PMID:30926315]
ChEMBL Inhibition of JAK1 (unknown origin) B 8.23 pIC50 5.9 nM IC50 J Med Chem (2021) 64: 11090-11128 [PMID:34270254]
ChEMBL Inhibition of JAK 1 (unknown origin) B 8.23 pIC50 5.9 nM IC50 J Med Chem (2022) 65: 893-921 [PMID:33539089]
ChEMBL Reversible inhibition of JAK1 (unknown origin) B 8.23 pIC50 5.9 nM IC50 J Med Chem (2021) 64: 1283-1345 [PMID:33481605]
ChEMBL Inhibition of JAK: The study of the effect of compounds on the activity of purified recombinant JAK was performed by studying the inhibitory activity of the compounds on JAK from the enzymatic level. The experimental principle is to use a luminescence kinase assay to detect the ADP content produced by the reaction of JAK with the substrate Poly (4:1 Glu, Tyr) peptide: after ADP is converted to ATP, ATP can act as a substrate for the Ultra-Glo luciferase catalytic reaction, producing an optical signal. The luminescence signal is positively correlated with the amount of ADP and kinase activity. Therefore, the inhibitory effect of the compounds on the recombinant JAK was determined by observing the luminescence signal produced by the reaction of JAK and the substrate, and was expressed by IC50. B 8.23 pIC50 5.9 nM IC50 US-11414413-B2. Heterocyclic compound as JAK inhibitor, and salts and therapeutic use thereof (2022)
ChEMBL Inhibition of recombinant JAK1 (837 to 1142 residues) (unknown origin) by HTRF assay B 8.23 pIC50 5.9 nM IC50 J Med Chem (2022) 65: 4121-4155 [PMID:35171586]
ChEMBL Inhibition of recombinant epitope tagged JAK1 (unknown origin) (837 to 1142 residues) using peptide as substrate in presence of ATP by homogeneous time-resolved fluorescence assay B 8.23 pIC50 5.9 nM IC50 Eur J Med Chem (2022) 239: 114551-114551 [PMID:35749986]
ChEMBL Inhibition of JAK1 (unknown origin) B 8.23 pIC50 5.9 nM IC50 Eur J Med Chem (2023) 261: 115848-115848 [PMID:37793326]
ChEMBL Inhibition of recombinant JAK1 (unknown origin) (837 to 1142 residues) in presence of ATP by homogeneous time-resolved fluorescence assay B 8.23 pIC50 5.9 nM IC50 Eur J Med Chem (2024) 267: 116210-116210 [PMID:38359535]
ChEMBL Inhibition of JAK1 (unknown origin) B 8.23 pIC50 5.9 nM IC50 J Med Chem (2023) 66: 5753-5773 [PMID:37057760]
GtoPdb - - 8.23 pIC50 5.9 nM IC50 J Immunol (2010) 184: 5298-307 [PMID:20363976]
ChEMBL Inhibition of recombinant epitope tagged JAK1 (unknown origin) (837 to 1142 residues) using peptide substrate in presence of ATP by time-resolved fluorescence assay B 8.24 pIC50 5.8 nM IC50 J Med Chem (2023) 66: 6725-6742 [PMID:37163463]
ChEMBL Inhibition of JAK1 (unknown origin) B 8.4 pIC50 4 nM IC50 J Med Chem (2014) 57: 5023-5038 [PMID:24417533]
ChEMBL Inhibition of JAK1 (unknown origin) B 8.4 pIC50 4 nM IC50 Bioorg Med Chem (2016) 24: 2660-2672 [PMID:27137359]
ChEMBL Inhibition of recombinant human JAK1 using 5'FAM-KKSRGDYMTMQID as substrate in presence of 1 mM ATP by mobility shift assay B 8.4 pIC50 4 nM IC50 J Med Chem (2018) 61: 1130-1152 [PMID:29298069]
ChEMBL Inhibition of recombinant human N-terminal GST-tagged JAK1 (850 to 1154 residues) expressed in baculovirus expression system B 8.4 pIC50 4 nM IC50 Eur J Med Chem (2021) 218: 113394-113394 [PMID:33813153]
ChEMBL Inhibition of JAK1 (unknown origin) B 8.4 pIC50 4 nM IC50 RSC Med Chem (2022) 13: 1300-1321 [PMID:36439976]
GtoPdb - - 8.4 pIC50 4 nM IC50 J Med Chem (2014) 57: 5023-38 [PMID:24417533]
ChEMBL Inhibition of JAK1 JH1 domain (unknown origin) using FITC-Ahx-KKSRGDYMTMQIG-NH2 peptide as substrate incubated for 60 mins in the presence of ATP by caliper microfluidic mobility shift technology B 8.62 pIC50 2.4 nM IC50 J Med Chem (2023) 66: 2161-2168 [PMID:36657024]
