Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
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
FGFR1_HUMAN
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 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 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 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 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
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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