Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T80975 Target Info
Target Name Vascular endothelial growth factor receptor 2 (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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Target Type Successful Target
Gene Name KDR
Biochemical Class Kinase
UniProt ID
VGFR2_HUMAN
Co-Targets of This Target  Top
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) HKI-272 Drug Info IC50 = 0.08 nM Click to Show More [1]
2 Drug Info IC50 = 2.96 nM [22]
3 HKI-272 Drug Info IC50 = 3 nM [23]
4 Drug Info IC50 = 6.27 nM [29]
5 Vandetanib Drug Info IC50 = 11 nM [36]
6 Cabozantinib Drug Info IC50 = 19 nM [38]
7 Sunitinib Drug Info IC50 = 31.8 nM [42]
8 VATALANIB Drug Info IC50 = 457.7 nM [1]
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) Axitinib Drug Info IC50 = 0.2 nM Click to Show More [2]
2 Drug Info IC50 = 80 nM [8]
3 Vandetanib Drug Info IC50 = 86 nM [43]
4 Sunitinib Drug Info IC50 = 410 nM [10]
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 Click to Show More [3]
2 XL880 Drug Info IC50 = 0.4 nM [4]
3 Cabozantinib Drug Info IC50 = 1.3 nM [12]
4 Altiratinib Drug Info IC50 = 2.7 nM [7]
5 E-7050 Drug Info IC50 = 14 nM [3]
Co-Target Name Serine/threonine-protein kinase B-raf (BRAF) Successful Target
UniProt ID BRAF_HUMAN
Gene Name BRAF
Synonyms
V-Raf murine sarcoma viral oncogene homolog B1; RAFB1; Proto-oncogene B-Raf; P94; BRAF1; BRAF(V599E); BRAF serine/threonine kinase; B-raf protein; B-Raf
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Representative Drug(s) RAF265 Drug Info IC50 = 0.5 nM Click to Show More [5]
2 Drug Info IC50 = 1 nM [8]
3 Regorafenib Drug Info IC50 = 1.5 nM [13]
4 PLX-4720 Drug Info Ki = 2.6 nM [21]
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) Sunitinib Drug Info IC50 = 0.7 nM Click to Show More [6]
2 Drug Info IC50 = 2 nM [15]
3 Cabozantinib Drug Info IC50 = 4 nM [25]
4 XL880 Drug Info IC50 = 4 nM [26]
5 Regorafenib Drug Info IC50 = 6.1 nM [28]
6 OSI-930 Drug Info IC50 = 10 nM [34]
7 Drug Info IC50 = 10 nM [8]
8 RAF265 Drug Info IC50 = 20 nM [5]
9 Romiplostim Drug Info IC50 = 35 nM [43]
10 Vandetanib Drug Info IC50 = 343 nM [43]
11 VATALANIB Drug Info IC50 = 730 nM [58]
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 [7]
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 [7]
2 CEP-11981 Drug Info IC50 = 3 nM [24]
3 MK-2461 Drug Info IC50 = 46 nM [39]
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) HKI-272 Drug Info IC50 = 1 nM Click to Show More [9]
2 HKI-272 Drug Info IC50 = 3 nM [23]
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) Sunitinib Drug Info IC50 < 1 nM Click to Show More [10]
2 Lenvatinib Drug Info Ki = 1.5 nM [14]
3 Cabozantinib Drug Info IC50 = 2.4 nM [19]
4 CEP-11981 Drug Info IC50 = 5 nM [24]
5 Drug Info IC50 = 6 nM [14]
6 TAK-593 Drug Info IC50 = 18 nM [27]
7 Vandetanib Drug Info IC50 = 49 nM [45]
8 Romiplostim Drug Info IC50 = 170 nM [52]
9 MK-2461 Drug Info IC50 = 640 nM [39]
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) Drug Info IC50 = 1.3 nM Click to Show More [11]
2 Sunitinib Drug Info IC50 = 2.5 nM [20]
3 XL880 Drug Info IC50 = 3.6 nM [4]
4 Cabozantinib Drug Info IC50 = 6 nM [7]
5 MK-2461 Drug Info IC50 = 22 nM [39]
6 CYC116 Drug Info IC50 = 25.12 nM [40]
