NMS-P715 [Ligand Id: 9401] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1236095
  • 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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  • tyrosine kinase non receptor 2/Activated CDC42 kinase 1 in Human [ChEMBL: CHEMBL4599] [GtoPdb: 2246] [UniProtKB: Q07912]
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  • ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
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  • casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II subunit alpha in Human [ChEMBL: CHEMBL3629] [GtoPdb: 1549] [UniProtKB: P68400]
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  • cell division cycle 7/CDC7/DBF4 (Cell division cycle 7-related protein kinase/Activator of S phase kinase) in Human [ChEMBL: CHEMBL2111377] [GtoPdb: 1960] [UniProtKB: O00311, Q9UBU7]
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  • cell division cycle 7/Cell division cycle 7-related protein kinase in Human [ChEMBL: CHEMBL5443] [GtoPdb: 1960] [UniProtKB: O00311]
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  • cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078]
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  • TTK protein kinase/Dual specificity protein kinase TTK in Human [ChEMBL: CHEMBL3983] [GtoPdb: 2264] [UniProtKB: P33981]
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  • epidermal growth factor receptor/Epidermal growth factor receptor in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • eukaryotic elongation factor 2 kinase/Eukaryotic elongation factor 2 kinase in Human [ChEMBL: CHEMBL5026] [GtoPdb: 2014] [UniProtKB: O00418]
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  • eukaryotic translation initiation factor 2 alpha kinase 3/Eukaryotic translation initiation factor 2-alpha kinase 3 in Human [ChEMBL: CHEMBL6030] [GtoPdb: 2017] [UniProtKB: Q9NZJ5]
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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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  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
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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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  • High affinity immunoglobulin gamma Fc receptor I in Human [ChEMBL: CHEMBL5349] [UniProtKB: P12314]
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  • neurotrophic receptor tyrosine kinase 1/High affinity nerve growth factor receptor in Human [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629]
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  • component of inhibitor of nuclear factor kappa B kinase complex/Inhibitor of nuclear factor kappa-B kinase subunit alpha in Human [ChEMBL: CHEMBL3476] [GtoPdb: 1989] [UniProtKB: O15111]
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  • inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa-B kinase subunit beta in Human [ChEMBL: CHEMBL1991] [GtoPdb: 2039] [UniProtKB: O14920]
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  • MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137]
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  • MAPK interacting serine/threonine kinase 2/MAP kinase-interacting serine/threonine-protein kinase 2 in Human [ChEMBL: CHEMBL4204] [GtoPdb: 2105] [UniProtKB: Q9HBH9]
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  • KIT proto-oncogene, receptor tyrosine kinase/Mast/stem cell growth factor receptor Kit in Human [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
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  • maternal embryonic leucine zipper kinase/Maternal embryonic leucine zipper kinase in Human [ChEMBL: CHEMBL4578] [GtoPdb: 2102] [UniProtKB: Q14680]
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  • 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 14/Mitogen-activated protein kinase 14 in Human [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
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  • BUB1 mitotic checkpoint serine/threonine kinase/Mitotic checkpoint serine/threonine-protein kinase BUB1 in Human [ChEMBL: CHEMBL1772932] [GtoPdb: 1949] [UniProtKB: O43683]
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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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  • platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234]
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  • protein kinase C alpha/Protein kinase C alpha 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 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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  • pyruvate dehydrogenase kinase 1/[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial in Human [ChEMBL: CHEMBL4766] [GtoPdb: 2915] [UniProtKB: Q15118]
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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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  • fms related receptor tyrosine kinase 3/Receptor-type tyrosine-protein kinase FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
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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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  • checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757]
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  • histone H3 associated protein kinase/Serine/threonine-protein kinase haspin in Human [ChEMBL: CHEMBL1075163] [GtoPdb: 2028] [UniProtKB: Q8TF76]
