Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T63966 Target Info
Target Name Vascular endothelial growth factor receptor 1 (FLT-1)
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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Target Type Successful Target
Gene Name FLT1
Biochemical Class Kinase
UniProt ID
VGFR1_HUMAN
Co-Targets of This Target  Top
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) Tivozanib Drug Info IC50 = 0.16 nM Click to Show More [1]
2 Famitinib Drug Info IC50 = 2 nM [2]
3 CEP-11981 Drug Info IC50 = 4 nM [4]
4 E-3810 Drug Info IC50 = 25 nM [5]
5 E-3810 Drug Info IC50 = 25 nM [7]
Co-Target Name Tyrosine-protein kinase Kit (KIT) Successful Target
UniProt ID KIT_HUMAN
Gene Name KIT
Synonyms
v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog; p145 c-kit; Proto-oncogene tyrosine-protein kinase Kit; Proto-oncogene c-Kit; Piebald trait protein; PBT; Mast/stem cell growth factor receptor Kit; CD117 antigen; CD117; C-kit
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Representative Drug(s) Famitinib Drug Info IC50 = 2 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) Tivozanib Drug Info IC50 = 2.26 nM Click to Show More [3]
2 CEP-11981 Drug Info IC50 = 246 nM [4]
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) CEP-11981 Drug Info IC50 = 3 nM [4]
Co-Target Name Platelet-derived growth factor receptor beta (PDGFRB) Successful Target
UniProt ID PGFRB_HUMAN
Gene Name PDGFRB
Synonyms
Platelet-derived growth factor receptor 1; PDGFR1; PDGFR-beta; PDGFR-1; PDGFR; PDGF-R-beta; CD140b antigen; CD140b; CD140 antigen-like family member B; Beta-type platelet-derived growth factor receptor; Beta-PDGFR; Beta platelet-derived growth factor receptor
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Representative Drug(s) Famitinib Drug Info IC50 = 4 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) CEP-11981 Drug Info IC50 = 5 nM [4]
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) CEP-11981 Drug Info IC50 = 5 nM [4]
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) CEP-11981 Drug Info IC50 = 13 nM Click to Show More [4]
2 E-3810 Drug Info IC50 = 17.5 nM [5]
3 E-3810 Drug Info IC50 = 17.5 nM [6]
Co-Target Name Proto-oncogene c-Src (SRC) Successful Target
UniProt ID SRC_HUMAN
Gene Name SRC
Synonyms
pp60c-src; Tyrosine kinase (pp60(src)); Src tyrosine kinase; SRC1; Proto-oncogene tyrosine-protein kinase Src; Pp60(src); P60-Src; C-src TK; C-Src
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Representative Drug(s) CEP-11981 Drug Info IC50 = 37 nM [4]
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) CEP-11981 Drug Info IC50 = 71 nM [4]
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) E-3810 Drug Info IC50 = 82.5 nM Click to Show More [5]
2 E-3810 Drug Info IC50 = 82.5 nM [6]
Co-Target Name Tyrosine-protein kinase BTK (ATK) Successful Target
UniProt ID BTK_HUMAN
Gene Name BTK
Synonyms
Bruton's tyrosine kinase; Bruton tyrosine kinase; BPK; B-cell progenitor kinase; B cell progenitor kinase; Agammaglobulinemia tyrosine kinase; Agammaglobulinaemia tyrosine kinase; AGMX1
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Representative Drug(s) CEP-11981 Drug Info IC50 = 93 nM [4]
Co-Target Name ALK tyrosine kinase receptor (ALK) Successful Target
UniProt ID ALK_HUMAN
Gene Name ALK
Synonyms
CD246; Anaplastic lymphoma kinase
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Representative Drug(s) CEP-11981 Drug Info IC50 = 132 nM [4]
Co-Target Name Adenosine A2a receptor (ADORA2A) Successful Target
UniProt ID AA2AR_HUMAN
Gene Name ADORA2A
Synonyms
Adenosine receptor A2a; ADORA2; A2a Adenosine receptor; A(2A) adenosine receptor
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Representative Drug(s) CEP-11981 Drug Info Ki = 500 nM [4]
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) Tivozanib Drug Info IC50 = 0.24 nM Click to Show More [5]
