Co-Target(s) Information
Target General Information | Top | ||||
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Target ID | T47101 | Target Info | |||
Target Name | Fibroblast growth factor receptor 1 (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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Target Type | Successful Target | ||||
Gene Name | FGFR1 | ||||
Biochemical Class | Kinase | ||||
UniProt ID |
Co-Targets of This Target | Top | |||||
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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 | 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) | Infigratinib | Drug Info | IC50 = 1 nM | Click to Show More | [2] | |
2 | Infigratinib | Drug Info | IC50 = 1.4 nM | [3] | ||
3 | Erdafitinib | Drug Info | IC50 = 2.5 nM | [4] | ||
4 | Debio 1347 | Drug Info | IC50 = 7.6 nM | [6] | ||
5 | MK-2461 | Drug Info | IC50 = 39 nM | [8] | ||
6 | E-3810 | Drug Info | IC50 = 82.5 nM | [9] | ||
7 | E-3810 | Drug Info | IC50 = 82.5 nM | [14] | ||
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) | KW-2449 | Drug Info | IC50 = 6.6 nM | Click to Show More | [5] | |
2 | MK-2461 | Drug Info | IC50 = 22 nM | [8] | ||
3 | Romiplostim | Drug Info | IC50 = 160 nM | [16] | ||
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) | Romiplostim | Drug Info | IC50 = 12.9 nM | Click to Show More | [7] | |
2 | E-3810 | Drug Info | IC50 = 25 nM | [9] | ||
3 | E-3810 | Drug Info | IC50 = 25 nM | [2] | ||
4 | Erdafitinib | Drug Info | IC50 = 36.8 nM | [4] | ||
5 | MK-2461 | Drug Info | IC50 = 44 nM | [8] | ||
6 | Rosiglitazone + metformin | Drug Info | IC50 = 135 nM | [15] | ||
7 | Infigratinib | Drug Info | IC50 = 180 nM | [3] | ||
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 | [10] | |
2 | Infigratinib | Drug Info | IC50 = 750 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 | [8] | ||
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) | Infigratinib | Drug Info | Ki = 46.5 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) | Rosiglitazone + metformin | Drug Info | IC50 = 50 nM | Click to Show More | [12] | |
2 | Romiplostim | Drug Info | IC50 = 68 nM | [13] | ||
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 | [8] | ||
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 | [8] | |
2 | Romiplostim | Drug Info | IC50 = 200 nM | [17] | ||
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 | [16] | |
2 | MK-2461 | Drug Info | IC50 = 640 nM | [8] | ||
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 | [8] | ||
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) | Infigratinib | Drug Info | IC50 = 0.7 nM | Click to Show More | [3] | |
2 | Infigratinib | Drug Info | IC50 = 1 nM | [2] | ||
3 | Erdafitinib | Drug Info | IC50 = 3 nM | [19] | ||
4 | Debio 1347 | Drug Info | IC50 = 22 nM | [21] | ||
5 | MK-2461 | Drug Info | IC50 = 50 nM | [8] | ||
6 | E-3810 | Drug Info | IC50 = 237.5 nM | [14] | ||
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) | Infigratinib | Drug Info | IC50 = 0.82 nM | Click to Show More | [18] | |
2 | Erdafitinib | Drug Info | IC50 = 5.7 nM | [4] | ||
3 | Infigratinib | Drug Info | IC50 = 60 nM | [3] | ||
4 | Debio 1347 | Drug Info | IC50 = 290 nM | [21] | ||
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 | [9] | |
2 | E-3810 | Drug Info | IC50 = 7 nM | [14] | ||
3 | Romiplostim | Drug Info | IC50 = 8 nM | [20] | ||
4 | MK-2461 | Drug Info | IC50 = 10 nM | [8] | ||
5 | Rosiglitazone + metformin | Drug Info | IC50 = 28 nM | [15] | ||
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 | [8] | ||
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 | [9] | |
2 | E-3810 | Drug Info | IC50 = 10 nM | [2] | ||
3 | Romiplostim | Drug Info | IC50 = 50 nM | [10] | ||
4 | MK-2461 | Drug Info | IC50 = 78 nM | [8] | ||
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 | [8] | ||
