Co-Target(s) Information
| Target General Information | Top | ||||
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| Target ID | T53524 | Target Info | |||
| Target Name | Platelet-derived growth factor receptor alpha (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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| Target Type | Successful Target | ||||
| Gene Name | PDGFRA | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
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| 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) | CP-868596 | Drug Info | IC50 = 0.06 nM | Click to Show More | [1] | |
| 2 | Romiplostim | Drug Info | IC50 = 160 nM | [9] | ||
| 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) | Drug Info | IC50 = 2 nM | Click to Show More | [2] | ||
| 2 | Romiplostim | Drug Info | IC50 = 12.9 nM | [3] | ||
| 3 | E-3810 | Drug Info | IC50 = 25 nM | [4] | ||
| 4 | E-3810 | Drug Info | IC50 = 25 nM | [6] | ||
| 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) | Drug Info | IC50 = 2 nM | Click to Show More | [2] | ||
| 2 | Romiplostim | Drug Info | IC50 = 35 nM | [7] | ||
| 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) | Drug Info | IC50 = 4 nM | Click to Show More | [2] | ||
| 2 | Romiplostim | Drug Info | IC50 = 68 nM | [8] | ||
| 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 | [4] | |
| 2 | E-3810 | Drug Info | IC50 = 17.5 nM | [5] | ||
| 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 | [4] | |
| 2 | E-3810 | Drug Info | IC50 = 82.5 nM | [5] | ||
| 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 | [9] | ||
| Co-Target Name | Tyrosine-protein kinase UFO (AXL) | Successful Target | ||||
| UniProt ID | UFO_HUMAN | |||||
| Gene Name | AXL | |||||
| Synonyms |
UFO; Tyrosine-protein kinase receptor UFO; AXL oncogene
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| Representative Drug(s) | MP470 | Drug Info | IC50 < 1000 nM | [10] | ||
| 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 | [4] | |
| 2 | E-3810 | Drug Info | IC50 = 7 nM | [5] | ||
| 3 | Romiplostim | Drug Info | IC50 = 8 nM | [11] | ||
| 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 | [4] | |
| 2 | E-3810 | Drug Info | IC50 = 10 nM | [6] | ||
| 3 | Romiplostim | Drug Info | IC50 = 50 nM | [7] | ||
| 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 | [7] | ||
| 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) | E-3810 | Drug Info | IC50 = 237.5 nM | [5] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Dual FLT3 inhibitors: Against the drug resistance of acute myeloid leukemia in recent decade. Eur J Med Chem. 2019 Sep 15;178:468-483. | ||||
| 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 | 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 | Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors. J Med Chem. 2012 Dec 27;55(24):10797-822. | ||||
| REF 5 | 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 6 | 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 7 | Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93. | ||||
| REF 8 | Synthesis of hybrid anticancer agents based on kinase and histone deacetylase inhibitors. Medchemcomm. 2014;5:1829-33. | ||||
| REF 9 | 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 10 | AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective. J Med Chem. 2016 Apr 28;59(8):3593-608. | ||||
| REF 11 | New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven a... J Med Chem. 2000 Jun 15;43(12):2310-23. | ||||
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