Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T40474 | Target Info | |||
| Target Name | Proto-oncogene c-Met (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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| Target Type | Successful Target | ||||
| Gene Name | MET | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| 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) | Cabozantinib | Drug Info | IC50 = 0.035 nM | Click to Show More | [1] | |
| 2 | XL880 | Drug Info | IC50 = 0.8 nM | [4] | ||
| 3 | MGCD516 | Drug Info | IC50 = 5 nM | [7] | ||
| 4 | Altiratinib | Drug Info | IC50 = 9.2 nM | [13] | ||
| 5 | E-7050 | Drug Info | IC50 = 16 nM | [1] | ||
| 6 | MK-2461 | Drug Info | IC50 = 44 nM | [17] | ||
| 7 | BMS-777607 | Drug Info | IC50 = 138.7 nM | [21] | ||
| 8 | Crizotinib | Drug Info | IC50 ~ 1000 nM | [25] | ||
| 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 | [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 | Click to Show More | [3] | |
| 2 | XL880 | Drug Info | Ki = 8.2 nM | [3] | ||
| 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) | Altiratinib | Drug Info | IC50 = 0.83 nM | [1] | ||
| 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) | Altiratinib | Drug Info | IC50 = 0.85 nM | Click to Show More | [1] | |
| 2 | Crizotinib | Drug Info | IC50 < 1 nM | [5] | ||
| 3 | MGCD516 | Drug Info | IC50 = 5 nM | [7] | ||
| 4 | MK-2461 | Drug Info | IC50 = 46 nM | [17] | ||
| 5 | BMS-777607 | Drug Info | IC50 = 290 nM | [15] | ||
| 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 | Click to Show More | [5] | |
| 2 | BMS-777607 | Drug Info | IC50 = 1.1 nM | [6] | ||
| 3 | MGCD516 | Drug Info | IC50 = 1.5 nM | [7] | ||
| 4 | LY2801653 | Drug Info | IC50 = 2 nM | [8] | ||
| 5 | Cabozantinib | Drug Info | IC50 = 3.4 nM | [9] | ||
| 6 | XL880 | Drug Info | IC50 = 11 nM | [8] | ||
| 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 | [5] | |
| 2 | BMS-777607 | Drug Info | IC50 = 120 nM | [15] | ||
| 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 | [5] | |
| 2 | Altiratinib | Drug Info | IC50 = 4.6 nM | [1] | ||
| 3 | MGCD516 | Drug Info | IC50 = 9 nM | [7] | ||
| 4 | MK-2461 | Drug Info | IC50 = 61 nM | [17] | ||
| 5 | BMS-777607 | Drug Info | IC50 = 190 nM | [15] | ||
| 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) | Cabozantinib | Drug Info | IC50 = 2.4 nM | Click to Show More | [9] | |
| 2 | BMS-777607 | Drug Info | IC50 = 594 nM | [19] | ||
| 3 | MK-2461 | Drug Info | IC50 = 640 nM | [17] | ||
| 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) | XL880 | Drug Info | IC50 = 3.6 nM | Click to Show More | [10] | |
| 2 | Cabozantinib | Drug Info | IC50 = 6 nM | [1] | ||
| 3 | MGCD516 | Drug Info | IC50 = 8 nM | [7] | ||
| 4 | BMS-777607 | Drug Info | IC50 = 16 nM | [15] | ||
| 5 | MK-2461 | Drug Info | IC50 = 22 nM | [17] | ||
| 6 | Crizotinib | Drug Info | IC50 ~ 1000 nM | [25] | ||
| 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) | XL880 | Drug Info | IC50 = 3.6 nM | Click to Show More | [1] | |
| 2 | BMS-777607 | Drug Info | IC50 = 28 nM | [19] | ||
| 3 | MK-2461 | Drug Info | IC50 < 100 nM | [17] | ||
| 4 | Crizotinib | Drug Info | IC50 ~ 1000 nM | [25] | ||
| 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) | Cabozantinib | Drug Info | IC50 = 4 nM | Click to Show More | [11] | |
| 2 | XL880 | Drug Info | IC50 = 4 nM | [12] | ||
| 3 | MGCD516 | Drug Info | IC50 = 6 nM | [7] | ||
| 4 | BMS-777607 | Drug Info | IC50 = 144 nM | [19] | ||
| 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) | XL880 | Drug Info | IC50 = 9.4 nM | Click to Show More | [14] | |
| 2 | BMS-777607 | Drug Info | IC50 ~ 500 nM | [15] | ||
| 3 | Crizotinib | Drug Info | IC50 ~ 1000 nM | [25] | ||
