Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T07303 | Target Info | |||
| Target Name | Vascular endothelial growth factor receptor 3 (FLT-4) | ||||
| Synonyms |
VEGFR3; VEGFR-3; VEGF-3 receptor; Tyrosine-protein kinase receptor FLT4; Fms-like tyrosine kinase 4
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| Target Type | Successful Target | ||||
| Gene Name | FLT4 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| 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 | [3] | ||
| 3 | ABT-869 | Drug Info | IC50 = 2.3 nM | [5] | ||
| 4 | VATALANIB | Drug Info | IC50 = 10 nM | [7] | ||
| 5 | E-3810 | Drug Info | IC50 = 25 nM | [9] | ||
| 6 | E-3810 | Drug Info | IC50 = 25 nM | [12] | ||
| 7 | MK-2461 | Drug Info | IC50 = 44 nM | [11] | ||
| 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 | [2] | ||
| 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 | Click to Show More | [3] | |
| 2 | ABT-869 | Drug Info | IC50 = 14 nM | [6] | ||
| 3 | VATALANIB | Drug Info | IC50 = 730 nM | [17] | ||
| 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 | [4] | |
| 2 | ABT-869 | Drug Info | IC50 = 15 nM | [8] | ||
| 3 | MK-2461 | Drug Info | IC50 < 100 nM | [11] | ||
| 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) | ABT-869 | Drug Info | IC50 = 4 nM | Click to Show More | [6] | |
| 2 | MK-2461 | Drug Info | IC50 = 22 nM | [11] | ||
| 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 | Click to Show More | [3] | |
| 2 | ABT-869 | Drug Info | IC50 = 60 nM | [13] | ||
| 3 | VATALANIB | Drug Info | IC50 = 490 nM | [16] | ||
| 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) | E-3810 | Drug Info | IC50 = 17.5 nM | Click to Show More | [9] | |
| 2 | E-3810 | Drug Info | IC50 = 17.5 nM | [10] | ||
| 3 | MK-2461 | Drug Info | IC50 = 65 nM | [11] | ||
| 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 | Click to Show More | [11] | |
| 2 | E-3810 | Drug Info | IC50 = 82.5 nM | [9] | ||
| 3 | E-3810 | Drug Info | IC50 = 82.5 nM | [10] | ||
| 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 | [11] | ||
| 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 | [11] | ||
| Co-Target Name | Smoothened homolog (SMO) | Successful Target | ||||
| UniProt ID | SMO_HUMAN | |||||
| Gene Name | SMO | |||||
| Synonyms |
Smo-D473H; SMOH; Protein Gx
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| Representative Drug(s) | ABT-869 | Drug Info | Ki = 87.6 nM | [14] | ||
| 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 | [11] | ||
| 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 | [15] | ||
| 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 | [11] | ||
| 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) | Tivozanib | Drug Info | IC50 = 0.21 nM | Click to Show More | [9] | |
| 2 | ABT-869 | Drug Info | IC50 = 3 nM | [6] | ||
| 3 | E-3810 | Drug Info | IC50 = 7 nM | [9] | ||
| 4 | E-3810 | Drug Info | IC50 = 7 nM | [10] | ||
| 5 | MK-2461 | Drug Info | IC50 = 10 nM | [11] | ||
| 6 | VATALANIB | Drug Info | IC50 = 54 nM | [18] | ||
| 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) | ABT-869 | Drug Info | IC50 = 3 nM | [6] | ||
| 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 | [11] | ||
| 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 | [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 | [11] | ||
| 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 | Click to Show More | [11] | |
| 2 | E-3810 | Drug Info | IC50 = 237.5 nM | [10] | ||
| 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) | ABT-869 | Drug Info | IC50 = 170 nM | [19] | ||
| 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 | Click to Show More | [11] | |
| 2 | ABT-869 | Drug Info | IC50 = 760 nM | [20] | ||
| Co-Target Name | Cyclin-dependent kinase 8 (CDK8) | Patented-recorded Target | ||||
| UniProt ID | CDK8_HUMAN | |||||
| Gene Name | CDK8 | |||||
| Synonyms |
Protein kinase K35; Mediator of RNA polymerase II transcription subunit CDK8; Mediator complex subunit CDK8; Cell division protein kinase 8
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| Representative Drug(s) | ABT-869 | Drug Info | IC50 = 14 nM | [6] | ||
| Co-Target Name | Cyclin-dependent kinase 19 (CDK19) | Co-Target | ||||
| UniProt ID | CDK19_HUMAN | |||||
| Gene Name | CDK19 | |||||
| Synonyms |
CDC2-related protein kinase 6; Cell division cycle 2-like protein kinase 6; Cell division protein kinase 19; Cyclin-dependent kinase 11; Death-preventing kinase
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| Representative Drug(s) | ABT-869 | Drug Info | IC50 = 24 nM | [6] | ||
| 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 | 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 3 | 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 4 | Design, synthesis and biological evaluation of deuterated Tivozanib for improving pharmacokinetic properties. Bioorg Med Chem Lett. 2015 Jun 1;25(11):2425-8. | ||||
| REF 5 | Discovery of a New Series of Naphthamides as Potent VEGFR-2 Kinase Inhibitors. ACS Med Chem Lett. 2014 Feb 24;5(5):592-7. | ||||
| REF 6 | Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?. J Med Chem. 2018 Jun 28;61(12):5073-92. | ||||
| REF 7 | Selectivity data: assessment, predictions, concordance, and implications. J Med Chem. 2013 Sep 12;56(17):6991-7002. | ||||
| REF 8 | Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRalpha) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). J Med Chem. 2017 Jun 22;60(12):5099-5119. | ||||
| REF 9 | Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors. J Med Chem. 2012 Dec 27;55(24):10797-822. | ||||
| REF 10 | 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 11 | 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 12 | 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 13 | Design, synthesis and structure-activity relationship of diaryl-ureas with novel isoxazol[3,4-b]pyridine-3-amino-structure as multi-target inhibitors against receptor tyrosine kinase. Bioorg Med Chem. 2018 Sep 1;26(16):4735-44. | ||||
| REF 14 | Dual MET and SMO Negative Modulators Overcome Resistance to EGFR Inhibitors in Human Nonsmall Cell Lung Cancer. J Med Chem. 2017 Sep 14;60(17):7447-58. | ||||
| REF 15 | 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 16 | Chemical modulation of receptor signaling inhibits regenerative angiogenesis in adult zebrafish. Nat Chem Biol. 2006 May;2(5):265-73. | ||||
| REF 17 | 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 18 | ortho-Substituted azoles as selective and dual inhibitors of VEGF receptors 1 and 2. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1369-75. | ||||
| REF 19 | Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted ... J Med Chem. 2007 Apr 5;50(7):1584-97. | ||||
| REF 20 | Discovery and evaluation of 3-phenyl-1H-5-pyrazolylamine-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3). Bioorg Med Chem. 2011 Jul 15;19(14):4173-82. | ||||
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