Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T56418 Target Info
Target Name ALK tyrosine kinase receptor (ALK)
Synonyms
CD246; Anaplastic lymphoma kinase
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Target Type Successful Target
Gene Name ALK
Biochemical Class Kinase
UniProt ID
ALK_HUMAN
Co-Targets of This Target  Top
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) PF-06463922 Drug Info Ki < 0.02 nM Click to Show More [1]
2 Lorlatinib Drug Info Ki < 0.02 nM [1]
3 Ceritinib Drug Info Ki = 0.4 nM [4]
4 Crizotinib Drug Info Ki = 0.6 nM [4]
5 AP26113 Drug Info IC50 = 1.9 nM [9]
6 Brigatinib Drug Info IC50 = 1.9 nM [10]
7 Entrectinib Drug Info IC50 = 5 nM [11]
8 Repotrectinib Drug Info IC50 = 8.4 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) Entrectinib Drug Info IC50 = 0.22 nM Click to Show More [2]
2 Repotrectinib Drug Info IC50 = 0.4 nM [3]
3 Crizotinib Drug Info IC50 < 1 nM [7]
4 TSR-011 Drug Info IC50 < 3 nM [3]
5 PF-06463922 Drug Info IC50 = 24 nM [1]
6 Lorlatinib Drug Info IC50 = 24 nM [1]
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) Crizotinib Drug Info IC50 = 0.51 nM Click to Show More [5]
2 X-396 Drug Info IC50 = 0.69 nM [6]
3 Ensartinib Drug Info IC50 = 0.74 nM [5]
4 Ceritinib Drug Info IC50 = 271 nM [18]
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) Crizotinib Drug Info IC50 < 1 nM [7]
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) Brigatinib Drug Info IC50 = 1 nM Click to Show More [8]
2 Ceritinib Drug Info IC50 = 19 nM [14]
3 Crizotinib Drug Info IC50 = 681 nM [19]
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) Crizotinib Drug Info IC50 < 1 nM Click to Show More [7]
2 Ceritinib Drug Info IC50 = 560 nM [13]
3 Entrectinib Drug Info IC50 ~ 1000 nM [11]
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) Crizotinib Drug Info IC50 = 2 nM Click to Show More [7]
2 TSR-011 Drug Info IC50 < 3 nM [3]
3 Entrectinib Drug Info IC50 = 3 nM [11]
4 PF-06463922 Drug Info Ki = 23 nM [4]
5 Lorlatinib Drug Info Ki = 23 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) Brigatinib Drug Info IC50 = 2.1 nM Click to Show More [10]
2 Ceritinib Drug Info IC50 = 60 nM [13]
3 Entrectinib Drug Info IC50 = 164 nM [11]
4 Crizotinib Drug Info IC50 ~ 1000 nM [20]
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) TSR-011 Drug Info IC50 < 3 nM Click to Show More [3]
2 Entrectinib Drug Info IC50 = 3 nM [11]
3 PF-06463922 Drug Info IC50 = 46 nM [1]
4 Lorlatinib Drug Info IC50 = 46 nM [1]
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) AP26113 Drug Info IC50 = 3.2 nM Click to Show More [10]
2 Ceritinib Drug Info IC50 = 8 nM [13]
3 Brigatinib Drug Info IC50 = 24.9 nM [10]
4 Entrectinib Drug Info IC50 = 122 nM [11]
5 Crizotinib Drug Info IC50 = 143 nM [10]
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) Alectinib Drug Info IC50 = 4.8 nM Click to Show More [12]
2 Entrectinib Drug Info IC50 = 393 nM [11]
3 Ceritinib Drug Info IC50 = 400 nM [13]
Co-Target Name Proto-oncogene c-Src (SRC) Successful Target
UniProt ID SRC_HUMAN
Gene Name SRC
Synonyms
pp60c-src; Tyrosine kinase (pp60(src)); Src tyrosine kinase; SRC1; Proto-oncogene tyrosine-protein kinase Src; Pp60(src); P60-Src; C-src TK; C-Src
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Representative Drug(s) Repotrectinib Drug Info IC50 = 5.3 nM Click to Show More [5]
2 Crizotinib Drug Info IC50 ~ 1000 nM [20]
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) Ceritinib Drug Info IC50 = 7 nM Click to Show More [13]
2 AP26113 Drug Info IC50 = 100 nM [10]
3 Crizotinib Drug Info IC50 = 102 nM [7]
4 Brigatinib Drug Info IC50 = 196 nM [10]
5 Entrectinib Drug Info IC50 = 209 nM [11]
6 TSR-011 Drug Info IC50 = 231 nM [17]
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) Crizotinib Drug Info IC50 = 24 nM Click to Show More [7]
2 Entrectinib Drug Info IC50 ~ 1000 nM [11]
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) Crizotinib Drug Info IC50 = 27 nM Click to Show More [15]
2 Entrectinib Drug Info IC50 = 40 nM [11]
3 Ceritinib Drug Info IC50 = 610 nM [13]
Co-Target Name Multidrug resistance protein 1 (ABCB1) Clinical trial Target
UniProt ID MDR1_HUMAN
Gene Name ABCB1
Synonyms