7 CEP-11981 Drug Info IC50 = 71 nM [24]
8 Regorafenib Drug Info IC50 = 82 nM [51]
9 Romiplostim Drug Info IC50 = 160 nM [52]
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) Regorafenib Drug Info IC50 = 1.5 nM Click to Show More [13]
2 XL999 Drug Info IC50 = 4 nM [16]
3 Drug Info IC50 = 4.63 nM [22]
4 Cabozantinib Drug Info IC50 = 11.3 nM [7]
5 CEP-11981 Drug Info IC50 = 13 nM [24]
6 E-3810 Drug Info IC50 = 17.5 nM [34]
7 E-3810 Drug Info IC50 = 17.5 nM [37]
8 Brivanib Drug Info IC50 = 28 nM [41]
9 MK-2461 Drug Info IC50 = 65 nM [39]
10 Sunitinib Drug Info IC50 = 170 nM [53]
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) Regorafenib Drug Info IC50 = 1.5 nM Click to Show More [13]
2 Sunitinib Drug Info IC50 = 2 nM [17]
3 Drug Info IC50 = 4 nM [15]
4 RAF265 Drug Info IC50 = 6 nM [5]
5 XL880 Drug Info IC50 = 9.4 nM [33]
6 Drug Info IC50 = 10 nM [8]
7 TAK-593 Drug Info IC50 = 13 nM [27]
8 Rosiglitazone + metformin Drug Info IC50 = 50 nM [46]
9 Romiplostim Drug Info IC50 = 68 nM [49]
10 Vandetanib Drug Info IC50 = 477 nM [43]
11 VATALANIB Drug Info IC50 = 490 nM [57]
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) XL999 Drug Info IC50 = 2 nM Click to Show More [16]
2 Drug Info IC50 = 2.26 nM [18]
3 XL880 Drug Info IC50 = 3.6 nM [7]
4 TAK-593 Drug Info IC50 = 4.3 nM [27]
5 MK-2461 Drug Info IC50 < 100 nM [39]
6 Sunitinib Drug Info IC50 = 130 nM [20]
7 Romiplostim Drug Info IC50 = 200 nM [55]
8 CEP-11981 Drug Info IC50 = 246 nM [24]
9 KRN633 Drug Info IC50 = 970 nM [60]
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) HKI-272 Drug Info IC50 = 3 nM [23]
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) Cabozantinib Drug Info IC50 = 3.4 nM Click to Show More [19]
2 Sunitinib Drug Info IC50 = 9 nM [32]
3 XL880 Drug Info IC50 = 11 nM [35]
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) Altiratinib Drug Info IC50 = 4.6 nM Click to Show More [7]
2 CEP-11981 Drug Info IC50 = 5 nM [24]
3 MK-2461 Drug Info IC50 = 61 nM [39]
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) XL880 Drug Info Ki = 8.2 nM [30]
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) Sunitinib Drug Info IC50 = 8.9 nM Click to Show More [31]
2 OSI-930 Drug Info IC50 = 22 nM [34]
3 Drug Info IC50 = 60 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) CEP-11981 Drug Info IC50 = 37 nM Click to Show More [24]
2 Vandetanib Drug Info IC50 = 44 nM [44]
3 Sunitinib Drug Info IC50 = 152.8 nM [31]
4 Cabozantinib Drug Info IC50 = 178 nM [54]
5 Drug Info IC50 = 390 nM [10]
6 CYC116 Drug Info Ki = 820 nM [59]
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 Click to Show More [39]
2 E-3810 Drug Info IC50 = 82.5 nM [34]
3 E-3810 Drug Info IC50 = 82.5 nM [37]
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) Sunitinib Drug Info IC50 = 54.64 nM Click to Show More [31]
2 CEP-11981 Drug Info IC50 = 132 nM [24]
Co-Target Name 5-HT 2B receptor (HTR2B) Successful Target
UniProt ID 5HT2B_HUMAN
Gene Name HTR2B
Synonyms
Serotonin receptor 2B; 5-hydroxytryptamine receptor 2B; 5-HT2B; 5-HT-2B; 5-HT 2B
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Representative Drug(s) Drug Info Ki = 56 nM [47]
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 [48]
Co-Target Name Platelet-derived growth factor receptor (PDGFR) Successful Target