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  • NIMA related kinase 6/Serine/threonine-protein kinase Nek6 in Human [ChEMBL: CHEMBL4309] [GtoPdb: 2121] [UniProtKB: Q9HC98]
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  • serine/threonine-protein kinase NIM1/Serine/threonine-protein kinase NIM1 in Human [ChEMBL: CHEMBL3542] [GtoPdb: 2291] [UniProtKB: Q8IY84]
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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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  • Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-1 in Human [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309]
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  • Pim-2 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-2 in Human [ChEMBL: CHEMBL4523] [GtoPdb: 2159] [UniProtKB: Q9P1W9]
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  • polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350]
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  • polo like kinase 2/Serine/threonine-protein kinase PLK2 in Human [ChEMBL: CHEMBL5938] [GtoPdb: 2169] [UniProtKB: Q9NYY3]
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  • polo like kinase 3/Serine/threonine-protein kinase PLK3 in Human [ChEMBL: CHEMBL4897] [GtoPdb: 2170] [UniProtKB: Q9H4B4]
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  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL1 in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
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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 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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  • zeta chain of T cell receptor associated protein kinase 70/Tyrosine-protein kinase ZAP-70 in Human [ChEMBL: CHEMBL2803] [GtoPdb: 2285] [UniProtKB: P43403]
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  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
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  • fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a PRKAA1 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
tyrosine kinase non receptor 2/Activated CDC42 kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4599] [GtoPdb: 2246] [UniProtKB: Q07912]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a TNK2 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant ACK1 (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
ChEMBL Inhibition of recombinant ALK (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
aurora kinase A/Aurora kinase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
ChEMBL Inhibition of N-terminal His-tagged Aurora A (unknown origin) using 5FAM-LRRASLG-CONH2 as substrate after 60 mins by fluorescence assay B 4.52 pIC50 >30000 nM IC50 J Med Chem (2013) 56: 10045-10065 [PMID:24256217]
ChEMBL Inhibition of Aur-A assessed as [33P]-gamma-ATP incorporation into substrate by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 4507-4511 [PMID:21723120]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a STK6 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
aurora kinase B/Aurora kinase B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a AURKB B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3629] [GtoPdb: 1549] [UniProtKB: P68400]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a CSNK2A1 B 5.24 pIC50 5700 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
cell division cycle 7/CDC7/DBF4 (Cell division cycle 7-related protein kinase/Activator of S phase kinase) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111377] [GtoPdb: 1960] [UniProtKB: O00311, Q9UBU7]
ChEMBL Inhibition of recombinant CDC7/DBF4 (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
cyclin dependent kinase 2/CDK2/Cyclin A2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038469] [GtoPdb: 1973] [UniProtKB: P20248, P24941]
ChEMBL Inhibition of full length CDK2/Cyclin A (unknown origin) using 5FAMQSPKKG-CONH2 as substrate after 60 mins by fluorescence assay B 4 pIC50 >100000 nM IC50 J Med Chem (2013) 56: 10045-10065 [PMID:24256217]
cell division cycle 7/Cell division cycle 7-related protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5443] [GtoPdb: 1960] [UniProtKB: O00311]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a CDC7 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094127] [GtoPdb: 1961] [UniProtKB: O95067, P06493, P14635, Q8WWL7]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a CDK1 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907602] [GtoPdb: 1961] [UniProtKB: P06493, P14635]
ChEMBL Inhibition of recombinant CDK1/CYCB (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094128] [GtoPdb: 1973] [UniProtKB: P20248, P24941, P78396]
ChEMBL Inhibition of CDK2/Cyclin A assessed as [33P]-gamma-ATP incorporation into substrate by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 4507-4511 [PMID:21723120]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a CDK2 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094126] [GtoPdb: 1973] [UniProtKB: O96020, P24864, P24941]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a CDK2 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907605] [GtoPdb: 1973] [UniProtKB: P24864, P24941]
ChEMBL Inhibition of recombinant CDK2/CYCE1 (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