PGY1; P-glycoprotein 1; MDR1; CD243 antigen; CD243; ATP-binding cassette sub-family B member 1
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Representative Drug(s) Ceritinib Drug Info EC50 = 89 nM [16]
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 Click to Show More [11]
2 Crizotinib Drug Info IC50 = 563 nM [15]
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) Ceritinib Drug Info IC50 = 260 nM [13]
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 [11]
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) Crizotinib Drug Info IC50 ~ 1000 nM [20]
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) Crizotinib Drug Info IC50 ~ 1000 nM Click to Show More [20]
2 Entrectinib Drug Info IC50 ~ 1000 nM [11]
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) Crizotinib Drug Info IC50 ~ 1000 nM Click to Show More [20]
2 Entrectinib Drug Info IC50 ~ 1000 nM [11]
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 [11]
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) Crizotinib Drug Info IC50 ~ 1000 nM [20]
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) Crizotinib Drug Info IC50 ~ 1000 nM [20]
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 [11]
Co-Target Name Angiopoietin 1 receptor (TEK) Clinical trial Target
UniProt ID TIE2_HUMAN
Gene Name TEK
Synonyms
hTIE2; VMCM1; VMCM; Tyrosine-protein kinase receptor TIE-2; Tyrosine-protein kinase receptor TEK; Tyrosine kinase with Ig and EGF homology domains-2; Tunica interna endothelial cell kinase; TIE2; P140 TEK; Endothelial tyrosine kinase; Endothelial Cell-Specific Receptor TIE-2; CD202b antigen; CD202b
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Representative Drug(s) Crizotinib Drug Info IC50 = 5 nM [7]
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) PF-06463922 Drug Info IC50 = 17 nM Click to Show More [1]
2 Lorlatinib Drug Info IC50 = 17 nM [1]
3 Entrectinib Drug Info IC50 = 140 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) Crizotinib Drug Info IC50 ~ 100 nM [20]
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 [11]
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 [11]
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) Crizotinib Drug Info IC50 = 300 nM [21]
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) Ceritinib Drug Info IC50 = 430 nM [13]
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) Ceritinib Drug Info IC50 = 840 nM [13]
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) Ceritinib Drug Info IC50 = 950 nM [13]
Co-Target Name Ephrin type-A receptor 2 (EPHA2) Clinical trial Target
UniProt ID EPHA2_HUMAN
Gene Name EPHA2
Synonyms
Tyrosine-protein kinase receptor ECK; Epithelial cell kinase; EphA2receptor; ECK
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Representative Drug(s) Crizotinib Drug Info IC50 ~ 1000 nM [20]
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) Crizotinib Drug Info IC50 ~ 1000 nM [20]
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) Entrectinib Drug Info IC50 ~ 1000 nM [11]
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 [11]
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 [11]
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) PF-06463922 Drug Info IC50 = 17 nM Click to Show More [1]
2 Lorlatinib Drug Info IC50 = 17 nM [1]
3 Entrectinib Drug Info IC50 = 70 nM [11]
Co-Target Name TYRO3 tyrosine kinase receptor (TYRO3) Patented-recorded Target
UniProt ID TYRO3_HUMAN
Gene Name TYRO3
Synonyms
Tyrosine-protein kinase receptor TYRO3; Tyrosine-protein kinase TIF; Tyrosine-protein kinase SKY; Tyrosine-protein kinase RSE; Tyrosine-protein kinase DTK; Tyrosine-protein kinase BYK; TIF; SKY; RSE; DTK; BYK
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Representative Drug(s) Crizotinib Drug Info IC50 ~ 100 nM [20]
Co-Target Name SRSF protein kinase 1 (SRPK1) Patented-recorded Target
UniProt ID SRPK1_HUMAN
Gene Name SRPK1
Synonyms
Serine/arginine-rich protein-specific kinase 1; SR-protein-specific kinase 1; SFRS protein kinase 1
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Representative Drug(s) Alectinib Drug Info IC50 = 195 nM [22]
Co-Target Name Leukocyte receptor tyrosine kinase (LTK) Literature-reported Target
