Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T01973 Target Info
Target Name Macrophage-stimulating protein receptor (RON)
Synonyms
p185Ron; Proteintyrosine kinase 8; Macrophagestimulating protein receptor beta chain; Macrophagestimulating protein receptor; MST1R; MSP receptor; CDw136; CD136
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Target Type Clinical trial Target
Gene Name MST1R
Biochemical Class Kinase
UniProt ID
RON_HUMAN
Co-Targets of This Target  Top
Co-Target Name Proto-oncogene c-Met (MET) Successful Target
UniProt ID MET_HUMAN
Gene Name MET
Synonyms
Tyrosine-protein kinase Met; Scatter factor receptor; SF receptor; Met proto-oncogene tyrosine kinase; Hepatocyte growth factor receptor; HGF/SF receptor; HGF-SF receptor; HGF receptor; C-met; C-Met receptor tyrosine kinase
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Representative Drug(s) MK-2461 Drug Info IC50 = 0.4 nM [1]
Co-Target Name Fms-like tyrosine kinase 3 (FLT-3) Successful Target
UniProt ID FLT3_HUMAN
Gene Name FLT3
Synonyms
Stem cell tyrosine kinase 1; STK1; STK-1; Receptor-type tyrosine-protein kinase FLT3; Fetal liver kinase-2; FLT-3; FLK2; FLK-2; FL cytokine receptor; CD135
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Representative Drug(s) MK-2461 Drug Info IC50 = 22 nM [2]
Co-Target Name Fibroblast growth factor receptor 2 (FGFR2) Successful Target
UniProt ID FGFR2_HUMAN
Gene Name FGFR2
Synonyms
Keratinocyte growth factor receptor 2; Keratinocyte growth factor receptor; KSAM; KGFR; K-sam; FGFR-2; FGF-2 receptor; CD332; BEK
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Representative Drug(s) MK-2461 Drug Info IC50 = 39 nM [2]
Co-Target Name Vascular endothelial growth factor receptor 2 (KDR) Successful Target
UniProt ID VGFR2_HUMAN
Gene Name KDR
Synonyms
VEGFR2; VEGFR-2; VEGF-2 receptor; Protein-tyrosine kinase receptor flk-1; Kinase insert domain receptor; Fetal liver kinase 1; FLK1; FLK-1; CD309
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Representative Drug(s) MK-2461 Drug Info IC50 = 44 nM [2]
Co-Target Name Tropomyosin-related kinase A (TrkA) Successful Target
UniProt ID NTRK1_HUMAN
Gene Name NTRK1
Synonyms
gp140trk; Tyrosine kinase receptor A; Tyrosine kinase receptor; Trk-A; TRKA; TRK1-transforming tyrosine kinase protein; TRK1 transforming tyrosinekinase protein; TRK; P140-TrkA; Neurotrophic tyrosine kinase receptor type 1; NGF-trk receptor type A; MTC; High affinity nerve growth factor receptor
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Representative Drug(s) MK-2461 Drug Info IC50 = 46 nM [2]
Co-Target Name BDNF/NT-3 growth factors receptor (TrkB) Successful Target
UniProt ID NTRK2_HUMAN
Gene Name NTRK2
Synonyms
Tropomyosin-related kinase B; TrkB tyrosine kinase; Trk-B; TRKB; Neurotrophic tyrosine kinase receptor type 2; GP145-TrkB
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Representative Drug(s) MK-2461 Drug Info IC50 = 61 nM [2]
Co-Target Name Fibroblast growth factor receptor 1 (FGFR1) Successful Target
UniProt ID FGFR1_HUMAN
Gene Name FGFR1
Synonyms
c-fgr; bFGF-R-1; bFGF-R; N-sam; HBGFR; Fms-like tyrosine kinase 2; FLT2; FLT-2; FLG; FGFR-1; FGFBR; CEK; CD331 antigen; CD331; Basic fibroblast growth factor receptor 1; BFGFR
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Representative Drug(s) MK-2461 Drug Info IC50 = 65 nM [2]
