compound 38 [PMID: 20817473] [Ligand Id: 8768] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1258913
  • 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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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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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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  • High affinity immunoglobulin gamma Fc receptor I in Human [ChEMBL: CHEMBL5349] [UniProtKB: P12314]
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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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  • inhibitor of nuclear factor kappa B kinase subunit epsilon/Inhibitor of nuclear factor kappa B kinase epsilon subunit in Human [ChEMBL: CHEMBL3529] [GtoPdb: 2040] [UniProtKB: Q14164]
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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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  • mitogen-activated protein kinase 1/MAP kinase ERK2 in Human [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
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  • mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
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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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  • 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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  • aurora kinase C/Serine/threonine-protein kinase Aurora-C in Human [ChEMBL: CHEMBL3935] [GtoPdb: 1938] [UniProtKB: Q9UQB9]
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  • checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757]
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  • serine/threonine-protein kinase MST4/Serine/threonine-protein kinase MST4 in Human [ChEMBL: CHEMBL5941] [GtoPdb: 2287] [UniProtKB: Q9P289]
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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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  • 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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  • protein tyrosine kinase 6/Tyrosine-protein kinase BRK in Human [ChEMBL: CHEMBL4601] [GtoPdb: 2182] [UniProtKB: Q13882]
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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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  • 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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  • serine/threonine kinase 4 in Human [GtoPdb: 2225] [UniProtKB: Q13043]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 6.48 pIC50 332 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
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 CDC7 B 5.71 pIC50 1970 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094128] [GtoPdb: 1973] [UniProtKB: P20248P24941P78396]
ChEMBL Inhibition of CDK2/cyclinA B 5 pIC50 >10000 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibition of EGFR1 B 5 pIC50 >10000 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
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 7.85 pIC50 14 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
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 5 pIC50 >10000 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
ChEMBL Inhibition of MET B 5 pIC50 >10000 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
High affinity immunoglobulin gamma Fc receptor I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5349] [UniProtKB: P12314]
ChEMBL Inhibition of IGFR1 B 5 pIC50 >10000 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
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 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
inhibitor of nuclear factor kappa B kinase subunit epsilon/Inhibitor of nuclear factor kappa B kinase epsilon subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3529] [GtoPdb: 2040] [UniProtKB: Q14164]
ChEMBL Inhibition of IKKi B 5 pIC50 >10000 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213]
ChEMBL Inhibition of IR B 5.15 pIC50 7012 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137]
ChEMBL Inhibition of MAPKAPK2 B 5 pIC50 >10000 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
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 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
ChEMBL Inhibition of p38alpha B 5 pIC50 >10000 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
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 6.74 pIC50 181 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
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 5.92 pIC50 1212 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
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 6.12 pIC50 762 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
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 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
GtoPdb - - 7.74 pIC50 18 nM IC50 Bioorg Med Chem (2010) 18: 7113-20 [PMID:20817473]
ChEMBL Inhibition of AurA B 7.74 pIC50 18 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
ChEMBL Inhibition of aurora B B 7.35 pIC50 45 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
GtoPdb - - 7.35 pIC50 45 nM IC50 Bioorg Med Chem (2010) 18: 7113-20 [PMID:20817473]
aurora kinase C/Serine/threonine-protein kinase Aurora-C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3935] [GtoPdb: 1938] [UniProtKB: Q9UQB9]
ChEMBL Inhibition of aurora C B 7.21 pIC50 62 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
GtoPdb - - 7.21 pIC50 62 nM IC50 Bioorg Med Chem (2010) 18: 7113-20 [PMID:20817473]
checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757]
ChEMBL Inhibition of CHK1 B 5.79 pIC50 1634 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
serine/threonine-protein kinase MST4/Serine/threonine-protein kinase MST4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5941] [GtoPdb: 2287] [UniProtKB: Q9P289]
ChEMBL Inhibition of MST4 B 6.39 pIC50 412 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
serine/threonine-protein kinase NIM1/Serine/threonine-protein kinase NIM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3542] [GtoPdb: 2291] [UniProtKB: Q8IY84]
ChEMBL Inhibition of NIM1 B 5 pIC50 >10000 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
p21 (RAC1) activated kinase 4/Serine/threonine-protein kinase PAK 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4482] [GtoPdb: 2136] [UniProtKB: O96013]
ChEMBL Inhibition of PAK4 B 6.34 pIC50 455 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
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 B 5 pIC50 >10000 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
ChEMBL Inhibition of KIT B 7.46 pIC50 35 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
ChEMBL Inhibition of ABL B 5 pIC50 >10000 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
protein tyrosine kinase 6/Tyrosine-protein kinase BRK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4601] [GtoPdb: 2182] [UniProtKB: Q13882]
ChEMBL Inhibition of BRK B 5 pIC50 >10000 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
ChEMBL Inhibition of JAK2 B 5.76 pIC50 1721 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
ChEMBL Inhibition of JAK3 B 5.43 pIC50 3710 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
ChEMBL Inhibition of LCK B 5 pIC50 >10000 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948]
ChEMBL Inhibition of LYN B 5 pIC50 >10000 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
ChEMBL Inhibition of RET B 6.95 pIC50 113 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
zeta chain of T cell receptor associated protein kinase 70/Tyrosine-protein kinase ZAP-70 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2803] [GtoPdb: 2285] [UniProtKB: P43403]
ChEMBL Inhibition of ZAP70 B 5 pIC50 >10000 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
ChEMBL Inhibition of VEGFR2 B 6.79 pIC50 162 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916]
ChEMBL Inhibition of VEGFR3 B 7.72 pIC50 19 nM IC50 Bioorg Med Chem (2010) 18: 7113-7120 [PMID:20817473]
serine/threonine kinase 4 in Human [GtoPdb: 2225] [UniProtKB: Q13043]
GtoPdb - - 6.39 pIC50 412 nM IC50 Bioorg Med Chem (2010) 18: 7113-20 [PMID:20817473]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]