Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T84703 Target Info
Target Name BDNF/NT-3 growth factors receptor (TrkB)
Synonyms
Tropomyosin-related kinase B; TrkB tyrosine kinase; Trk-B; TRKB; Neurotrophic tyrosine kinase receptor type 2; GP145-TrkB
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Target Type Successful Target
Gene Name NTRK2
Biochemical Class Kinase
UniProt ID
NTRK2_HUMAN
Co-Targets of This Target  Top
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) Entrectinib Drug Info IC50 = 0.22 nM Click to Show More [1]
2 Larotrectinib Drug Info IC50 = 2 nM [3]
3 MK-2461 Drug Info IC50 = 46 nM [6]
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 NT-3 growth factor receptor (TrkC) Successful Target
UniProt ID NTRK3_HUMAN
Gene Name NTRK3
Synonyms
TrkC tyrosine kinase; Trk-C; TRKC; Neurotrophic tyrosine kinase receptor type 3; NT3 growth factor receptor; GP145TrkC; GP145-TrkC
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Representative Drug(s) Entrectinib Drug Info IC50 = 3 nM Click to Show More [4]
2 Larotrectinib Drug Info IC50 = 3.49 nM [5]
Co-Target Name Proto-oncogene c-Ros (ROS1) Successful Target
UniProt ID ROS1_HUMAN
Gene Name ROS1
Synonyms
c-Ros receptor tyrosine kinase; Receptor tyrosine kinase c-ros oncogene 1; ROS; Proto-oncogene tyrosine-protein kinase ROS; Proto-oncogene c-Ros-1; MCF3
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Representative Drug(s) Entrectinib Drug Info IC50 = 5 nM [4]
Co-Target Name ALK tyrosine kinase receptor (ALK) Successful Target
UniProt ID ALK_HUMAN
Gene Name ALK
Synonyms
CD246; Anaplastic lymphoma kinase
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Representative Drug(s) Entrectinib Drug Info Ki = 6.2 nM [4]
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 Click to Show More [6]
2 Entrectinib Drug Info IC50 = 164 nM [4]
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 [6]
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) Entrectinib Drug Info IC50 = 40 nM Click to Show More [4]
2 MK-2461 Drug Info IC50 = 230 nM [6]
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) MK-2461 Drug Info IC50 = 44 nM Click to Show More [6]
2 Entrectinib Drug Info IC50 ~ 1000 nM [4]
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) MK-2461 Drug Info IC50 = 65 nM Click to Show More [6]
2 Entrectinib Drug Info IC50 ~ 1000 nM [4]
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 [6]
Co-Target Name Janus kinase 1 (JAK-1) Successful Target
UniProt ID JAK1_HUMAN
Gene Name JAK1
Synonyms
Tyrosine-protein kinase JAK1; JAK1B; JAK1A
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Representative Drug(s) Entrectinib Drug Info IC50 = 112 nM [4]
Co-Target Name Insulin-like growth factor I receptor (IGF1R) Successful Target
UniProt ID IGF1R_HUMAN
Gene Name IGF1R
Synonyms
Type 1 insulin-like growth factor receptor; Insulin-like growth factor 1 receptor; IGF-IR; IGF-I receptor; IGF-1R; IGF-1 receptor; CD221 antigen; CD221
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Representative Drug(s) Entrectinib Drug Info IC50 = 122 nM [4]
Co-Target Name Insulin receptor (INSR) Successful Target
UniProt ID INSR_HUMAN
Gene Name INSR
Synonyms
IR; CD220 antigen; CD220
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Representative Drug(s) Entrectinib Drug Info IC50 = 209 nM [4]
Co-Target Name Janus kinase 3 (JAK-3) Successful Target
UniProt ID JAK3_HUMAN
Gene Name JAK3
Synonyms
Tyrosine-protein kinase JAK3; Leukocyte janus kinase; L-JAK
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Representative Drug(s) Entrectinib Drug Info IC50 = 349 nM [4]
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) Entrectinib Drug Info IC50 = 393 nM Click to Show More [4]
2 MK-2461 Drug Info IC50 = 640 nM [6]
Co-Target Name Tyrosine-protein kinase ABL1 (ABL) Successful Target
UniProt ID ABL1_HUMAN
Gene Name ABL1
Synonyms
p150; Proto-oncogene tyrosine-protein kinase ABL1; Proto-oncogene c-Abl; JTK7; C-ABL; Abl; Abelson tyrosine-protein kinase 1; Abelson murine leukemia viral oncogene homolog 1