Co-Target Name | Aurora kinase B (AURKB) | Clinical trial Target | ||||
UniProt ID | AURKB_HUMAN | |||||
Gene Name | AURKB | |||||
Synonyms |
Serine/threonine-protein kinase aurora-B; Serine/threonine-protein kinase 5; Serine/threonine-protein kinase 12; Serine/threonine protein kinase 12; STK5; STK12; Aurora/IPL1-related kinase 2; Aurora-related kinase 2; Aurora-B; Aurora-2 kinase; Aurora-2; Aurora- and Ipl1-like midbody-associated protein 1; Aurora 1; ARK2; ARK-2; AIRK2; AIM1; AIM-1; AIK2
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Representative Drug(s) | Rosiglitazone + metformin | Drug Info | IC50 = 35 nM | [22] | ||
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 | [10] | ||
Co-Target Name | Aurora kinase C (AURKC) | Clinical trial Target | ||||
UniProt ID | AURKC_HUMAN | |||||
Gene Name | AURKC | |||||
Synonyms |
Serine/threonine-protein kinase aurora-C; STK13; Aurora/Ipl1/Eg2 protein 2; Aurora/Ipl1-related kinase 3; Aurora-related kinase 3; Aurora-C; Aurora 3; ARK3; ARK-3; AIRK3; AIK3; AIE2
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Representative Drug(s) | Rosiglitazone + metformin | Drug Info | IC50 = 210 nM | [22] | ||
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 | [8] | ||
Co-Target Name | Tyrosine-protein kinase Lyn (JTK8) | Clinical trial Target | ||||
UniProt ID | LYN_HUMAN | |||||
Gene Name | LYN | |||||
Synonyms |
p56Lyn; p53Lyn; V-yes-1 Yamaguchi sarcoma viral related oncogene homolog; Lck/Yes-related novel protein tyrosine kinase
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Representative Drug(s) | Infigratinib | Drug Info | IC50 = 300 nM | [3] |
References | Top | ||||
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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 | 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 3 | Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase. J Med Chem. 2011 Oct 27;54(20):7066-83. | ||||
REF 4 | Fibroblast Growth Factor Receptor 4 (FGFR4) Selective Inhibitors as Hepatocellular Carcinoma Therapy: Advances and Prospects. J Med Chem. 2019 Mar 28;62(6):2905-2915. | ||||
REF 5 | Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases. Eur J Med Chem. 2019 Dec 15;184:111710. | ||||
REF 6 | 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 7 | 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 8 | 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 9 | Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors. J Med Chem. 2012 Dec 27;55(24):10797-822. | ||||
REF 10 | Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93. | ||||
REF 11 | 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 12 | 5-Substituted pyrido[2,3-d]pyrimidine, an inhibitor against three receptor tyrosine kinases. Bioorg Med Chem Lett. 2009 Feb 1;19(3):745-50. | ||||
REF 13 | Synthesis of hybrid anticancer agents based on kinase and histone deacetylase inhibitors. Medchemcomm. 2014;5:1829-33. | ||||
REF 14 | 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 15 | The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2012 Aug 1;22(15):4979-85. | ||||
REF 16 | 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 17 | 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 18 | Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region. Medchemcomm. 2017 Jun 8;8(8):1604-13. | ||||
REF 19 | A successful collaboration between academia, biotech and pharma led to discovery of erdafitinib, a selective FGFR inhibitor recently approved by the FDA. Med. Chem. Commun. 2019;10:1509-1511. | ||||
REF 20 | 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. | ||||
REF 21 | 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. | ||||
REF 22 | The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315. |
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