ChEMBL Inhibition of JAK1 (unknown origin) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent substrate phosphorylation after 45 mins by TR-FRET assay B 9 pIC50 0.99 nM IC50 J Med Chem (2016) 59: 733-749 [PMID:26701356]
ChEMBL Kinase Assay: A kinase selectivity panel which measures substrate peptide phosphorylation was set-up for recombinant human Jak1 (aa 866-1154), Jak2 (aa808-1132), Jak3 (aa811-1124) and Tyk2 (aa888-1187). The technology used for the described assay is based on the separation and quantification of substrate and product in an electrical field. In the course of the kinase reaction the peptide substrate is phosphorylated by a kinase. The transfer of a phosphate residue also causes the introduction of two additional negative charges and hence to a change in the net charge of the phospho-peptide compared to the unphosphorylated peptide. Due to this difference in charge the phosphorylated und unphosphorylated peptides migrate with different velocities in an electrical field.In the applied method, this separation takes place inside a chip that contains a complex capillary system for simultaneous analysis of 12 samples (12-sipper chip, Caliper Technologies Corp., Mountain View, USA). In order to allow the detection and quantification of the peptides in the capillary system, the peptides carry a fluorescent label (fluorescein). With this label the peptides can be quantified by fluorescence intensity through the instruments laser and detection system (LC3000, Caliper Life Sciences).The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ß-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35.Plates with terminated kinase reactions were transferred to the Caliper LC3000 workstation (Caliper Technologies Corp., Mountain View, USA) for reading. The relative amount of phosphorylated peptide r, was calculated using the heights of the substrate peak, s, and the product peak, p: r=p/(p+s). B 9.15 pIC50 0.7 nM IC50 US-10112907-B2. Substituted indazoles for treating tendon and/or ligament injuries (2018)
ChEMBL Biochemical Activity Assay: The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ß-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35. B 9.15 pIC50 0.7 nM IC50 US-10766894-B2. Aza-indazole compounds for use in tendon and/or ligament injuries (2020)
ChEMBL Biochemical Activity Assay: The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ��-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35. B 9.15 pIC50 0.7 nM IC50 US-11203595-B2. Aza-indazole compounds for use in tendon and/or ligament injuries (2021)
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
ChEMBL Inhibition of JAK2 signaling pathway in human TF-1 cells assessed as reduction in GM-CSF induced STAT5 phosphorylation preincubated for 2 hrs followed by GM-CSF addition and measured after 10 mins by HTRF method B 6.33 pIC50 470 nM IC50 Eur J Med Chem (2021) 218: 113394-113394 [PMID:33813153]
ChEMBL Inhibition of JAK2 in human PBMC assessed as reduction in GM-CSF-induced STAT5 phosphorylation preincubated for 5 mins followed by GM-CSF stimulation for 15 to 60 mins by flow cytometry analysis B 6.54 pIC50 290 nM IC50 J Med Chem (2016) 59: 733-749 [PMID:26701356]
ChEMBL Inhibition of JAK2 homodimer in human CD34+ cells spiked into human whole blood assessed as inhibition of EPO-induced STAT-5 phosphorylation preincubated for 45 mins followed by EPO addition measured after 15 mins by FACS analysis B 7.06 pIC50 87.8 nM IC50 J Med Chem (2014) 57: 5023-5038 [PMID:24417533]
ChEMBL Inhibition of JAK2 in human whole blood assessed as reduction in GM-CSF-induced STAT5 phosphorylation in CD3-positive T cell preincubated with compound for 30 mins followed by GM-CSF addition and measured after 20 mins by flow cytometry analysis B 7.19 pIC50 63.83 nM IC50 J Immunol (2013) 191: 3568-3577 [PMID:24006460]
