VTX-11e [Ligand Id: 9375] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL583042
  • citron rho-interacting serine/threonine kinase/Citron Rho-interacting kinase in Human [ChEMBL: CHEMBL5579] [GtoPdb: 1509] [UniProtKB: O14578]
  • This target only has 1 pki data point
  • 5
1 CHEMBL583042_lig_chart_1 Citron Rho-interacting kinase Human
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  • mitogen-activated protein kinase 10/c-Jun N-terminal kinase 3 in Human [ChEMBL: CHEMBL2637] [GtoPdb: 1498] [UniProtKB: P53779]
  • This target only has 1 pki data point
  • 5.85
2 CHEMBL583042_lig_chart_2 c-Jun N-terminal kinase 3 Human
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  • cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
  • 6.07
3 CHEMBL583042_lig_chart_3 Cyclin-dependent kinase 2 Human
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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]
  • This target only has 1 pki data point
  • 5.4
4 CHEMBL583042_lig_chart_4 Dual specificity mitogen-activated protein kinase kinase 1 Human
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  • protein tyrosine kinase 2/Focal adhesion kinase 1 in Human [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397]
  • This target only has 1 pki data point
  • 5
5 CHEMBL583042_lig_chart_5 Focal adhesion kinase 1 Human
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  • MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
  • This target only has 1 pki data point
  • 5.4
6 CHEMBL583042_lig_chart_6 Hepatocyte growth factor receptor Human
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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]
  • This target only has 1 pki data point
  • 5.3
7 CHEMBL583042_lig_chart_7 Inhibitor of nuclear factor kappa B kinase epsilon subunit Human
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  • interleukin 1 receptor associated kinase 1/Interleukin-1 receptor-associated kinase 1 in Human [ChEMBL: CHEMBL3357] [GtoPdb: 2042] [UniProtKB: P51617]
  • This target only has 1 pki data point
  • 5
8 CHEMBL583042_lig_chart_8 Interleukin-1 receptor-associated kinase 1 Human
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  • interleukin 1 receptor associated kinase 4/Interleukin-1 receptor-associated kinase 4 in Human [ChEMBL: CHEMBL3778] [GtoPdb: 2045] [UniProtKB: Q9NWZ3]
  • This target only has 1 pki data point
  • 5.4
9 CHEMBL583042_lig_chart_9 Interleukin-1 receptor-associated kinase 4 Human
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  • mitogen-activated protein kinase 1/MAP kinase ERK2 in Human [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
  • 8.7
10 CHEMBL583042_lig_chart_10 MAP kinase ERK2 Human
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  • mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
  • This target only has 1 pki data point
  • 5.4
11 CHEMBL583042_lig_chart_11 MAP kinase p38 alpha Human
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  • mitogen-activated protein kinase kinase kinase 10/Mitogen-activated protein kinase kinase kinase 10 in Human [ChEMBL: CHEMBL2873] [GtoPdb: 2070] [UniProtKB: Q02779]
  • This target only has 1 pki data point
  • 5
12 CHEMBL583042_lig_chart_12 Mitogen-activated protein kinase kinase kinase 10 Human
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  • mitogen-activated protein kinase kinase kinase 14/Mitogen-activated protein kinase kinase kinase 14 in Human [ChEMBL: CHEMBL5888] [GtoPdb: 2074] [UniProtKB: Q99558]
  • This target only has 1 pki data point
  • 5.3
13 CHEMBL583042_lig_chart_13 Mitogen-activated protein kinase kinase kinase 14 Human
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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]