UniProt ID PGFRA_HUMAN; PGFRB_HUMAN
Gene Name NO-GeName
Synonyms
Platelet-derived growth factor receptor tyrosine kinase; PDGFR kinase; PDGF-R
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Representative Drug(s) Sunitinib Drug Info IC50 = 80 nM [50]
Co-Target Name Tyrosine-protein kinase BTK (ATK) Successful Target
UniProt ID BTK_HUMAN
Gene Name BTK
Synonyms
Bruton's tyrosine kinase; Bruton tyrosine kinase; BPK; B-cell progenitor kinase; B cell progenitor kinase; Agammaglobulinemia tyrosine kinase; Agammaglobulinaemia tyrosine kinase; AGMX1
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Representative Drug(s) CEP-11981 Drug Info IC50 = 93 nM [24]
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 [39]
Co-Target Name Voltage-gated potassium channel Kv11.1 (KCNH2) Successful Target
UniProt ID KCNH2_HUMAN
Gene Name KCNH2
Synonyms
hERG1; hERG-1; Voltage-gated potassium channel subunit Kv11.1; Potassium voltage-gated channel subfamily H member 2; HERG K+ channel; HERG; H-ERG; Ether-a-go-go-related protein 1; Ether-a-go-go-related gene potassium channel 1; Ether-a-go-go related protein 1; Ether-a-go-go related gene potassium channel 1; Eag related protein 1; Eag homolog; ERG-1; ERG
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Representative Drug(s) Sunitinib Drug Info IC50 = 251.19 nM [56]
Co-Target Name 5-HT 2C receptor (HTR2C) Successful Target
UniProt ID 5HT2C_HUMAN
Gene Name HTR2C
Synonyms
Serotonin receptor 2C; HTR1C; 5HT-1C; 5-hydroxytryptamine receptor 2C; 5-hydroxytryptamine receptor 1C; 5-HTR2C; 5-HT2C receptor; 5-HT2C; 5-HT1C; 5-HT-2C; 5-HT-1C
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Representative Drug(s) Drug Info Ki = 417 nM [47]
Co-Target Name Adenosine A2a receptor (ADORA2A) Successful Target
UniProt ID AA2AR_HUMAN
Gene Name ADORA2A
Synonyms
Adenosine receptor A2a; ADORA2; A2a Adenosine receptor; A(2A) adenosine receptor
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Representative Drug(s) CEP-11981 Drug Info Ki = 500 nM [24]
Co-Target Name Fusion protein Bcr-Abl (Bcr-Abl) Successful Target
UniProt ID BCR_HUMAN-ABL1_HUMAN
Gene Name BCR-ABL1
Synonyms
BCR-ABL fusion protein; BCR-ABL
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Representative Drug(s) Sunitinib Drug Info EC50 ~ 1000 nM [61]
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) Axitinib Drug Info IC50 = 0.1 nM Click to Show More [62]
2 Drug Info IC50 = 0.21 nM [34]
3 XL880 Drug Info IC50 = 0.8 nM [34]
4 KRN633 Drug Info IC50 = 1 nM [60]
5 Sunitinib Drug Info IC50 = 1 nM [16]
6 Regorafenib Drug Info IC50 = 1.5 nM [13]
7 CEP-11981 Drug Info IC50 = 3 nM [24]
8 TAK-593 Drug Info IC50 = 3.2 nM [34]
9 Cediranib Drug Info IC50 = 5 nM [34]
10 E-3810 Drug Info IC50 = 7 nM [34]
11 E-3810 Drug Info IC50 = 7 nM [37]
12 Romiplostim Drug Info IC50 = 8 nM [69]
13 MK-2461 Drug Info IC50 = 10 nM [39]
14 Cabozantinib Drug Info IC50 = 12 nM [7]
15 Drug Info IC50 = 18 nM [73]
16 XL999 Drug Info IC50 = 20 nM [16]
17 Lenvatinib Drug Info IC50 = 22 nM [67]
18 Vandetanib Drug Info IC50 = 22 nM [76]
19 Rosiglitazone + metformin Drug Info IC50 = 28 nM [16]
20 VATALANIB Drug Info IC50 = 54 nM [76]
21 Brivanib Drug Info Ki = 60 nM [80]
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) Axitinib Drug Info IC50 = 0.1 nM Click to Show More [62]