ChEMBL Inhibition of JAK2 in human whole blood assessed as reduction in GM-CSF-induced STAT5 phosphorylation in CD3-positive T cell preincubated with compound for 30 mins followed by GM-CSF addition and measured after 20 mins by flow cytometry analysis B 7.2 pIC50 63.8 nM IC50 J Immunol (2013) 191: 3568-3577 [PMID:24006460]
GtoPdb - - 8.15 pIC50 7 nM IC50 J Med Chem (2014) 57: 5023-38 [PMID:24417533]
ChEMBL Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system B 8.15 pIC50 7 nM IC50 Eur J Med Chem (2021) 218: 113394-113394 [PMID:33813153]
ChEMBL Inhibition of JAK2 (unknown origin) B 8.15 pIC50 7 nM IC50 Bioorg Med Chem (2016) 24: 2660-2672 [PMID:27137359]
ChEMBL Inhibition of JAK2 (unknown origin) B 8.18 pIC50 6.6 nM IC50 J Med Chem (2014) 57: 5023-5038 [PMID:24417533]
ChEMBL Inhibition of JAK2 (unknown origin) B 8.18 pIC50 6.6 nM IC50 RSC Med Chem (2022) 13: 1300-1321 [PMID:36439976]
ChEMBL Inhibition of JAK2 (unknown origin) B 8.22 pIC50 6 nM IC50 J Med Chem (2015) 58: 7596-7602 [PMID:26351728]
GtoPdb - - 8.24 pIC50 5.7 nM IC50 J Immunol (2010) 184: 5298-307 [PMID:20363976]
ChEMBL Inhibition of JAK2 (unknown origin) using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition and measured by 30 mins by HTRF assay B 8.24 pIC50 5.7 nM IC50 Bioorg Med Chem (2019) 27: 2592-2597 [PMID:30926315]
ChEMBL Inhibition of JAK2 (unknown origin) B 8.24 pIC50 5.7 nM IC50 J Med Chem (2021) 64: 11090-11128 [PMID:34270254]
ChEMBL Inhibition of JAK 2 (unknown origin) B 8.24 pIC50 5.7 nM IC50 J Med Chem (2022) 65: 893-921 [PMID:33539089]
ChEMBL Reversible inhibition of JAK2 (unknown origin) B 8.24 pIC50 5.7 nM IC50 J Med Chem (2021) 64: 1283-1345 [PMID:33481605]
ChEMBL Inhibition of recombinant JAK2 (828 to 1132 residues) (unknown origin) by HTRF assay B 8.24 pIC50 5.7 nM IC50 J Med Chem (2022) 65: 4121-4155 [PMID:35171586]
ChEMBL Inhibition of recombinant epitope tagged JAK2 kinase domain (828 to 1132 residues) (unknown origin) using peptide substrate by fluorescence based assay B 8.24 pIC50 5.7 nM IC50 Bioorg Med Chem (2019) 27: 2592-2597 [PMID:30926315]
ChEMBL Inhibition of recombinant epitope tagged JAK2 (unknown origin) (828 to 1132 residues) using peptide substrate in presence of ATP by time-resolved fluorescence assay B 8.24 pIC50 5.7 nM IC50 J Med Chem (2023) 66: 6725-6742 [PMID:37163463]
ChEMBL Inhibition of recombinant epitope tagged JAK2 (unknown origin) (828 to 1132 residues) using peptide as substrate in presence of ATP by homogeneous time-resolved fluorescence assay B 8.24 pIC50 5.7 nM IC50 Eur J Med Chem (2022) 239: 114551-114551 [PMID:35749986]
ChEMBL Inhibition of JAK2 (unknown origin) B 8.24 pIC50 5.7 nM IC50 J Med Chem (2023) 66: 5753-5773 [PMID:37057760]
ChEMBL Inhibition of JAK2 (unknown origin) B 8.24 pIC50 5.7 nM IC50 Eur J Med Chem (2023) 261: 115848-115848 [PMID:37793326]
ChEMBL Inhibition of recombinant JAK2 (unknown origin) (828 to 1132 residues) in presence of ATP by homogeneous time-resolved fluorescence assay B 8.24 pIC50 5.7 nM IC50 Eur J Med Chem (2024) 267: 116210-116210 [PMID:38359535]
ChEMBL Inhibition of JAK2 (unknown origin) B 8.24 pIC50 5.7 nM IC50 Eur J Med Chem (2024) 275: 116540-116540 [PMID:38852338]
ChEMBL Inhibition of JAK: The study of the effect of compounds on the activity of purified recombinant JAK was performed by studying the inhibitory activity of the compounds on JAK from the enzymatic level. The experimental principle is to use a luminescence kinase assay to detect the ADP content produced by the reaction of JAK with the substrate Poly (4:1 Glu, Tyr) peptide: after ADP is converted to ATP, ATP can act as a substrate for the Ultra-Glo luciferase catalytic reaction, producing an optical signal. The luminescence signal is positively correlated with the amount of ADP and kinase activity. Therefore, the inhibitory effect of the compounds on the recombinant JAK was determined by observing the luminescence signal produced by the reaction of JAK and the substrate, and was expressed by IC50. B 8.26 pIC50 5.5 nM IC50 US-11414413-B2. Heterocyclic compound as JAK inhibitor, and salts and therapeutic use thereof (2022)