| 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) | Cabozantinib | Drug Info | IC50 = 11.3 nM | Click to Show More | [1] | |
| 2 | MK-2461 | Drug Info | IC50 = 65 nM | [17] | ||
| 3 | Crizotinib | Drug Info | IC50 ~ 1000 nM | [25] | ||
| 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) | Cabozantinib | Drug Info | IC50 = 19 nM | Click to Show More | [16] | |
| 2 | Crizotinib | Drug Info | IC50 = 681 nM | [24] | ||
| 3 | BMS-777607 | Drug Info | IC50 ~ 1000 nM | [19] | ||
| 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 | [5] | ||
| 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 | [18] | |
| 2 | MK-2461 | Drug Info | IC50 = 230 nM | [17] | ||
| 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 | [17] | ||
| 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) | XL880 | Drug Info | Ki = 59.7 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) | Crizotinib | Drug Info | IC50 = 102 nM | [5] | ||
| 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 | [22] | ||
| 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) | Cabozantinib | Drug Info | IC50 = 178 nM | Click to Show More | [23] | |
| 2 | BMS-777607 | Drug Info | IC50 ~ 500 nM | [15] | ||
| 3 | Crizotinib | Drug Info | IC50 ~ 1000 nM | [25] | ||
| 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 | [18] | ||
| 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 | [25] | ||
| 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) | XL880 | Drug Info | IC50 = 0.8 nM | Click to Show More | [26] | |
| 2 | MK-2461 | Drug Info | IC50 = 10 nM | [17] | ||
| 3 | Cabozantinib | Drug Info | IC50 = 12 nM | [1] | ||
| 4 | Crizotinib | Drug Info | IC50 ~ 1000 nM | [25] | ||
| 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) | XL880 | Drug Info | IC50 = 1.1 nM | Click to Show More | [1] | |
| 2 | Crizotinib | Drug Info | IC50 = 5 nM | [5] | ||
| 3 | Altiratinib | Drug Info | IC50 = 8 nM | [1] | ||
| 4 | Cabozantinib | Drug Info | IC50 = 14.3 nM | [29] | ||
| 5 | BMS-777607 | Drug Info | IC50 ~ 500 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) | LY2801653 | Drug Info | IC50 = 1.2 nM | Click to Show More | [7] | |
| 2 | BMS-777607 | Drug Info | IC50 = 1.8 nM | [15] | ||
| 3 | XL880 | Drug Info | IC50 = 3 nM | [1] | ||
| 4 | MK-2461 | Drug Info | IC50 = 7 nM | [17] | ||
| 5 | MK-8033 | Drug Info | IC50 = 7 nM | [28] | ||
| 6 | Cabozantinib | Drug Info | IC50 = 69 nM | [23] | ||
| 7 | Crizotinib | Drug Info | IC50 = 300 nM | [31] | ||
| 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) | XL880 | Drug Info | IC50 = 2.8 nM | Click to Show More | [26] | |
| 2 | Cabozantinib | Drug Info | IC50 = 6 nM | [27] | ||
| 3 | MK-2461 | Drug Info | IC50 = 78 nM | [17] | ||
| 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) | BMS-777607 | Drug Info | IC50 = 14 nM | Click to Show More | [15] | |
| 2 | MK-2461 | Drug Info | IC50 = 24 nM | [17] | ||
| 3 | Crizotinib | Drug Info | IC50 ~ 100 nM | [25] | ||
| 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 | [17] | ||
| 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) | BMS-777607 | Drug Info | IC50 = 78 nM | [15] | ||
| Co-Target Name | MAP kinase signal-integrating kinase 2 (MKNK2) | Clinical trial Target | ||||
| UniProt ID | MKNK2_HUMAN | |||||
| Gene Name | MKNK2 | |||||
| Synonyms |
Mnk2; MAPK signal-integrating kinase 2
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| Representative Drug(s) | LY2801653 | Drug Info | IC50 = 109 nM | Click to Show More | [30] | |
| 2 | BMS-777607 | Drug Info | IC50 ~ 500 nM | [15] | ||
| Co-Target Name | MAPK signal-integrating kinase 1 (MKNK1) | Clinical trial Target | ||||
| UniProt ID | MKNK1_HUMAN | |||||
| Gene Name | MKNK1 | |||||
| Synonyms |
