compound 8 [PMID: 17480064] [Ligand Id: 8763] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL225519 (PHA-767491)
  • ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
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  • protein kinase, cAMP-dependent, catalytic, alpha subunit/cAMP-dependent protein kinase alpha-catalytic subunit in Human [ChEMBL: CHEMBL4101] [GtoPdb: 1476] [UniProtKB: P17612]
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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 1/Cyclin-dependent kinase 1 in Human [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493]
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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 5/Cyclin-dependent kinase 5 in Human [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535]
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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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  • fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
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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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  • inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa B kinase beta subunit 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 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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  • mitogen-activated protein kinase 1/MAP kinase ERK2 in Human [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
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  • MAPK interacting serine/threonine kinase 1/MAP kinase-interacting serine/threonine-protein kinase MNK1 in Human [ChEMBL: CHEMBL4718] [GtoPdb: 2104] [UniProtKB: Q9BUB5]
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  • mitogen-activated protein kinase 11/MAP kinase p38 beta in Human [ChEMBL: CHEMBL3961] [GtoPdb: 1500] [UniProtKB: Q15759]
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  • MAPK interacting serine/threonine kinase 2/MAP kinase signal-integrating kinase 2 in Human [ChEMBL: CHEMBL4204] [GtoPdb: 2105] [UniProtKB: Q9HBH9]
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  • neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629]
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  • protein kinase C beta/Protein kinase C beta in Human [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771]
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  • pyruvate dehydrogenase kinase 1/Pyruvate dehydrogenase kinase isoform 1 in Human [ChEMBL: CHEMBL4766] [GtoPdb: 2915] [UniProtKB: Q15118]
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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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  • STE20 like kinase/Serine/threonine-protein kinase 2 in Human [ChEMBL: CHEMBL4202] [GtoPdb: 2200] [UniProtKB: Q9H2G2]
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  • AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
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  • aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
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  • aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
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  • checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757]
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  • checkpoint kinase 2/Serine/threonine-protein kinase Chk2 in Human [ChEMBL: CHEMBL2527] [GtoPdb: 1988] [UniProtKB: O96017]
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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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  • polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350]
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  • TAO kinase 3/Serine/threonine-protein kinase TAO3 in Human [ChEMBL: CHEMBL5701] [GtoPdb: 2235] [UniProtKB: Q9H2K8]
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  • KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
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  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
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  • LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
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  • ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
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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
ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
ChEMBL Inhibition of Alk B 5 pIC50 >10000 nM IC50 Nat Chem Biol (2008) 4: 357-365 [PMID:18469809]
protein kinase, cAMP-dependent, catalytic, alpha subunit/cAMP-dependent protein kinase alpha-catalytic subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4101] [GtoPdb: 1476] [UniProtKB: P17612]
ChEMBL Inhibition of PKAalpha B 5 pIC50 >10000 nM IC50 Nat Chem Biol (2008) 4: 357-365 [PMID:18469809]
cell division cycle 7/Cell division cycle 7-related protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5443] [GtoPdb: 1960] [UniProtKB: O00311]
ChEMBL Inhibition of human Cdc7 B 8 pIC50 10 nM IC50 J Med Chem (2008) 51: 487-501 [PMID:18201066]
ChEMBL Inhibition of human Cdc7 assessed as inhibition of rate of phosphorylation of Mcm2 protein B 8 pIC50 10 nM IC50 J Med Chem (2009) 52: 293-307 [PMID:19115845]
ChEMBL Inhibition of cdc7 B 8 pIC50 10 nM IC50 Nat Chem Biol (2008) 4: 357-365 [PMID:18469809]
ChEMBL Inhibition of Cdc7 B 8 pIC50 10 nM IC50 J Med Chem (2010) 53: 7296-7315 [PMID:20873740]
cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493]
ChEMBL Inhibition of cdk1 B 6.6 pIC50 250 nM IC50 Nat Chem Biol (2008) 4: 357-365 [PMID:18469809]
ChEMBL Inhibition of CDK2 B 6.77 pIC50 170 nM IC50 J Med Chem (2007) 50: 2647-2654 [PMID:17480064]
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
ChEMBL Inhibition of cdk2 B 6.62 pIC50 240 nM IC50 Nat Chem Biol (2008) 4: 357-365 [PMID:18469809]
cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535]
ChEMBL Inhibition of cdk5 B 6.34 pIC50 460 nM IC50 Nat Chem Biol (2008) 4: 357-365 [PMID:18469809]
cyclin dependent kinase 7/Cyclin-dependent kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3055] [GtoPdb: 1979] [UniProtKB: P50613]
ChEMBL Inhibition of Cdk7 B 5 pIC50 >10000 nM IC50 Nat Chem Biol (2008) 4: 357-365 [PMID:18469809]
cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750]
ChEMBL Inhibition of CDK9 B 7.47 pIC50 34 nM IC50 J Med Chem (2009) 52: 293-307 [PMID:19115845]
ChEMBL Inhibition of cdk9 B 7.47 pIC50 34 nM IC50 Nat Chem Biol (2008) 4: 357-365 [PMID:18469809]
fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
ChEMBL Inhibition of FGFR1 B 5 pIC50 >10000 nM IC50 Nat Chem Biol (2008) 4: 357-365 [PMID:18469809]
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
ChEMBL Inhibition of GSK3-beta B 6.66 pIC50 220 nM IC50 Nat Chem Biol (2008) 4: 357-365 [PMID:18469809]
MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
ChEMBL Inhibition of c-Met B 5 pIC50 >10000 nM IC50 Nat Chem Biol (2008) 4: 357-365 [PMID:18469809]
inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa B kinase beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1991] [GtoPdb: 2039] [UniProtKB: O14920]
ChEMBL Inhibition of IKK2 B 5 pIC50 >10000 nM IC50 J Med Chem (2007) 50: 2647-2654 [PMID:17480064]
ChEMBL Inhibition of IKK2 B 5 pIC50 >10000 nM IC50 Nat Chem Biol (2008) 4: 357-365 [PMID:18469809]
Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213]
ChEMBL Inhibition of IR B 5 pIC50 >10000 nM IC50 Nat Chem Biol (2008) 4: 357-365 [PMID:18469809]
MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137]
ChEMBL Inhibition of Mk2 B 6.33 pIC50 470 nM IC50 Nat Chem Biol (2008) 4: 357-365 [PMID:18469809]
ChEMBL Inhibition of MK2 B 6.77 pIC50 171 nM IC50 J Med Chem (2007) 50: 2647-2654 [PMID:17480064]
GtoPdb - - 6.77 pIC50 171 nM IC50 J Med Chem (2007) 50: 2647-54 [PMID:17480064]
MAPK activated protein kinase 3/MAP kinase-activated protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4670] [GtoPdb: 2095] [UniProtKB: Q16644]
ChEMBL Inhibition of MK3 B 4.24 pIC50 57700 nM IC50 J Med Chem (2007) 50: 2647-2654 [PMID:17480064]
MAPK activated protein kinase 5/MAP kinase-activated protein kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3094] [GtoPdb: 2096] [UniProtKB: Q8IW41]
ChEMBL Inhibition of MK5 B 6.3 pIC50 500 nM IC50 J Med Chem (2007) 50: 2647-2654 [PMID:17480064]
mitogen-activated protein kinase 1/MAP kinase ERK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
ChEMBL Inhibition of ERK2 B 5 pIC50 >10000 nM IC50 Nat Chem Biol (2008) 4: 357-365 [PMID:18469809]
MAPK interacting serine/threonine kinase 1/MAP kinase-interacting serine/threonine-protein kinase MNK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4718] [GtoPdb: 2104] [UniProtKB: Q9BUB5]
ChEMBL Inhibition of MNK1 B 5.57 pIC50 2670 nM IC50 J Med Chem (2007) 50: 2647-2654 [PMID:17480064]
ChEMBL Inhibition of MNK1 B 5.57 pIC50 2670 nM IC50 J Med Chem (2010) 53: 6618-6628 [PMID:20722422]
mitogen-activated protein kinase 11/MAP kinase p38 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3961] [GtoPdb: 1500] [UniProtKB: Q15759]
ChEMBL Inhibition of P38beta B 5 pIC50 >10000 nM IC50 Nat Chem Biol (2008) 4: 357-365 [PMID:18469809]
MAPK interacting serine/threonine kinase 2/MAP kinase signal-integrating kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4204] [GtoPdb: 2105] [UniProtKB: Q9HBH9]
ChEMBL Inhibition of MNK2 B 6.77 pIC50 171 nM IC50 J Med Chem (2010) 53: 6618-6628 [PMID:20722422]
neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629]
ChEMBL Inhibition of TRKA B 5 pIC50 >10000 nM IC50 Nat Chem Biol (2008) 4: 357-365 [PMID:18469809]
protein kinase C beta/Protein kinase C beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771]
ChEMBL Inhibition of PKCbeta B 5 pIC50 >10000 nM IC50 Nat Chem Biol (2008) 4: 357-365 [PMID:18469809]
pyruvate dehydrogenase kinase 1/Pyruvate dehydrogenase kinase isoform 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4766] [GtoPdb: 2915] [UniProtKB: Q15118]
ChEMBL Inhibition of PDK1 B 5 pIC50 >10000 nM IC50 Nat Chem Biol (2008) 4: 357-365 [PMID:18469809]
ribosomal protein S6 kinase A4/Ribosomal protein S6 kinase alpha 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3125] [GtoPdb: 1524] [UniProtKB: O75676]
GtoPdb - - 5.52 pIC50 3010 nM IC50 J Med Chem (2007) 50: 2647-54 [PMID:17480064]
ChEMBL Inhibition of MSK2 B 5.52 pIC50 3010 nM IC50 J Med Chem (2007) 50: 2647-2654 [PMID:17480064]
ribosomal protein S6 kinase A5/Ribosomal protein S6 kinase alpha 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4237] [GtoPdb: 1523] [UniProtKB: O75582]
ChEMBL Inhibition of MSK1 B 5.63 pIC50 2340 nM IC50 J Med Chem (2007) 50: 2647-2654 [PMID:17480064]
STE20 like kinase/Serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4202] [GtoPdb: 2200] [UniProtKB: Q9H2G2]
ChEMBL Inhibition of STLK2 B 5 pIC50 >10000 nM IC50 Nat Chem Biol (2008) 4: 357-365 [PMID:18469809]
AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
ChEMBL Inhibition of AKT1 B 5 pIC50 >10000