Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T58454 | Target Info | |||
| Target Name | Fibroblast growth factor receptor 2 (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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| Target Type | Successful Target | ||||
| Gene Name | FGFR2 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| 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) | LY2874455 | Drug Info | IC50 = 0.3 nM | Click to Show More | [1] | |
| 2 | Debio 1347 | Drug Info | IC50 = 9.3 nM | [6] | ||
| 3 | E-3810 | Drug Info | IC50 = 17.5 nM | [3] | ||
| 4 | E-3810 | Drug Info | IC50 = 17.5 nM | [7] | ||
| 5 | MK-2461 | Drug Info | IC50 = 65 nM | [8] | ||
| 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 | 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) | AEE-788 | Drug Info | IC50 = 2 nM | Click to Show More | [3] | |
| 2 | AEE-788 | Drug Info | IC50 = 2 nM | [4] | ||
| Co-Target Name | Erbb2 tyrosine kinase receptor (HER2) | Successful Target | ||||
| UniProt ID | ERBB2_HUMAN | |||||
| Gene Name | ERBB2 | |||||
| Synonyms |
p185erbB2; Tyrosine kinase-type cell surface receptor HER2; Receptor tyrosine-protein kinase erbB-2; Proto-oncogene c-ErbB-2; Proto-oncogene Neu; NGL; NEU; Metastatic lymph node gene 19 protein; MLN19; MLN 19; HER2; CD340
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| Representative Drug(s) | AEE-788 | Drug Info | IC50 = 2 nM | [3] | ||
| Co-Target Name | Erbb4 tyrosine kinase receptor (Erbb-4) | Successful Target | ||||
| UniProt ID | ERBB4_HUMAN | |||||
| Gene Name | ERBB4 | |||||
| Synonyms |
Tyrosine kinase-type cell surface receptor HER4; Receptor tyrosine-protein kinase erbB-4; Proto-oncogene-like protein c-ErbB-4; P180erbB4; HER4
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| Representative Drug(s) | AEE-788 | Drug Info | IC50 = 2 nM | [3] | ||
| 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) | LY2874455 | Drug Info | IC50 = 5.8 nM | Click to Show More | [5] | |
| 2 | E-3810 | Drug Info | IC50 = 25 nM | [3] | ||
| 3 | E-3810 | Drug Info | IC50 = 25 nM | [6] | ||
| 4 | MK-2461 | Drug Info | IC50 = 44 nM | [8] | ||
| 5 | AEE-788 | Drug Info | IC50 = 77 nM | [3] | ||
| 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 | [8] | ||
| 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 | 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 | [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 | 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 | Click to Show More | [8] | |
| 2 | AEE-788 | Drug Info | IC50 = 740 nM | [9] | ||
| Co-Target Name | Erbb3 tyrosine kinase receptor (Erbb-3) | Clinical trial Target | ||||
| UniProt ID | ERBB3_HUMAN | |||||
| Gene Name | ERBB3 | |||||
| Synonyms |
Tyrosine kinase-type cell surface receptor HER3; Receptor tyrosine-protein kinase erbB-3; Proto-oncogene-like protein c-ErbB-3; HER3; C-erbB3; C-erbB-3 protein
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| Representative Drug(s) | AEE-788 | Drug Info | IC50 = 2 nM | [3] | ||
| 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) | LY2874455 | Drug Info | IC50 = 3.2 nM | Click to Show More | [1] | |
| 2 | Debio 1347 | Drug Info | IC50 = 290 nM | [12] | ||
| 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) | LY2874455 | Drug Info | IC50 = 6.4 nM | Click to Show More | [10] | |
| 2 | Debio 1347 | Drug Info | IC50 = 22 nM | [12] | ||
| 3 | MK-2461 | Drug Info | IC50 = 50 nM | [8] | ||
| 4 | E-3810 | Drug Info | IC50 = 237.5 nM | [7] | ||
| 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 | [3] | |
| 2 | E-3810 | Drug Info | IC50 = 7 nM | [7] | ||
| 3 | MK-2461 | Drug Info | IC50 = 10 nM | [8] | ||
| 4 | AEE-788 | Drug Info | IC50 = 59 nM | [3] | ||
| 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 | [3] | |
| 2 | E-3810 | Drug Info | IC50 = 10 nM | [6] | ||
| 3 | MK-2461 | Drug Info | IC50 = 78 nM | [8] | ||
| Co-Target Name | Yes tyrosine kinase (YES) | Clinical trial Target | ||||
| UniProt ID | YES_HUMAN | |||||
| Gene Name | YES1 | |||||
| Synonyms |
p61-Yes; Yes p59-Fyn; Yes Protooncogene Syn; Tyrosine-protein kinase Yes; Proto-oncogene c-Yes
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| Representative Drug(s) | AEE-788 | Drug Info | IC50 = 13.1 nM | [11] | ||
| 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 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] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors. J Med Chem. 2018 Oct 25;61(20):9085-9104. | ||||
| 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 | Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors. J Med Chem. 2012 Dec 27;55(24):10797-822. | ||||
| REF 4 | Synthesis and in vitro EGFR (ErbB1) tyrosine kinase inhibitory activity of 4-N-substituted 6-aryl-7H-pyrrolo[2,3-d]pyrimidine-4-amines. Eur J Med Chem. 2011 Dec;46(12):6002-14. | ||||
| REF 5 | Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation. J Med Chem. 2016 Jul 28;59(14):6690-708. | ||||
| 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 | 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 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 | Pharmacophore modeling and virtual screening to identify potential RET kinase inhibitors. Bioorg Med Chem Lett. 2011 Aug 1;21(15):4490-7. | ||||
| REF 10 | 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 11 | Identification of potent Yes1 kinase inhibitors using a library screening approach. Bioorg Med Chem Lett. 2013 Aug 1;23(15):4398-403. | ||||
| REF 12 | 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. | ||||
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