cyclin dependent kinase 4/Cyclin-dependent kinase 4/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907601] [GtoPdb: 1976] [UniProtKB: P11802, P24385]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a CDK4 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant CDK4/CYCD1 (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a CDK5 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant CDK5/P25 (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
TTK protein kinase/Dual specificity protein kinase TTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3983] [GtoPdb: 2264] [UniProtKB: P33981]
ChEMBL Binding affinity to recombinant human MPS1 assessed as dissociation constant B 8.87 pKd 1.34 nM Kd Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
ChEMBL Affinity Biochemical interaction: (Enzymatic activity assay) EUB0000612a TTK B 9 pKi 0.99 nM Ki Affinity Biochemical Literature for EUbOPEN Chemogenomic Library
ChEMBL Time-dependent inhibition of full length N-terminal GST-tagged human recombinant MPS1 (2 to 857 residues) assessed as inhibition constant in presence of ATP B 9 pKi 0.99 nM Ki Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
ChEMBL Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using LS-174Tcell line, 72 h incubation)) EUB0000612a TTK F 5.71 pIC50 1955 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using MDA-MB-435S cell line, 72 h incubation)) EUB0000612a TTK F 5.71 pIC50 1955 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using LOVO cell line, 72 h incubation)) EUB0000612a TTK F 5.73 pIC50 1870 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using MCF-7 cell line, 72 h incubation)) EUB0000612a TTK F 5.73 pIC50 1860 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using SF295 cell line, 72 h incubation)) EUB0000612a TTK F 5.74 pIC50 1821 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using HCC2998 cell line, 72 h incubation)) EUB0000612a TTK F 5.74 pIC50 1813 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using SW403 cell line, 72 h incubation)) EUB0000612a TTK F 5.8 pIC50 1569 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using CL-11 cell line, 72 h incubation)) EUB0000612a TTK F 5.88 pIC50 1323 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using SW480 cell line, 72 h incubation)) EUB0000612a TTK F 5.89 pIC50 1298 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using COLO-320 cell line, 72 h incubation)) EUB0000612a TTK F 5.89 pIC50 1284 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using COLO-206F cell line, 72 h incubation)) EUB0000612a TTK F 5.91 pIC50 1239 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using BT-474 cell line, 72 h incubation)) EUB0000612a TTK F 5.94 pIC50 1157 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using IGROV-1cell line, 72 h incubation)) EUB0000612a TTK F 5.94 pIC50 1152 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using BT-549 cell line, 72 h incubation)) EUB0000612a TTK F 5.98 pIC50 1049 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using ACHN cell line, 72 h incubation)) EUB0000612a TTK F 5.99 pIC50 1015 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using A2780 cell line, 72 h incubation)) EUB0000612a TTK F 6 pIC50 1000 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using 786-0 cell line, 72 h incubation)) EUB0000612a TTK F 6.04 pIC50 917 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using MDA-MB-231 cell line, 72 h incubation)) EUB0000612a TTK F 6.05 pIC50 899 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using SU-DHL-6 cell line, 72 h incubation)) EUB0000612a TTK F 6.08 pIC50 829 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using SF295 cell line, 72 h incubation)) EUB0000612a TTK F 6.09 pIC50 807 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using A375 cell line, 72 h incubation)) EUB0000612a TTK F 6.1 pIC50 796 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using M14 cell line, 72 h incubation)) EUB0000612a TTK F 6.16 pIC50 698 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using A431 cell line, 72 h incubation)) EUB0000612a TTK F 6.21 pIC50 619 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using Colo-205 cell line, 72 h incubation)) EUB0000612a TTK F 6.23 pIC50 592 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using KM12 cell line, 72 h incubation)) EUB0000612a TTK F 6.23 pIC50 586 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using SW48 cell line, 72 h incubation)) EUB0000612a TTK F 6.26 pIC50 551 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using SW620 cell line, 72 h incubation)) EUB0000612a TTK F 6.28 pIC50 519 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using HCT-116 cell line, 72 h incubation)) EUB0000612a TTK F 6.33 pIC50 472 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using U251 cell line, 72 h incubation)) EUB0000612a TTK F 6.33 pIC50 469 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, inhibition of cell growth in HCT15 cells)) EUB0000612a TTK F 6.63 pIC50 232 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using MOLT4 cell line, 72 h incubation)) EUB0000612a TTK F 6.72 pIC50 192 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant MPS1 (unknown origin) B 6.74 pIC50 182 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
ChEMBL Inhibition of MPS1 (unknown origin) B 6.74 pIC50 182 nM IC50 Eur J Med Chem (2019) 175: 247-268 [PMID:31121430]