  • This target only has 1 pki data point
  • 5.4
14 CHEMBL583042_lig_chart_14 Mitogen-activated protein kinase kinase kinase 3 Human
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  • mitogen-activated protein kinase kinase kinase 7/Mitogen-activated protein kinase kinase kinase 7 in Human [ChEMBL: CHEMBL5776] [GtoPdb: 2082] [UniProtKB: O43318]
  • This target only has 1 pki data point
  • 5.52
15 CHEMBL583042_lig_chart_15 Mitogen-activated protein kinase kinase kinase 7 Human
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  • mitogen-activated protein kinase kinase kinase 8/Mitogen-activated protein kinase kinase kinase 8 in Human [ChEMBL: CHEMBL4899] [GtoPdb: 2083] [UniProtKB: P41279]
  • This target only has 1 pki data point
  • 5.4
16 CHEMBL583042_lig_chart_16 Mitogen-activated protein kinase kinase kinase 8 Human
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  • pyruvate dehydrogenase kinase 1/Pyruvate dehydrogenase kinase isoform 1 in Human [ChEMBL: CHEMBL4766] [GtoPdb: 2915] [UniProtKB: Q15118]
  • This target only has 1 pki data point
  • 5
17 CHEMBL583042_lig_chart_17 Pyruvate dehydrogenase kinase isoform 1 Human
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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]
  • This target only has 1 pki data point
  • 5.85
18 CHEMBL583042_lig_chart_18 Rho-associated protein kinase 1 Human
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  • AKT serine/threonine kinase 3/Serine/threonine-protein kinase AKT3 in Human [ChEMBL: CHEMBL4816] [GtoPdb: 2286] [UniProtKB: Q9Y243]
  • This target only has 1 pki data point
  • 5.4
19 CHEMBL583042_lig_chart_19 Serine/threonine-protein kinase AKT3 Human
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  • aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
  • 6.27
20 CHEMBL583042_lig_chart_20 Serine/threonine-protein kinase Aurora-A Human
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  • polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350]
  • This target only has 1 pki data point
  • 5.4
21 CHEMBL583042_lig_chart_21 Serine/threonine-protein kinase PLK1 Human
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  • serum/glucocorticoid regulated kinase 1/Serine/threonine-protein kinase Sgk1 in Human [ChEMBL: CHEMBL2343] [GtoPdb: 1534] [UniProtKB: O00141]
  • This target only has 1 pki data point
  • 5
22 CHEMBL583042_lig_chart_22 Serine/threonine-protein kinase Sgk1 Human
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  • TANK binding kinase 1/Serine/threonine-protein kinase TBK1 in Human [ChEMBL: CHEMBL5408] [GtoPdb: 2237] [UniProtKB: Q9UHD2]
  • This target only has 1 pki data point
  • 5
23 CHEMBL583042_lig_chart_23 Serine/threonine-protein kinase TBK1 Human
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  • IL2 inducible T cell kinase/Tyrosine-protein kinase ITK/TSK in Human [ChEMBL: CHEMBL2959] [GtoPdb: 2046] [UniProtKB: Q08881]
  • This target only has 1 pki data point
  • 5.4
24 CHEMBL583042_lig_chart_24 Tyrosine-protein kinase ITK/TSK Human
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  • Janus kinase 2/Tyrosine-protein kinase JAK2 in Human [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
  • This target only has 1 pki data point
  • 5.4
25 CHEMBL583042_lig_chart_25 Tyrosine-protein kinase JAK2 Human
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  • Janus kinase 3/Tyrosine-protein kinase JAK3 in Human [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
  • This target only has 1 pki data point
  • 5.4
26 CHEMBL583042_lig_chart_26 Tyrosine-protein kinase JAK3 Human
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  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