2 Drug Info IC50 = 0.24 nM [34]
3 TAK-593 Drug Info IC50 = 1.1 nM [34]
4 XL880 Drug Info IC50 = 2.8 nM [34]
5 Cediranib Drug Info IC50 = 3 nM [34]
6 Drug Info IC50 = 3 nM [66]
7 BAY-57-9352 Drug Info IC50 = 4 nM [34]
8 Lenvatinib Drug Info IC50 = 5.2 nM [34]
9 Cabozantinib Drug Info IC50 = 6 nM [67]
10 Sunitinib Drug Info IC50 = 8.9 nM [66]
11 E-3810 Drug Info IC50 = 10 nM [34]
12 E-3810 Drug Info IC50 = 10 nM [70]
13 Romiplostim Drug Info IC50 = 50 nM [43]
14 MK-2461 Drug Info IC50 = 78 nM [39]
15 KRN633 Drug Info IC50 = 125 nM [60]
16 VATALANIB Drug Info IC50 = 195 nM [34]
17 Vandetanib Drug Info IC50 = 233 nM [43]
Co-Target Name Ephrin type-B receptor 4 (EPHB4) Clinical trial Target
UniProt ID EPHB4_HUMAN
Gene Name EPHB4
Synonyms
Tyrosine-protein kinase TYRO11; TYRO11; MYK1; Hepatoma transmembrane kinase; HTK
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Representative Drug(s) Drug Info IC50 = 0.2 nM [63]
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) Drug Info IC50 = 0.39 nM Click to Show More [64]
2 XL880 Drug Info IC50 = 1.1 nM [7]
3 Regorafenib Drug Info IC50 = 1.5 nM [13]
4 Altiratinib Drug Info IC50 = 8 nM [7]
5 Cabozantinib Drug Info IC50 = 14.3 nM [71]
6 CP-547632 Drug Info IC50 = 18 nM [74]
7 CEP-11981 Drug Info IC50 = 22 nM [24]
8 Vandetanib Drug Info IC50 = 567 nM [43]
Co-Target Name Soluble epoxide hydrolase (EPHX2) Clinical trial Target
UniProt ID HYES_HUMAN
Gene Name EPHX2
Synonyms
Bifunctional epoxide hydrolase 2
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Representative Drug(s) Regorafenib Drug Info IC50 = 0.5 nM Click to Show More [65]
2 Drug Info IC50 = 12 nM [65]
Co-Target Name Proto-oncogene c-RAF (c-RAF) Clinical trial Target
UniProt ID RAF1_HUMAN
Gene Name RAF1
Synonyms
cRaf; Raf-1; RAF proto-oncogene serine/threonine-protein kinase; RAF
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Representative Drug(s) Drug Info IC50 = 1 nM Click to Show More [8]
2 Regorafenib Drug Info IC50 = 1.5 nM [13]
3 PLX-4720 Drug Info Ki = 3.3 nM [21]
4 RAF265 Drug Info IC50 = 19 nM [5]
5 OSI-930 Drug Info IC50 = 41 nM [34]
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) HKI-272 Drug Info IC50 = 3 nM [23]
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) XL880 Drug Info IC50 = 3 nM Click to Show More [7]
2 MK-2461 Drug Info IC50 = 7 nM [39]
3 Cabozantinib Drug Info IC50 = 69 nM [54]
Co-Target Name Protein delta homolog 1 (DLK1) Clinical trial Target
UniProt ID DLK1_HUMAN
Gene Name DLK1
Synonyms
pG2; DLK-1
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Representative Drug(s) Sunitinib Drug Info Ki = 6.3 nM [68]
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) CYC116 Drug Info Ki = 8 nM Click to Show More [59]
2 CEP-11981 Drug Info IC50 = 42 nM [24]
3 MK-2461 Drug Info IC50 = 290 nM [39]
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) CYC116 Drug Info Ki = 9.2 nM Click to Show More [59]
2 Rosiglitazone + metformin Drug Info IC50 = 35 nM [78]
Co-Target Name Macrophage colony-stimulating factor 1 receptor (CSF1R) Clinical trial Target
UniProt ID CSF1R_HUMAN
Gene Name CSF1R
Synonyms
Proto-oncogene c-Fms; M-CSF-R; FMS; CSF-1R; CSF-1-R; CSF-1 receptor; CD115
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Representative Drug(s) TAK-593 Drug Info IC50 = 10 nM Click to Show More [27]