ChEMBL Inhibition of full-length MPS1 (unknown origin) in presence of ATP B 6.74 pIC50 182 nM IC50 J Med Chem (2023) 66: 16484-16514 [PMID:38095579]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a TTK B 6.74 pIC50 182 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of full length N-terminal GST-tagged human recombinant MPS1 (2 to 857 residues) in presence of ATP B 6.74 pIC50 182 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
ChEMBL Inhibition of MPS1 assessed as [33P]-gamma-ATP incorporation into substrate P38-betatide by gamma counting B 6.74 pIC50 182 nM IC50 Bioorg Med Chem Lett (2011) 21: 4507-4511 [PMID:21723120]
GtoPdb - - 6.74 pIC50 182 nM IC50 Bioorg Med Chem Lett (2011) 21: 4507-11 [PMID:21723120]
ChEMBL Inhibition of Myc-tagged wild type MPS1 autophosphorylation in human HCT116 cells after 2 hrs in presence of proteosome inhibitor MG132 B 6.8 pIC50 160 nM IC50 J Med Chem (2013) 56: 10045-10065 [PMID:24256217]
ChEMBL Inhibition of recombinant Mps1 (519-808 residues) (unknown origin) incubated for 10 min by invitro kinase assay B 7.15 pIC50 71.3 nM IC50 Oncogene (2016) 35: 2518-2528 [PMID:26364596]
ChEMBL Competitive inhibition of full length N-terminal GST-tagged human recombinant MPS1 (2 to 857 residues) in presence of 90 uM ATP incubated for 60 mins B 7.21 pIC50 61.4 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
ChEMBL Competitive inhibition of full length N-terminal GST-tagged human recombinant MPS1 (2 to 857 residues) in presence of 30 uM ATP incubated for 60 mins B 7.6 pIC50 24.9 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
ChEMBL Inhibition of MPS1 (unknown origin) B 8.1 pIC50 8 nM IC50 J Med Chem (2013) 56: 4343-4356 [PMID:23634759]
ChEMBL Selectivity interaction (Enzymatic assay) EUB0000612a TTK B 8.1 pIC50 8 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Competitive inhibition of full length N-terminal GST-tagged human recombinant MPS1 (2 to 857 residues) in presence of 10 uM ATP incubated for 60 mins B 8.12 pIC50 7.6 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
ChEMBL Inhibition of N-terminal 6XHis-tagged/GST-tagged full length human MPS1 expressed in recombinant baculovirus infected sf9 insect cells using 5FAM-DHTGFLTEYVATRCONH2 as substrate after 60 to 90 mins by fluorescence assay B 8.15 pIC50 7 nM IC50 J Med Chem (2013) 56: 10045-10065 [PMID:24256217]
ChEMBL Competitive inhibition of full length N-terminal GST-tagged human recombinant MPS1 (2 to 857 residues) in presence of 3.3 uM ATP incubated for 60 mins B 8.31 pIC50 4.9 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
ChEMBL TTK Enzyme Assay: The inhibitory activity of compounds on biochemically purified full-length TTK (Life Technologies, Madison, Wis., U.S.A.) was determined in the IMAP® assay (Molecular Devices, Sunnyvale, Calif., U.S.A.). Compounds were dissolved in 100% dimethylsulfoxide (DMSO). At the day of the experiment, the compound stock was diluted in 3.16 fold steps in 100% DMSO, to obtain a 10-point dilution series, followed by further dilution in IMAP reaction buffer, which consists of 10 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 0.01% Tween-20, 0.1% NaN3 and 1 mM freshly prepared dithiothreitol. Compound solution was mixed with an equal volume of full-length TTK enzyme in IMAP reaction buffer. After pre-incubation of 1 hour in the dark at room temperature, fluorescein-labeled MBP-derived substrate peptide (Molecular Devices) was added and ATP to start the reaction. Final enzyme concentration was 3.9 nM, final substrate concentration 50 nM, and final ATP concentration was 5 μM. The reaction was allowed to proceed for 2 hours at room temperature in the dark. The reaction was stopped by quenching with IMAP progressive binding solution according to the protocol of the manufacturer (Molecular Devices). Fluorescein polarization was measured on an Envision multimode reader (Perkin Elmer, Waltham, Mass., USA). Dose-response curves were fitted to a four-parameter logarithmic equation in XLfit™ 5 (ID Business Solutions, Ltd., Guildford, U.K.). B 9.2 pIC50 0.63 nM IC50 US-11208696-B2. Prognostic biomarkers for TTK inhibitor chemotherapy (2021)
ChEMBL Affinity On-target Cellular interaction: (ArrayScan analysis of histone H3 Ser10 phosphorylation in nocodazole-arrested U20S cells) EUB0000612a TTK B 7.19 pEC50 65 nM EC50 Affinity On-target Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of MPS1 in human nocodazole-arrested U2OS cells assessed as effect on histone H3 phosphorylation at ser10 residue incubated for 2 hrs by arrayscan analysis B 7.19 pEC50 65 nM EC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
epidermal growth factor receptor/Epidermal growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a EGFR B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant EGFR1 (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
eukaryotic elongation factor 2 kinase/Eukaryotic elongation factor 2 kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5026] [GtoPdb: 2014] [UniProtKB: O00418]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a EEF2K B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant EEF2K (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
eukaryotic translation initiation factor 2 alpha kinase 3/Eukaryotic translation initiation factor 2-alpha kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6030] [GtoPdb: 2017] [UniProtKB: Q9NZJ5]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a EIF2AK3 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant PERK (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a FGFR1 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant FGFR1 (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