Mnk1; MAP kinase signal-integrating kinase 1
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| Representative Drug(s) | LY2801653 | Drug Info | IC50 = 130 nM | [30] | ||
| 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 | [17] | ||
| Co-Target Name | Ephrin type-A receptor 3 (EPHA3) | Clinical trial Target | ||||
| UniProt ID | EPHA3_HUMAN | |||||
| Gene Name | EPHA3 | |||||
| Synonyms |
hEK4; Tyrosineprotein kinase receptor ETK1; Tyrosineprotein kinase TYRO4; Tyrosine-protein kinase receptor ETK1; Tyrosine-protein kinase TYRO4; TYRO4; Human embryo kinase; HEK; Ephrin typeA receptor 3; Ephlike tyrosine kinase 1; Eph-like tyrosine kinase 1; ETK1; ETK protein; EPHlike kinase 4; EPH-like kinase 4; EK4
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| Representative Drug(s) | BMS-777607 | Drug Info | IC50 ~ 500 nM | [15] | ||
| 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 | [25] | ||
| 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) | BMS-777607 | Drug Info | IC50 = 4.3 nM | Click to Show More | [15] | |
| 2 | Crizotinib | Drug Info | IC50 ~ 100 nM | [25] | ||
| Co-Target Name | B lymphocyte kinase (BLK) | Patented-recorded Target | ||||
| UniProt ID | BLK_HUMAN | |||||
| Gene Name | BLK | |||||
| Synonyms |
p55-Blk; Tyrosine-protein kinase Blk
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| Representative Drug(s) | BMS-777607 | Drug Info | IC50 ~ 500 nM | [15] | ||
| Co-Target Name | Muscle-specific kinase receptor (MUSK) | Literature-reported Target | ||||
| UniProt ID | MUSK_HUMAN | |||||
| Gene Name | MUSK | |||||
| Synonyms |
Muscle-specific tyrosine-protein kinase receptor; Muscle, skeletal receptor tyrosine-protein kinase; MuSK
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| Representative Drug(s) | BMS-777607 | Drug Info | IC50 ~ 500 nM | [15] | ||
| 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 | [32] | ||
| 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 | [33] | ||
| Co-Target Name | Kinesin 1 heavy chain-Tyrosine protein kinase receptor RET (KIF5B-RET) | Co-Target | ||||
| UniProt ID | KINH_HUMAN-RET_HUMAN | |||||
| Gene Name | KIF5B-RET | |||||
| Representative Drug(s) | Cabozantinib | Drug Info | IC50 = 190 nM | [34] | ||
| Co-Target Name | Serine/threonine-protein kinase 10 (STK10) | Co-Target | ||||
| UniProt ID | STK10_HUMAN | |||||
| Gene Name | STK10 | |||||
| Synonyms |
Lymphocyte-oriented kinase
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| Representative Drug(s) | BMS-777607 | Drug Info | IC50 ~ 500 nM | [15] | ||
| Co-Target Name | Coiled coil domain containing protein 6-Proto oncogene c Ret complex (CCDC6-RET) | Co-Target | ||||
| UniProt ID | CCDC6_HUMAN-RET_HUMAN | |||||
| Gene Name | CCDC6-RET | |||||
| Representative Drug(s) | Cabozantinib | Drug Info | IC50 = 889 nM | [35] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | The "Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules. J Med Chem. 2016 Oct 13;59(19):8712-56. | ||||
| REF 2 | 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 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 | Design, synthesis and structure-activity relationships of novel 4-phenoxyquinoline derivatives containing pyridazinone moiety as potential antitumor agents. Eur J Med Chem. 2014 Aug 18;83:581-93. | ||||
| REF 5 | 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 6 | Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors. ACS Med Chem Lett. 2011 Dec 8;2(12):907-912. | ||||
| REF 7 | Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application. J Med Chem. 2019 Feb 28;62(4):1731-1760. | ||||
| REF 8 | AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective. J Med Chem. 2016 Apr 28;59(8):3593-608. | ||||