Co-Target Name Platelet-derived growth factor receptor alpha (PDGFRA) Successful Target
UniProt ID PGFRA_HUMAN
Gene Name PDGFRA
Synonyms
RHEPDGFRA; Platelet-derived growth factor receptor 2; Platelet-derived growth factor alpha receptor; PDGFR2; PDGFR-alpha; PDGFR-2; PDGF-R-alpha; CD140a antigen; CD140a; CD140 antigen-like family member A; Alpha-type platelet-derived growth factor receptor; Alpha platelet-derived growth factor receptor
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Representative Drug(s) MK-2461 Drug Info IC50 < 100 nM [2]
Co-Target Name Janus kinase 2 (JAK-2) Successful Target
UniProt ID JAK2_HUMAN
Gene Name JAK2
Synonyms
Tyrosine-protein kinase JAK2
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Representative Drug(s) MK-2461 Drug Info IC50 = 230 nM [2]
Co-Target Name Proto-oncogene c-Ret (RET) Successful Target
UniProt ID RET_HUMAN
Gene Name RET
Synonyms
RET51; RET receptor tyrosine kinase; RET mutant Y791F; RET mutant V804M; RET mutant V804L; RET mutant S891A; RET mutant M918T; RET mutant G691S; Proto-oncogene tyrosine-protein kinase receptor Ret; PTC; Cadherin family member 12; CDHR16; CDHF12; C-ret
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Representative Drug(s) MK-2461 Drug Info IC50 = 640 nM [2]
Co-Target Name Vascular endothelial growth factor receptor 1 (FLT-1) Clinical trial Target
UniProt ID VGFR1_HUMAN
Gene Name FLT1
Synonyms
Vascular permeability factor receptor; VEGFR1; VEGFR-1; VEGF-1 receptor; Tyrosine-protein kinase receptor FLT; Tyrosine-protein kinase FRT; Fms-like tyrosine kinase 1; FRT; FLT
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Representative Drug(s) MK-2461 Drug Info IC50 = 10 nM [2]
Co-Target Name Tyrosine-protein kinase Mer (MERTK) Clinical trial Target
UniProt ID MERTK_HUMAN
Gene Name MERTK
Synonyms
Receptor tyrosine kinase MerTK; Proto-oncogene c-Mer
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Representative Drug(s) MK-2461 Drug Info IC50 = 24 nM [2]
Co-Target Name Fibroblast growth factor receptor 3 (FGFR3) Clinical trial Target
UniProt ID FGFR3_HUMAN
Gene Name FGFR3
Synonyms
JTK4; FGFR-3; CD333
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Representative Drug(s) MK-2461 Drug Info IC50 = 50 nM [2]
Co-Target Name Vascular endothelial growth factor receptor 3 (FLT-4) Clinical trial Target
UniProt ID VGFR3_HUMAN
Gene Name FLT4
Synonyms
VEGFR3; VEGFR-3; VEGF-3 receptor; Tyrosine-protein kinase receptor FLT4; Fms-like tyrosine kinase 4
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Representative Drug(s) MK-2461 Drug Info IC50 = 78 nM [2]
Co-Target Name Aurora kinase A (AURKA) Clinical trial Target
UniProt ID AURKA_HUMAN
Gene Name AURKA
Synonyms
hARK1; Serine/threonine-protein kinase aurora-A; Serine/threonine-protein kinase 6; Serine/threonine-protein kinase 15; Serine/threonine kinase 15; STK6; STK15; IAK1; Breast tumor-amplified kinase; BTAK; Aurora/IPL1-related kinase 1; Aurora-related kinase 1; Aurora-A; Aurora 2; AYK1; AURA; ARK1; ARK-1; AIRK1; AIK
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Representative Drug(s) MK-2461 Drug Info IC50 = 290 nM [2]
References  Top
REF 1 Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs. Eur J Med Chem. 2016 Jan 27;108:495-504.
REF 2 Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer. J Med Chem. 2011 Jun 23;54(12):4092-108.

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