protein tyrosine kinase 2/Focal adhesion kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a PTK2 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant FAK (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a GSK3B B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant GSK3beta (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a MET B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
High affinity immunoglobulin gamma Fc receptor I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5349] [UniProtKB: P12314]
ChEMBL Inhibition of recombinant IGFR1 (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
neurotrophic receptor tyrosine kinase 1/High affinity nerve growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a NTRK1 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant TRKA (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
component of inhibitor of nuclear factor kappa B kinase complex/Inhibitor of nuclear factor kappa-B kinase subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3476] [GtoPdb: 1989] [UniProtKB: O15111]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a CHUK B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa-B kinase subunit beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1991] [GtoPdb: 2039] [UniProtKB: O14920]
ChEMBL Inhibition of recombinant IKK2 (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a INSR B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant IR (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a MAPKAPK2 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant MAPKAPK2 (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
MAPK interacting serine/threonine kinase 2/MAP kinase-interacting serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4204] [GtoPdb: 2105] [UniProtKB: Q9HBH9]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a MKNK2 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant MNK2 (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
KIT proto-oncogene, receptor tyrosine kinase/Mast/stem cell growth factor receptor Kit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a KIT B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant KIT (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
maternal embryonic leucine zipper kinase/Maternal embryonic leucine zipper kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4578] [GtoPdb: 2102] [UniProtKB: Q14680]
ChEMBL Inhibition of recombinant MELK (unknown origin) preincubated for 60 mins B 5 pIC50 <10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a MELK B 5.22 pIC50 6010 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant MELK (unknown origin) B 5.22 pIC50 6010 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
mitogen-activated protein kinase 1/Mitogen-activated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a MAPK1 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant ERK2 (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
mitogen-activated protein kinase 14/Mitogen-activated protein kinase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a MAPK14 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant P38alpha (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
BUB1 mitotic checkpoint serine/threonine kinase/Mitotic checkpoint serine/threonine-protein kinase BUB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1772932] [GtoPdb: 1949] [UniProtKB: O43683]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a BUB1 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant BUB1 (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
tyrosine kinase 2/Non-receptor tyrosine-protein kinase TYK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a TYK2 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant TYK 2 (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a PDGFRA B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
protein kinase C alpha/Protein kinase C alpha type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252]
ChEMBL Inhibition of recombinant PKAalpha (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
protein kinase C beta/Protein kinase C beta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a PRKCB B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant PKCbeta (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
protein tyrosine kinase 6/Protein-tyrosine kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4601] [GtoPdb: 2182] [UniProtKB: Q13882]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a PTK6 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant BRK (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
ret proto-oncogene/Proto-oncogene tyrosine-protein kinase receptor Ret in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a RET B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant RET (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
pyruvate dehydrogenase kinase 1/[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4766] [GtoPdb: 2915] [UniProtKB: Q15118]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a PDK1 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant PDK1 (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
AKT serine/threonine kinase 1/RAC-alpha serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a AKT1 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant AKT1 (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