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Representative Drug(s) Larotrectinib Drug Info IC50 ~ 1000 nM Click to Show More [5]
2 Entrectinib Drug Info IC50 ~ 1000 nM [4]
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) Entrectinib Drug Info IC50 ~ 1000 nM [4]
Co-Target Name LCK tyrosine protein kinase (LCK) Successful Target
UniProt ID LCK_HUMAN
Gene Name LCK
Synonyms
p56-LCK; Tyrosine-protein kinase Lck; T cell-specific protein-tyrosine kinase; Proto-oncogene tyrosine-protein kinase LCK; Proto-oncogene Lck; Protein YT16; Lymphocyte cell-specific protein-tyrosine kinase; Leukocyte C-terminal Src kinase; LSK; LCK p59-Fyn; LCK Protooncogene Syn
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Representative Drug(s) Entrectinib Drug Info IC50 ~ 1000 nM [4]
Co-Target Name Tyrosine-protein kinase SYK (SYK) Successful Target
UniProt ID KSYK_HUMAN
Gene Name SYK
Synonyms
p72-Syk; Spleen tyrosine kinase
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Representative Drug(s) Entrectinib Drug Info IC50 ~ 1000 nM [4]
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 [6]
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) MK-2461 Drug Info IC50 = 10 nM [6]
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 [6]
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 [6]
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) MK-2461 Drug Info IC50 = 78 nM Click to Show More [6]
2 Entrectinib Drug Info IC50 ~ 1000 nM [4]
Co-Target Name Focal adhesion kinase 1 (FAK) Clinical trial Target
UniProt ID FAK1_HUMAN
Gene Name PTK2
Synonyms
pp125FAK; p125FAK; Protein-tyrosine kinase 2; Protein phosphatase 1 regulatory subunit 71; PPP1R71; Focal adhesion kinase-related nonkinase; FRNK; FAK1; FADK 1; FADK
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Representative Drug(s) Entrectinib Drug Info IC50 = 140 nM [4]
Co-Target Name Tyrosine-protein kinase BRK (PTK6) Clinical trial Target
UniProt ID PTK6_HUMAN
Gene Name PTK6
Synonyms
Protein-tyrosine kinase 6; Breast tumor kinase; BRK
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Representative Drug(s) Entrectinib Drug Info IC50 = 195 nM [4]
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) Entrectinib Drug Info IC50 = 215 nM Click to Show More [4]
2 MK-2461 Drug Info IC50 = 290 nM [6]
Co-Target Name Protein kinase C beta (PRKCB) Clinical trial Target
UniProt ID KPCB_HUMAN
Gene Name PRKCB
Synonyms
Protein kinase C beta type; PRKCB1; PKCB; PKC-beta; PKC-B
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Representative Drug(s) Entrectinib Drug Info IC50 ~ 1000 nM [4]
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) Entrectinib Drug Info IC50 ~ 1000 nM [4]
Co-Target Name Activated CDC42 kinase 1 (ACK-1) Patented-recorded Target
UniProt ID ACK1_HUMAN
Gene Name TNK2
Synonyms
Tyrosine kinase non-receptor protein 2; ACK1; ACK-1
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Representative Drug(s) Entrectinib Drug Info IC50 = 70 nM [4]
Co-Target Name Echinoderm microtubule associated protein like 4-ALK tyrosine kinase receptor fusion protein (EML4-ALK) Co-Target
UniProt ID EMAL4_HUMAN-ALK_HUMAN
Gene Name EML4-ALK
Representative Drug(s) Entrectinib Drug Info IC50 = 28 nM [4]
Co-Target Name Cyclin dependent kinase 2-Cyclin A2 complex (CDK2-CCNA2) Co-Target
UniProt ID CDK2_HUMAN-CCNA2_HUMAN
Gene Name CDK2-CCNA2
Representative Drug(s) Entrectinib Drug Info IC50 ~ 1000 nM [4]
References  Top
REF 1 Type 2 inhibitor leads of human tropomyosin receptor kinase (hTrkA). Bioorg Med Chem Lett. 2019 Oct 1;29(19):126624.
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 Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application. J Med Chem. 2019 Feb 28;62(4):1731-1760.
REF 4 Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor. J Med Chem. 2016 Apr 14;59(7):3392-408.
REF 5 Design, synthesis and biological evaluation of 3-(imidazo[1,2-a]pyrazin-3-ylethynyl)-2-methylbenzamides as potent and selective pan-tropomyosin receptor kinase (TRK) inhibitors. Eur J Med Chem. 2019 Oct 1;179:470-482.
REF 6 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.

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