Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T91331 Target Info
Target Name Fibroblast growth factor receptor 3 (FGFR3)
Synonyms
JTK4; FGFR-3; CD333
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Target Type Successful Target
Gene Name FGFR3
Biochemical Class Kinase
UniProt ID
FGFR3_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 Epidermal growth factor receptor (EGFR) Successful Target
UniProt ID EGFR_HUMAN
Gene Name EGFR
Synonyms
Receptor tyrosine-protein kinase erbB-1; Proto-oncogene c-ErbB-1; HER1; ERBB1; ERBB
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Representative Drug(s) AEE-788 Drug Info IC50 = 2 nM [2]
Co-Target Name Erbb2 tyrosine kinase receptor (HER2) Successful Target
UniProt ID ERBB2_HUMAN
Gene Name ERBB2
Synonyms
p185erbB2; Tyrosine kinase-type cell surface receptor HER2; Receptor tyrosine-protein kinase erbB-2; Proto-oncogene c-ErbB-2; Proto-oncogene Neu; NGL; NEU; Metastatic lymph node gene 19 protein; MLN19; MLN 19; HER2; CD340
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Representative Drug(s) AEE-788 Drug Info IC50 = 2 nM [3]
Co-Target Name Erbb4 tyrosine kinase receptor (Erbb-4) Successful Target
UniProt ID ERBB4_HUMAN
Gene Name ERBB4
Synonyms
Tyrosine kinase-type cell surface receptor HER4; Receptor tyrosine-protein kinase erbB-4; Proto-oncogene-like protein c-ErbB-4; P180erbB4; HER4
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Representative Drug(s) AEE-788 Drug Info IC50 = 2 nM [3]
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) Debio 1347 Drug Info IC50 = 7.6 nM Click to Show More [4]
2 MK-2461 Drug Info IC50 = 39 nM [7]
3 E-3810 Drug Info IC50 = 82.5 nM [3]
4 E-3810 Drug Info IC50 = 82.5 nM [6]
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) Debio 1347 Drug Info IC50 = 9.3 nM Click to Show More [5]
2 E-3810 Drug Info IC50 = 17.5 nM [3]
3 E-3810 Drug Info IC50 = 17.5 nM [6]
4 MK-2461 Drug Info IC50 = 65 nM [7]
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 [7]
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) E-3810 Drug Info IC50 = 25 nM Click to Show More [3]
2 E-3810 Drug Info IC50 = 25 nM [5]
3 MK-2461 Drug Info IC50 = 44 nM [7]
4 AEE-788 Drug Info IC50 = 77 nM [3]
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 [7]
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 [7]
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 [7]
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 [7]
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 Click to Show More [7]
2 AEE-788 Drug Info IC50 = 740 nM [8]
Co-Target Name Erbb3 tyrosine kinase receptor (Erbb-3) Clinical trial Target
UniProt ID ERBB3_HUMAN
Gene Name ERBB3
Synonyms
Tyrosine kinase-type cell surface receptor HER3; Receptor tyrosine-protein kinase erbB-3; Proto-oncogene-like protein c-ErbB-3; HER3; C-erbB3; C-erbB-3 protein
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Representative Drug(s) AEE-788 Drug Info IC50 = 2 nM [3]
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) E-3810 Drug Info IC50 = 7 nM Click to Show More [3]
2 E-3810 Drug Info IC50 = 7 nM [6]
3 MK-2461 Drug Info IC50 = 10 nM [7]
4 AEE-788 Drug Info IC50 = 59 nM [3]
Co-Target Name Macrophage-stimulating protein receptor (RON) Clinical trial Target
UniProt ID RON_HUMAN
Gene Name MST1R
Synonyms
p185Ron; Proteintyrosine kinase 8; Macrophagestimulating protein receptor beta chain; Macrophagestimulating protein receptor; MST1R; MSP receptor; CDw136; CD136
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Representative Drug(s) MK-2461 Drug Info IC50 = 7 nM [7]
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) E-3810 Drug Info IC50 = 10 nM Click to Show More [3]
2 E-3810 Drug Info IC50 = 10 nM [5]
3 MK-2461 Drug Info IC50 = 78 nM [7]
Co-Target Name Yes tyrosine kinase (YES) Clinical trial Target
UniProt ID YES_HUMAN
Gene Name YES1
Synonyms
p61-Yes; Yes p59-Fyn; Yes Protooncogene Syn; Tyrosine-protein kinase Yes; Proto-oncogene c-Yes
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Representative Drug(s) AEE-788 Drug Info IC50 = 13.1 nM [9]
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 [7]
Co-Target Name Fibroblast growth factor receptor 4 (FGFR4) Clinical trial Target
UniProt ID FGFR4_HUMAN
Gene Name FGFR4
Synonyms
TKF; JTK2; FGFR-4; CD334
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Representative Drug(s) Debio 1347 Drug Info IC50 = 290 nM [10]
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 [7]
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 Synthesis and in vitro EGFR (ErbB1) tyrosine kinase inhibitory activity of 4-N-substituted 6-aryl-7H-pyrrolo[2,3-d]pyrimidine-4-amines. Eur J Med Chem. 2011 Dec;46(12):6002-14.
REF 3 Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors. J Med Chem. 2012 Dec 27;55(24):10797-822.
REF 4 Identification of an Indazole-Based Pharmacophore for the Inhibition of FGFR Kinases Using Fragment-Led de Novo Design. ACS Med Chem Lett. 2017 Nov 11;8(12):1264-1268.
REF 5 An overview of the binding models of FGFR tyrosine kinases in complex with small molecule inhibitors. Eur J Med Chem. 2017 Jan 27;126:476-90.
REF 6 Design, synthesis and biological evaluation of a series of novel 2-benzamide-4-(6-oxy-N-methyl-1-naphthamide)-pyridine derivatives as potent fibroblast growth factor receptor (FGFR) inhibitors. Eur J Med Chem. 2018 Jun 25;154:9-28.
REF 7 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.
REF 8 Pharmacophore modeling and virtual screening to identify potential RET kinase inhibitors. Bioorg Med Chem Lett. 2011 Aug 1;21(15):4490-7.
REF 9 Identification of potent Yes1 kinase inhibitors using a library screening approach. Bioorg Med Chem Lett. 2013 Aug 1;23(15):4398-403.
REF 10 Discovery of [5-Amino-1-(2-methyl-3H-benzimidazol-5-yl)pyrazol-4-yl]-(1H-indol-2-yl)methanone (CH5183284/Debio 1347), An Orally Available and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor. J Med Chem. 2016 Dec 8;59(23):10586-10600.

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