  • This target only has 1 pki data point
  • 5.85
27 CHEMBL583042_lig_chart_27 Tyrosine-protein kinase receptor FLT3 Human
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  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
  • This target only has 1 pki data point
  • 5.4
28 CHEMBL583042_lig_chart_28 Tyrosine-protein kinase SRC Human
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  • spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405]
  • This target only has 1 pki data point
  • 5.4
29 CHEMBL583042_lig_chart_29 Tyrosine-protein kinase SYK Human
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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]
  • This target only has 1 pki data point
  • 5.4
30 CHEMBL583042_lig_chart_30 Tyrosine-protein kinase ZAP-70 Human
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  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
  • This target only has 1 pki data point
  • 5.4
31 CHEMBL583042_lig_chart_31 Vascular endothelial growth factor receptor 2 Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
citron rho-interacting serine/threonine kinase/Citron Rho-interacting kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5579] [GtoPdb: 1509] [UniProtKB: O14578]
ChEMBL Inhibition of CIT B 5 pKi >10000 nM Ki J. Med. Chem. (2009) 52: 6362-6368 [PMID:19827834]
mitogen-activated protein kinase 10/c-Jun N-terminal kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2637] [GtoPdb: 1498] [UniProtKB: P53779]
ChEMBL Inhibition of JNK3 B 5.85 pKi 1400 nM Ki J. Med. Chem. (2009) 52: 6362-6368 [PMID:19827834]
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 6.07 pKi 852 nM Ki J. Med. Chem. (2009) 52: 6362-6368 [PMID:19827834]
GtoPdb - - 6.07 pKi 852 nM Ki J Med Chem (2009) 52: 6362-8 [PMID:19827834]
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 Inhibition of MEK1 B 5.4 pKi >4000 nM Ki J. Med. Chem. (2009) 52: 6362-6368 [PMID:19827834]
protein tyrosine kinase 2/Focal adhesion kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397]
ChEMBL Inhibition of FAK B 5 pKi >10000 nM Ki J. Med. Chem. (2009) 52: 6362-6368 [PMID:19827834]
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 5.4 pKi >4000 nM Ki J. Med. Chem. (2009) 52: 6362-6368 [PMID:19827834]
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 5.3 pKi >5000 nM Ki J. Med. Chem. (2009) 52: 6362-6368 [PMID:19827834]
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 Inhibition of IRAK1 B 5 pKi >10000 nM Ki J. Med. Chem. (2009) 52: 6362-6368 [PMID:19827834]
interleukin 1 receptor associated kinase 4/Interleukin-1 receptor-associated kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3778] [GtoPdb: 2045] [UniProtKB: Q9NWZ3]
ChEMBL Inhibition of IRAK4 B 5.4 pKi >4000 nM Ki J. Med. Chem. (2009) 52: 6362-6368 [PMID:19827834]
mitogen-activated protein kinase 1/MAP kinase ERK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
ChEMBL Inhibition of ERK2 after 10 mins by spectrophotometric coupled-enzyme assay B 8.7 pKi <2 nM Ki J. Med. Chem. (2009) 52: 6362-6368 [PMID:19827834]
GtoPdb - - 8.7 pKi <2 nM Ki J Med Chem (2009) 52: 6362-8 [PMID:19827834]
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 5.4 pKi >4000 nM Ki J. Med. Chem. (2009) 52: 6362-6368 [PMID:19827834]
mitogen-activated protein kinase kinase kinase 10/Mitogen-activated protein kinase kinase kinase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2873] [GtoPdb: 2070] [UniProtKB: Q02779]
ChEMBL Inhibition of MLK2 B 5 pKi >10000 nM Ki J. Med. Chem. (2009) 52: 6362-6368 [PMID:19827834]
mitogen-activated protein kinase kinase kinase 14/Mitogen-activated protein kinase kinase kinase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5888] [GtoPdb: 2074] [UniProtKB: Q99558]