ChEMBL Kinase Assay: A kinase selectivity panel which measures substrate peptide phosphorylation was set-up for recombinant human Jak1 (aa 866-1154), Jak2 (aa808-1132), Jak3 (aa811-1124) and Tyk2 (aa888-1187). The technology used for the described assay is based on the separation and quantification of substrate and product in an electrical field. In the course of the kinase reaction the peptide substrate is phosphorylated by a kinase. The transfer of a phosphate residue also causes the introduction of two additional negative charges and hence to a change in the net charge of the phospho-peptide compared to the unphosphorylated peptide. Due to this difference in charge the phosphorylated und unphosphorylated peptides migrate with different velocities in an electrical field.In the applied method, this separation takes place inside a chip that contains a complex capillary system for simultaneous analysis of 12 samples (12-sipper chip, Caliper Technologies Corp., Mountain View, USA). In order to allow the detection and quantification of the peptides in the capillary system, the peptides carry a fluorescent label (fluorescein). With this label the peptides can be quantified by fluorescence intensity through the instruments laser and detection system (LC3000, Caliper Life Sciences).The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ß-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35.Plates with terminated kinase reactions were transferred to the Caliper LC3000 workstation (Caliper Technologies Corp., Mountain View, USA) for reading. The relative amount of phosphorylated peptide r, was calculated using the heights of the substrate peak, s, and the product peak, p: r=p/(p+s). B 8.4 pIC50 4 nM IC50 US-10112907-B2. Substituted indazoles for treating tendon and/or ligament injuries (2018)
ChEMBL Biochemical Activity Assay: The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ß-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35. B 8.4 pIC50 4 nM IC50 US-10766894-B2. Aza-indazole compounds for use in tendon and/or ligament injuries (2020)
ChEMBL Biochemical Activity Assay: The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ��-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35. B 8.4 pIC50 4 nM IC50 US-11203595-B2. Aza-indazole compounds for use in tendon and/or ligament injuries (2021)
ChEMBL Inhibition of JAK2 JH1 domain (unknown origin) using Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK peptide as substrate incubated for 60 mins in the presence of ATP by caliper microfluidic mobility shift technology B 8.54 pIC50 2.9 nM IC50 J Med Chem (2023) 66: 2161-2168 [PMID:36657024]
ChEMBL Inhibition of JAK2 (unknown origin) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent substrate phosphorylation after 45 mins by TR-FRET assay B 9.1 pIC50 0.8 nM IC50 J Med Chem (2016) 59: 733-749 [PMID:26701356]
ChEMBL Inhibition of human JAK2 by radiometric assay B 9.54 pIC50 0.29 nM IC50 J Med Chem (2021) 64: 2228-2241 [PMID:33570945]
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
ChEMBL Inhibition of recombinant human JAK3 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay B 5.1 pIC50 >=8000 nM IC50 J Med Chem (2018) 61: 1130-1152 [PMID:29298069]
GtoPdb - - 6.1 pIC50 787 nM IC50 J Med Chem (2014) 57: 5023-38 [PMID:24417533]