fms related receptor tyrosine kinase 3/Receptor-type tyrosine-protein kinase FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a FLT3 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant FLT3 (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
SAFB-like transcription modulator in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523469] [UniProtKB: Q9NWH9]
ChEMBL Inhibition of recombinant MET (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
serine/threonine-protein kinase MST4/Serine/threonine-protein kinase 26 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5941] [GtoPdb: 2287] [UniProtKB: Q9P289]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a STK26 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant MST4 (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a CHEK1 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant CHK1 (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
histone H3 associated protein kinase/Serine/threonine-protein kinase haspin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075163] [GtoPdb: 2028] [UniProtKB: Q8TF76]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a GSG2 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant Haspin (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
NIMA related kinase 6/Serine/threonine-protein kinase Nek6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4309] [GtoPdb: 2121] [UniProtKB: Q9HC98]
ChEMBL Inhibition of recombinant NEK6 (unknown origin) preincubated for 60 mins B 5 pIC50 <10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a NEK6 B 5.22 pIC50 6020 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant NEK6 (unknown origin) B 5.22 pIC50 6020 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
serine/threonine-protein kinase NIM1/Serine/threonine-protein kinase NIM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3542] [GtoPdb: 2291] [UniProtKB: Q8IY84]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a NIM1K B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant NIM1 (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
p21 (RAC1) activated kinase 4/Serine/threonine-protein kinase PAK 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4482] [GtoPdb: 2136] [UniProtKB: O96013]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a PAK4 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant PAK4 (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
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 Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a PIM1 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant PIM1 (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
Pim-2 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523] [GtoPdb: 2159] [UniProtKB: Q9P1W9]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a PIM2 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant PIM2 (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350]
ChEMBL Inhibition of PLK1 assessed as [33P]-gamma-ATP incorporation into substrate by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 4507-4511 [PMID:21723120]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a PLK1 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant PLK1 (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
polo like kinase 2/Serine/threonine-protein kinase PLK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5938] [GtoPdb: 2169] [UniProtKB: Q9NYY3]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a PLK2 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant PLK2 (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
polo like kinase 3/Serine/threonine-protein kinase PLK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4897] [GtoPdb: 2170] [UniProtKB: Q9H4B4]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a PLK3 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant PLK3 (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
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 Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a ABL1 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a JAK1 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant JAK1 (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a JAK3 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant JAK3 (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lck in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a LCK B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant LCK (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a LYN B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant LYN (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a SYK B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant SYK (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
zeta chain of T cell receptor associated protein kinase 70/Tyrosine-protein kinase ZAP-70 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2803] [GtoPdb: 2285] [UniProtKB: P43403]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a ZAP70 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant ZAP70 (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a KDR B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant VEGFR2 (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]
fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916]
ChEMBL Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a FLT4 B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant VEGFR3 (unknown origin) B 5 pIC50 >10000 nM IC50 Cancer Res (2010) 70: 10255-10264 [PMID:21159646]

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]