ChEMBL Inhibition of NIK B 5.3 pKi >5000 nM Ki J. Med. Chem. (2009) 52: 6362-6368 [PMID:19827834]
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 Inhibition of MEKK3 B 5.4 pKi >4000 nM Ki J. Med. Chem. (2009) 52: 6362-6368 [PMID:19827834]
mitogen-activated protein kinase kinase kinase 7/Mitogen-activated protein kinase kinase kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5776] [GtoPdb: 2082] [UniProtKB: O43318]
ChEMBL Inhibition of TAK1 B 5.52 pKi 3000 nM Ki J. Med. Chem. (2009) 52: 6362-6368 [PMID:19827834]
mitogen-activated protein kinase kinase kinase 8/Mitogen-activated protein kinase kinase kinase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4899] [GtoPdb: 2083] [UniProtKB: P41279]
ChEMBL Inhibition of COT B 5.4 pKi >4000 nM Ki J. Med. Chem. (2009) 52: 6362-6368 [PMID:19827834]
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 pKi >10000 nM Ki J. Med. Chem. (2009) 52: 6362-6368 [PMID:19827834]
Rho associated coiled-coil containing protein kinase 1/Rho-associated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3231] [GtoPdb: 1503] [UniProtKB: Q13464]
ChEMBL Inhibition of ROCK1 B 5.85 pKi 1400 nM Ki J. Med. Chem. (2009) 52: 6362-6368 [PMID:19827834]
AKT serine/threonine kinase 3/Serine/threonine-protein kinase AKT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4816] [GtoPdb: 2286] [UniProtKB: Q9Y243]
ChEMBL Inhibition of AKT3 B 5.4 pKi >4000 nM Ki J. Med. Chem. (2009) 52: 6362-6368 [PMID:19827834]
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
ChEMBL Inhibition of AURA B 6.27 pKi 540 nM Ki J. Med. Chem. (2009) 52: 6362-6368 [PMID:19827834]
GtoPdb - - 6.27 pKi 540 nM Ki J Med Chem (2009) 52: 6362-8 [PMID:19827834]
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 5.4 pKi >4000 nM Ki J. Med. Chem. (2009) 52: 6362-6368 [PMID:19827834]
serum/glucocorticoid regulated kinase 1/Serine/threonine-protein kinase Sgk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2343] [GtoPdb: 1534] [UniProtKB: O00141]
ChEMBL Inhibition of SGK1 B 5 pKi >10000 nM Ki J. Med. Chem. (2009) 52: 6362-6368 [PMID:19827834]
TANK binding kinase 1/Serine/threonine-protein kinase TBK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5408] [GtoPdb: 2237] [UniProtKB: Q9UHD2]
ChEMBL Inhibition of NAK B 5 pKi >10000 nM Ki J. Med. Chem. (2009) 52: 6362-6368 [PMID:19827834]
IL2 inducible T cell kinase/Tyrosine-protein kinase ITK/TSK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2959] [GtoPdb: 2046] [UniProtKB: Q08881]
ChEMBL Inhibition of ITK B 5.4 pKi >4000 nM Ki J. Med. Chem. (2009) 52: 6362-6368 [PMID:19827834]
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
ChEMBL Inhibition of JAK2 B 5.4 pKi >4000 nM Ki J. Med. Chem. (2009) 52: 6362-6368 [PMID:19827834]
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
ChEMBL Inhibition of JAK3 B 5.4 pKi >4000 nM Ki J. Med. Chem. (2009) 52: 6362-6368 [PMID:19827834]
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
ChEMBL Inhibition of FLT3 B 5.85 pKi 1400 nM Ki J. Med. Chem. (2009) 52: 6362-6368 [PMID:19827834]
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
ChEMBL Inhibition of SRC B 5.4 pKi >4000 nM Ki J. Med. Chem. (2009) 52: 6362-6368 [PMID:19827834]
spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405]
ChEMBL Inhibition of SYK B 5.4 pKi >4000 nM Ki J. Med. Chem. (2009) 52: 6362-6368 [PMID:19827834]
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 5.4 pKi >4000 nM Ki J. Med. Chem. (2009) 52: 6362-6368 [PMID:19827834]
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 KDR B 5.4 pKi >4000 nM Ki J. Med. Chem. (2009) 52: 6362-6368 [PMID:19827834]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]