Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T90848 | Target Info | |||
| Target Name | HGF/Met signaling pathway (HGF/Met pathway) | ||||
| Target Type | Successful Target | ||||
| Gene Name | NO-GeName | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| 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) | Crizotinib | Drug Info | EC50 = 0.47 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 | [2] | ||
| 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) | Crizotinib | Drug Info | Ki = 0.6 nM | [3] | ||
| 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 | [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) | Crizotinib | Drug Info | IC50 < 1 nM | [4] | ||
| 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) | Crizotinib | Drug Info | IC50 < 1 nM | [4] | ||
| 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 | [4] | ||
| 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 | [4] | ||
| 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 | [5] | ||
| 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) | Crizotinib | Drug Info | IC50 = 102 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) | Crizotinib | Drug Info | IC50 = 143 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) | Crizotinib | Drug Info | IC50 = 563 nM | [5] | ||
| 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) | Crizotinib | Drug Info | IC50 = 681 nM | [7] | ||
| 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 | [8] | ||
| 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 | [8] | ||
| 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) | Crizotinib | Drug Info | IC50 ~ 1000 nM | [8] | ||
| 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 | [8] | ||
| 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) | Crizotinib | Drug Info | IC50 ~ 1000 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) | Crizotinib | Drug Info | IC50 ~ 1000 nM | [8] | ||
| 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 | [8] | ||
| 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 | [4] | ||
| 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 | [8] | ||
| 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 | [9] | ||
| 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 | [8] | ||
| 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 | [8] | ||
| 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 | [8] | ||
| Co-Target Name | Nucleophosmin-ALK tyrosine kinase receptor fusion protein (NPM-ALK) | Co-Target | ||||
| UniProt ID | NPM_HUMAN-ALK_HUMAN | |||||
| Gene Name | NPM1-ALK | |||||
| Representative Drug(s) | Crizotinib | Drug Info | IC50 = 51 nM | [10] | ||
| 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) | Crizotinib | Drug Info | IC50 = 56 nM | [11] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Identification of a potent kinase inhibitor targeting EML4-ALK fusion protein in non-small cell lung cancer. Medchemcomm. 2017 Aug 25;8(10):1914-8. | ||||
| REF 2 | Drug Discovery Targeting Anaplastic Lymphoma Kinase (ALK). J Med Chem. 2019 Dec 26;62(24):10927-10954. | ||||
| REF 3 | 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 4 | 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 5 | Design, synthesis and structure-activity relationship study of aminopyridine derivatives as novel inhibitors of Janus kinase 2. Bioorg Med Chem Lett. 2019 Jun 15;29(12):1507-1513. | ||||
| REF 6 | 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 7 | Discovery of novel mutant-combating ALK and ROS1 dual inhibitors bearing imidazolidin-2-one moiety with reasonable PK properties. Eur J Med Chem. 2019 Jun 1;171:297-309. | ||||
| REF 8 | Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase. Eur J Med Chem. 2016 Jan 27;108:322-33. | ||||
| REF 9 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. Proc Natl Acad Sci U S A. 2007 Dec 11;104(50):19936-41. | ||||
| REF 10 | Synthesis and biological evaluation of benzo[4,5]imidazo[1,2-c]pyrimidine and benzo[4,5]imidazo[1,2-a]pyrazine derivatives as anaplastic lymphoma kinase inhibitors. Bioorg Med Chem. 2014 Feb 15;22(4):1303-12. | ||||
| REF 11 | Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. J Med Chem. 2015 Dec 10;58(23):9296-9308. | ||||
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