| REF 9 | The discovery of novel benzothiazinones as highly selective non-ATP competitive glycogen synthase kinase 3beta inhibitors for the treatment of ovarian cancer. Eur J Med Chem. 2017 Jul 28;135:370-81. | ||||
| REF 10 | Design, synthesis and structure-activity relationships of novel 4-phenoxyquinoline derivatives containing 1,2,4-triazolone moiety as c-Met kinase inhibitors. Eur J Med Chem. 2016 Nov 10;123:431-46. | ||||
| REF 11 | Design, synthesis and evaluation of highly selective pyridone-based class II MET inhibitors. Bioorg Med Chem Lett. 2014 Aug 1;24(15):3351-5. | ||||
| REF 12 | Discovery and optimization of novel 4-phenoxy-6,7-disubstituted quinolines possessing semicarbazones as c-Met kinase inhibitors. Bioorg Med Chem. 2013 Sep 1;21(17):5246-60. | ||||
| REF 13 | Exploration of novel pyrrolo[2,1-f][1,2,4]triazine derivatives with improved anticancer efficacy as dual inhibitors of c-Met/VEGFR-2. Eur J Med Chem. 2018 Oct 5;158:814-31. | ||||
| REF 14 | Design, synthesis and evaluation of sulfonylurea-containing 4-phenoxyquinolines as highly selective c-Met kinase inhibitors. Bioorg Med Chem. 2019 Jul 1;27(13):2801-2812. | ||||
| REF 15 | Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607... J Med Chem. 2009 Mar 12;52(5):1251-4. | ||||
| REF 16 | Discovery of thiazolidin-4-one urea analogues as novel multikinase inhibitors that potently inhibit FLT3 and VEGFR2. Bioorg Med Chem. 2019 May 15;27(10):2127-2139. | ||||
| REF 17 | 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 18 | 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 19 | Synthesis and evaluation of a series of pyridine and pyrimidine derivatives as type II c-Met inhibitors. Bioorg Med Chem. 2017 Jun 15;25(12):3195-205. | ||||
| REF 20 | 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 21 | 2,7-naphthyridinone-based MET kinase inhibitors: A promising novel scaffold for antitumor drug development. Eur J Med Chem. 2019 Sep 15;178:705-714. | ||||
| REF 22 | 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 23 | Identification of novel N1-(2-aryl-1, 3-thiazolidin-4-one)-N3-aryl ureas showing potent multi-tyrosine kinase inhibitory activities. Eur J Med Chem. 2018 Feb 25;146:368-80. | ||||
| REF 24 | 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 25 | 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 26 | Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors. J Med Chem. 2012 Dec 27;55(24):10797-822. | ||||
| REF 27 | Evolution in medicinal chemistry of sorafenib derivatives for hepatocellular carcinoma. Eur J Med Chem. 2019 Oct 1;179:916-935. | ||||
| REF 28 | Discovery of 1-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]-N-(pyridin-2-ylmethyl)methanesulfonamide (MK-8033): A Specific c-Met/Ron dual kinase inhibitor with preferential affinity for the activated state of c-Met. J Med Chem. 2013 Mar 28;56(6):2294-310. | ||||
| REF 29 | Structure-based design, synthesis, and evaluation of 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine derivatives as novel c-Met inhibitors. Eur J Med Chem. 2017 Sep 29;138:942-951. | ||||
| REF 30 | Stepwise Evolution of Fragment Hits against MAPK Interacting Kinases 1 and 2. J Med Chem. 2020 Jan 23;63(2):621-637. | ||||
| REF 31 | 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 32 | 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 33 | Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. J Med Chem. 2015 Dec 10;58(23):9296-9308. | ||||
| REF 34 | The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity. Eur J Med Chem. 2016 Apr 13;112:20-32. | ||||
| REF 35 | 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. | ||||
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