ChEMBL Inhibition of JAK3 (unknown origin) B 6.1 pIC50 787 nM IC50 J Med Chem (2014) 57: 5023-5038 [PMID:24417533]
ChEMBL Inhibition of recombinant human N-terminal His-tagged JAK3 (795 to 1124 residues) expressed in baculovirus expression system B 6.1 pIC50 787 nM IC50 Eur J Med Chem (2021) 218: 113394-113394 [PMID:33813153]
ChEMBL Inhibition of JAK3 (unknown origin) B 6.1 pIC50 787 nM IC50 Bioorg Med Chem (2016) 24: 2660-2672 [PMID:27137359]
ChEMBL Inhibition of JAK3 (unknown origin) using TK-substrate-biotin as substrate preincubated for 5 mins followed by substrate addition and measured by 30 mins by HTRF assay B 6.25 pIC50 560 nM IC50 Bioorg Med Chem (2019) 27: 2592-2597 [PMID:30926315]
ChEMBL Inhibition of JAK: The study of the effect of compounds on the activity of purified recombinant JAK was performed by studying the inhibitory activity of the compounds on JAK from the enzymatic level. The experimental principle is to use a luminescence kinase assay to detect the ADP content produced by the reaction of JAK with the substrate Poly (4:1 Glu, Tyr) peptide: after ADP is converted to ATP, ATP can act as a substrate for the Ultra-Glo luciferase catalytic reaction, producing an optical signal. The luminescence signal is positively correlated with the amount of ADP and kinase activity. Therefore, the inhibitory effect of the compounds on the recombinant JAK was determined by observing the luminescence signal produced by the reaction of JAK and the substrate, and was expressed by IC50. B 6.4 pIC50 >400 nM IC50 US-11414413-B2. Heterocyclic compound as JAK inhibitor, and salts and therapeutic use thereof (2022)
ChEMBL Inhibition of JAK3 (unknown origin) B 6.4 pIC50 >400 nM IC50 J Med Chem (2015) 58: 7596-7602 [PMID:26351728]
ChEMBL Inhibition of recombinant epitope tagged JAK3 kinase domain (718 to 1124 residues) (unknown origin) using peptide substrate by fluorescence based assay B 6.4 pIC50 >400 nM IC50 Bioorg Med Chem (2019) 27: 2592-2597 [PMID:30926315]
ChEMBL Inhibition of recombinant epitope tagged JAK3 (unknown origin) (718 to 1124 residues) using peptide substrate in presence of ATP by time-resolved fluorescence assay B 6.4 pIC50 >400 nM IC50 J Med Chem (2023) 66: 6725-6742 [PMID:37163463]
ChEMBL Inhibition of recombinant epitope tagged JAK3 (unknown origin) (718 to 1124 residues) using peptide as substrate in presence of ATP by homogeneous time-resolved fluorescence assay B 6.4 pIC50 >400 nM IC50 Eur J Med Chem (2022) 239: 114551-114551 [PMID:35749986]
ChEMBL Inhibition of recombinant JAK3 (unknown origin) (718 to 1124 residues) in presence of ATP by homogeneous time-resolved fluorescence assay B 6.4 pIC50 >400 nM IC50 Eur J Med Chem (2024) 267: 116210-116210 [PMID:38359535]
ChEMBL Kinase Assay: A kinase selectivity panel which measures substrate peptide phosphorylation was set-up for recombinant human Jak1 (aa 866-1154), Jak2 (aa808-1132), Jak3 (aa811-1124) and Tyk2 (aa888-1187). The technology used for the described assay is based on the separation and quantification of substrate and product in an electrical field. In the course of the kinase reaction the peptide substrate is phosphorylated by a kinase. The transfer of a phosphate residue also causes the introduction of two additional negative charges and hence to a change in the net charge of the phospho-peptide compared to the unphosphorylated peptide. Due to this difference in charge the phosphorylated und unphosphorylated peptides migrate with different velocities in an electrical field.In the applied method, this separation takes place inside a chip that contains a complex capillary system for simultaneous analysis of 12 samples (12-sipper chip, Caliper Technologies Corp., Mountain View, USA). In order to allow the detection