2 E-3810 Drug Info IC50 = 10 nM [5]
3 E-3810 Drug Info IC50 = 10 nM [7]
Co-Target Name Ephrin type-B receptor 2 (EPHB2) Clinical trial Target
UniProt ID EPHB2_HUMAN
Gene Name EPHB2
Synonyms
hEK5; Tyrosine-protein kinase receptor EPH-3; Tyrosine-protein kinase TYRO5; TYRO5; Renal carcinoma antigen NY-REN-47; Receptor protein-tyrosine kinase HEK5; EphB2 receptor tyrosine kinase; EphB2; EPTH3; EPHT3; EPH-like kinase 5; EPH tyrosine kinase 3; ELK-related tyrosine kinase; EK5; Developmentally-regulated Eph-related tyrosine kinase; DRT
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Representative Drug(s) Tivozanib Drug Info IC50 = 17.5 nM [3]
Co-Target Name Angiopoietin 1 receptor (TEK) Clinical trial Target
UniProt ID TIE2_HUMAN
Gene Name TEK
Synonyms
hTIE2; VMCM1; VMCM; Tyrosine-protein kinase receptor TIE-2; Tyrosine-protein kinase receptor TEK; Tyrosine kinase with Ig and EGF homology domains-2; Tunica interna endothelial cell kinase; TIE2; P140 TEK; Endothelial tyrosine kinase; Endothelial Cell-Specific Receptor TIE-2; CD202b antigen; CD202b
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Representative Drug(s) CEP-11981 Drug Info IC50 = 22 nM [4]
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) CEP-11981 Drug Info IC50 = 42 nM [4]
Co-Target Name Macrophage colony-stimulating factor 1 receptor (CSF1R) Clinical trial Target
UniProt ID CSF1R_HUMAN
Gene Name CSF1R
Synonyms
Proto-oncogene c-Fms; M-CSF-R; FMS; CSF-1R; CSF-1-R; CSF-1 receptor; CD115
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Representative Drug(s) CEP-11981 Drug Info IC50 = 78 nM [4]
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) CEP-11981 Drug Info IC50 = 89 nM Click to Show More [4]
2 E-3810 Drug Info IC50 = 237.5 nM [6]
Co-Target Name Serine/threonine-protein kinase Chk2 (RAD53) Clinical trial Target
UniProt ID CHK2_HUMAN
Gene Name CHEK2
Synonyms
hCds1; Hucds1; Checkpoint kinase 2; Cds1 homolog; Cds1; CHK2 checkpoint homolog; CHK2
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Representative Drug(s) CEP-11981 Drug Info IC50 = 140 nM [4]
Co-Target Name Casein kinase I alpha (CSNK1A1) Patented-recorded Target
UniProt ID KC1A_HUMAN
Gene Name CSNK1A1
Synonyms
Casein kinase I isoform alpha; CKI-alpha; CK1
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Representative Drug(s) CEP-11981 Drug Info IC50 = 48 nM [4]
Co-Target Name Nuclear receptor subfamily 2 group C member 2 (NR2C2) Co-Target
UniProt ID NR2C2_HUMAN
Gene Name NR2C2
Synonyms
Orphan nuclear receptor TAK1; Orphan nuclear receptor TR4; Testicular receptor 4
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Representative Drug(s) CEP-11981 Drug Info IC50 = 14 nM [4]
Co-Target Name Serine/threonine-protein kinase MST2 (STK3) Co-Target
UniProt ID STK3_HUMAN
Gene Name STK3
Synonyms
Serine/threonine-protein kinase 3; Mammalian STE20-like protein kinase 2; MST-2; STE20-like kinase MST2; Serine/threonine-protein kinase Krs-1
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Representative Drug(s) CEP-11981 Drug Info IC50 = 21 nM [4]
References  Top
REF 1 Pharmacophore modeling and virtual screening studies for new VEGFR-2 kinase inhibitors. Eur J Med Chem. 2010 Nov;45(11):5420-7.
REF 2 Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives. J Med Chem. 2010 Nov 25;53(22):8140-9.
REF 3 Design, synthesis and biological evaluation of deuterated Tivozanib for improving pharmacokinetic properties. Bioorg Med Chem Lett. 2015 Jun 1;25(11):2425-8.
REF 4 Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one (CEP-11981): a novel oncology therapeutic agent. J Med Chem. 2012 Jan 26;55(2):903-13.
REF 5 Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors. J Med Chem. 2012 Dec 27;55(24):10797-822.
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 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.

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