Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T80782 | Target Info | |||
| Target Name | VEGFR1 messenger RNA (VEGFR1 mRNA) | ||||
| Synonyms |
Vascular permeability factor receptor (mRNA); VEGFR1 (mRNA); VEGFR-1 (mRNA); VEGF-1 receptor (mRNA); Tyrosine-protein kinase receptor FLT (mRNA); Tyrosine-protein kinase FRT (mRNA); Fms-like tyrosine kinase 1 (mRNA); FRT (mRNA); FLT (mRNA)
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| Target Type | Successful Target | ||||
| Gene Name | FLT1 | ||||
| Biochemical Class | mRNA target | ||||
| UniProt ID | |||||
| 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 | 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) | VATALANIB | Drug Info | IC50 = 10 nM | Click to Show More | [2] | |
| 2 | Romiplostim | Drug Info | IC50 = 12.9 nM | [3] | ||
| 3 | MK-2461 | Drug Info | IC50 = 44 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) | MK-2461 | Drug Info | IC50 = 22 nM | Click to Show More | [4] | |
| 2 | Romiplostim | Drug Info | IC50 = 160 nM | [8] | ||
| 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) | Romiplostim | Drug Info | IC50 = 35 nM | Click to Show More | [5] | |
| 2 | VATALANIB | Drug Info | IC50 = 730 nM | [12] | ||
| 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 | [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) | MK-2461 | Drug Info | IC50 = 46 nM | [4] | ||
| 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 | [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) | MK-2461 | Drug Info | IC50 = 65 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) | Romiplostim | Drug Info | IC50 = 68 nM | Click to Show More | [6] | |
| 2 | VATALANIB | Drug Info | IC50 = 490 nM | [11] | ||
| 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 | Click to Show More | [4] | |
| 2 | Romiplostim | Drug Info | IC50 = 200 nM | [9] | ||
| Co-Target Name | Vascular endothelial growth factor receptor (VEGFR) | Successful Target | ||||
| UniProt ID | VGFR1_HUMAN; VGFR2_HUMAN; VGFR3_HUMAN | |||||
| Gene Name | NO-GeName | |||||
| Representative Drug(s) | VATALANIB | Drug Info | IC50 = 100 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) | Romiplostim | Drug Info | IC50 = 170 nM | Click to Show More | [8] | |
| 2 | MK-2461 | Drug Info | IC50 = 640 nM | [4] | ||
| 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 | [4] | ||
| 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) | VATALANIB | Drug Info | IC50 = 457.7 nM | [10] | ||
| 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 | [4] | ||
| 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 | [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) | MK-2461 | Drug Info | IC50 = 50 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) | Romiplostim | Drug Info | IC50 = 50 nM | Click to Show More | [5] | |
| 2 | MK-2461 | Drug Info | IC50 = 78 nM | [4] | ||
| 3 | VATALANIB | Drug Info | IC50 = 195 nM | [13] | ||
| 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) | Romiplostim | Drug Info | IC50 = 84 nM | [5] | ||
| 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 | [4] | ||
| 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 | Selectivity data: assessment, predictions, concordance, and implications. J Med Chem. 2013 Sep 12;56(17):6991-7002. | ||||
| REF 3 | The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents. Bioorg Med Chem. 2015 May 15;23(10):2408-23. | ||||
| REF 4 | 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 5 | Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93. | ||||
| REF 6 | Synthesis of hybrid anticancer agents based on kinase and histone deacetylase inhibitors. Medchemcomm. 2014;5:1829-33. | ||||
| REF 7 | Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors. J Med Chem. 2005 Mar 10;48(5):1610-9. | ||||
| REF 8 | Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors. Bioorg Med Chem. 2010 Feb 15;18(4):1482-96. | ||||
| REF 9 | Vegfrecine, an inhibitor of VEGF receptor tyrosine kinases isolated from the culture broth of Streptomyces sp. J Nat Prod. 2013 Apr 26;76(4):715-9. | ||||
| REF 10 | Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cyst... Bioorg Med Chem. 2007 Jun 1;15(11):3635-48. | ||||
| REF 11 | Chemical modulation of receptor signaling inhibits regenerative angiogenesis in adult zebrafish. Nat Chem Biol. 2006 May;2(5):265-73. | ||||
| REF 12 | Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching. Bioorg Med Chem Lett. 2003 Sep 15;13(18):2967-71. | ||||
| REF 13 | Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors. J Med Chem. 2012 Dec 27;55(24):10797-822. | ||||
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