UniProt ID LTK_HUMAN
Gene Name LTK
Synonyms
TYK1; Protein tyrosine kinase 1; Leukocyte tyrosine kinase receptor
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Representative Drug(s) PF-06463922 Drug Info IC50 = 2.7 nM Click to Show More [1]
2 Lorlatinib Drug Info IC50 = 2.7 nM [1]
Co-Target Name Proto-oncogene c-Fer (FER) Literature-reported Target
UniProt ID FER_HUMAN
Gene Name FER
Synonyms
p94-Fer; Tyrosine-protein kinase Fer; Tyrosine kinase 3; TYK3; Fujinami poultry sarcoma/Feline sarcoma-related protein Fer; Feline encephalitis virus-related kinase FER
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Representative Drug(s) PF-06463922 Drug Info IC50 = 3.3 nM Click to Show More [1]
2 Lorlatinib Drug Info IC50 = 3.3 nM [1]
Co-Target Name Proto-oncogene c-Fes (FES) Literature-reported Target
UniProt ID FES_HUMAN
Gene Name FES
Synonyms
p93c-fes; Tyrosine-protein kinase Fes/Fps; Proto-oncogene c-Fps; Feline sarcoma/Fujinami avian sarcoma oncogene homolog; FPS
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Representative Drug(s) PF-06463922 Drug Info IC50 = 6 nM Click to Show More [1]
2 Lorlatinib Drug Info IC50 = 6 nM [1]
Co-Target Name Focal adhesion kinase 2 (PTK2B) Literature-reported Target
UniProt ID FAK2_HUMAN
Gene Name PTK2B
Synonyms
Related adhesion focal tyrosine kinase; RAFTK; Protein-tyrosine kinase 2-beta; Proline-rich tyrosine kinase 2; PYK2; FAK2; FADK 2; Cell adhesion kinase beta; Calcium-regulated non-receptor proline-rich tyrosine kinase; Calcium-dependent tyrosine kinase; CAKB; CAK-beta; CADTK
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Representative Drug(s) PF-06463922 Drug Info IC50 = 14 nM Click to Show More [1]
2 Lorlatinib Drug Info IC50 = 14 nM [1]
Co-Target Name Testis-specific serine/threonine-protein kinase 1 (TSSK1B) Co-Target
UniProt ID TSSK1_HUMAN
Gene Name TSSK1B
Synonyms
TSK-1; TSK1; TSSK-1; Testis-specific kinase 1; Serine/threonine-protein kinase 22A
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Representative Drug(s) Ceritinib Drug Info IC50 = 23 nM [13]
Co-Target Name Tyrosine-protein kinase FRK (FRK) Co-Target
UniProt ID FRK_HUMAN
Gene Name FRK
Synonyms
FYN-related kinase; Nuclear tyrosine protein kinase RAK; Protein-tyrosine kinase 5
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Representative Drug(s) PF-06463922 Drug Info IC50 = 53 nM Click to Show More [1]
2 Lorlatinib Drug Info IC50 = 53 nM [1]
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 [11]
References  Top
REF 1 Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations. J Med Chem. 2014 Jun 12;57(11):4720-44.
REF 2 Type 2 inhibitor leads of human tropomyosin receptor kinase (hTrkA). Bioorg Med Chem Lett. 2019 Oct 1;29(19):126624.
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 First macrocyclic 3rd-generation ALK inhibitor for treatment of ALK/ROS1 cancer: Clinical and designing strategy update of lorlatinib. Eur J Med Chem. 2017 Jul 7;134:348-56.
REF 5 Drug Discovery Targeting Anaplastic Lymphoma Kinase (ALK). J Med Chem. 2019 Dec 26;62(24):10927-10954.
REF 6 Novel 5-(benzyloxy)pyridin-2(1H)-one derivatives as potent c-Met inhibitors. Bioorg Med Chem Lett. 2013 Apr 15;23(8):2408-13.
REF 7 Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). J Med Chem. 2011 Sep 22;54(18):6342-63.
REF 8 Discovery of an Oleanolic Acid/Hederagenin-Nitric Oxide Donor Hybrid as an EGFR Tyrosine Kinase Inhibitor for Non-Small-Cell Lung Cancer. J Nat Prod. 2019 Nov 22;82(11):3065-3073.
REF 9 Synthesis and biological evaluation of new pyrazol-4-ylpyrimidine derivatives as potential ROS1 kinase inhibitors. Eur J Med Chem. 2015 Jan 27;90:195-208.
REF 10 Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. J Med Chem. 2016 May 26;59(10):4948-64.
REF 11 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 12 An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core. Eur J Med Chem. 2016 Aug 8;118:244-9.
REF 13 Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials. J Med Chem. 2013 Jul 25;56(14):5675-90.
REF 14 Discovery of a potent dual ALK and EGFR T790M inhibitor. Eur J Med Chem. 2017 Aug 18;136:497-510.
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