and quantification of the peptides in the capillary system, the peptides carry a fluorescent label (fluorescein). With this label the peptides can be quantified by fluorescence intensity through the instruments laser and detection system (LC3000, Caliper Life Sciences).The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ß-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35.Plates with terminated kinase reactions were transferred to the Caliper LC3000 workstation (Caliper Technologies Corp., Mountain View, USA) for reading. The relative amount of phosphorylated peptide r, was calculated using the heights of the substrate peak, s, and the product peak, p: r=p/(p+s). B 6.6 pIC50 250 nM IC50 US-10112907-B2. Substituted indazoles for treating tendon and/or ligament injuries (2018)
ChEMBL Biochemical Activity Assay: The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ß-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35. B 6.6 pIC50 250 nM IC50 US-10766894-B2. Aza-indazole compounds for use in tendon and/or ligament injuries (2020)
ChEMBL Biochemical Activity Assay: The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ��-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35. B 6.6 pIC50 250 nM IC50 US-11203595-B2. Aza-indazole compounds for use in tendon and/or ligament injuries (2021)
ChEMBL Inhibition of JAK3 JH1 domain (unknown origin) using Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK peptide as substrate incubated for 60 mins in the presence of ATP by caliper microfluidic mobility shift technology B 6.75 pIC50 178 nM IC50 J Med Chem (2023) 66: 2161-2168 [PMID:36657024]
ChEMBL Inhibition of JAK3 (unknown origin) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent substrate phosphorylation after 45 mins by TR-FRET assay B 7.6 pIC50 25 nM IC50 J Med Chem (2016) 59: 733-749 [PMID:26701356]
LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lck in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
tec protein tyrosine kinase/Tyrosine-protein kinase Tec in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4246] [GtoPdb: 2238] [UniProtKB: P42680]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
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 Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Tyrosine--tRNA ligase, cytoplasmic in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3179] [UniProtKB: P54577]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
U5 small nuclear ribonucleoprotein 200 kDa helicase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105972] [UniProtKB: O75643]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
UMP-CMP kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5681] [UniProtKB: P30085]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
aarF domain containing kinase 5/Uncharacterized aarF domain-containing protein kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105886] [GtoPdb: 1929] [UniProtKB: Q3MIX3]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
Uncharacterized protein FLJ45252 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105933] [UniProtKB: Q6ZSR9]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 7.11 pKd 78 nM Kd Science (2017) 358: null-null [PMID:29191878]
Very long-chain specific acyl-CoA dehydrogenase, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105892] [UniProtKB: P49748]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]
WEE1 G2 checkpoint kinase/Wee1-like protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5491] [GtoPdb: 2278] [UniProtKB: P30291]
ChEMBL Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. B 4.52 pKd >30000 nM Kd Science (2017) 358: null-null [PMID:29191878]

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]