2 Drug Info IC50 = 19 nM [8]
3 Sunitinib Drug Info IC50 = 35 nM [77]
4 CEP-11981 Drug Info IC50 = 78 nM [24]
5 Romiplostim Drug Info IC50 = 84 nM [43]
Co-Target Name Leucine-rich repeat kinase 2 (LRRK2) Clinical trial Target
UniProt ID LRRK2_HUMAN
Gene Name LRRK2
Synonyms
PARK8; Leucine-rich repeat serine/threonine-protein kinase 2; Dardarin
    Click to Show/Hide
Representative Drug(s) Sunitinib Drug Info IC50 = 15 nM [72]
Co-Target Name Serine/threonine-protein kinase Chk2 (RAD53) Clinical trial Target
UniProt ID CHK2_HUMAN
Gene Name CHEK2
Synonyms
hCds1; Hucds1; Checkpoint kinase 2; Cds1 homolog; Cds1; CHK2 checkpoint homolog; CHK2
    Click to Show/Hide
Representative Drug(s) Sunitinib Drug Info IC50 = 16.84 nM Click to Show More [31]
2 CEP-11981 Drug Info IC50 = 140 nM [24]
Co-Target Name Ephrin type-B receptor 2 (EPHB2) Clinical trial Target
UniProt ID EPHB2_HUMAN
Gene Name EPHB2
Synonyms
hEK5; Tyrosine-protein kinase receptor EPH-3; Tyrosine-protein kinase TYRO5; TYRO5; Renal carcinoma antigen NY-REN-47; Receptor protein-tyrosine kinase HEK5; EphB2 receptor tyrosine kinase; EphB2; EPTH3; EPHT3; EPH-like kinase 5; EPH tyrosine kinase 3; ELK-related tyrosine kinase; EK5; Developmentally-regulated Eph-related tyrosine kinase; DRT
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 17.5 nM [18]
Co-Target Name Extracellular signal-regulated kinase 1 (ERK1) Clinical trial Target
UniProt ID MK03_HUMAN
Gene Name MAPK3
Synonyms
PRKM3; P44-MAPK; P44-ERK1; P44 Mitogen-activated protein kinase; Mitogen-activated protein kinase 3; Microtubule-associated protein-2 kinase; Microtubule-associated protein 2 kinase; MAPK 3; MAP kinase isoform p44; MAP kinase 3; Insulin-stimulated MAP2 kinase; ERT2; ERK-1
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 18.1 nM [75]
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
    Click to Show/Hide
Representative Drug(s) MK-2461 Drug Info IC50 = 24 nM [39]
Co-Target Name Stress-activated protein kinase 2a (p38 alpha) Clinical trial Target
UniProt ID MK14_HUMAN
Gene Name MAPK14
Synonyms
SAPK2A; P38 mitogen activatedprotein kinase; P38 Mitogen-activatedprotein kinase alpha; Mitogen-activated protein kinase p38 alpha; Mitogen-activated protein kinase 14; MXI2; MAX-interacting protein 2; MAPK 14; MAP kinase p38alpha; MAP kinase p38 alpha; MAP kinase MXI2; MAP kinase 14; Cytokine suppressive anti-inflammatory drug-binding protein; Cytokine suppressive anti-inflammatory drug binding protein; CSPB1; CSBP2; CSBP1; CSBP; CSAID-binding protein; CSAID binding protein; CRK1
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 37.4 nM [75]
Co-Target Name Adaptor-associated kinase 1 (AAK1) Clinical trial Target
UniProt ID AAK1_HUMAN
Gene Name AAK1
Synonyms
Adaptor-associated kinase 1
    Click to Show/Hide
Representative Drug(s) Sunitinib Drug Info IC50 = 47.4 nM [79]
Co-Target Name Fibroblast growth factor receptor 3 (FGFR3) Clinical trial Target
UniProt ID FGFR3_HUMAN
Gene Name FGFR3
Synonyms
JTK4; FGFR-3; CD333
    Click to Show/Hide
Representative Drug(s) MK-2461 Drug Info IC50 = 50 nM Click to Show More [39]
2 CEP-11981 Drug Info IC50 = 89 nM [24]
3 E-3810 Drug Info IC50 = 237.5 nM [37]
Co-Target Name Aurora kinase C (AURKC) Clinical trial Target
UniProt ID AURKC_HUMAN
Gene Name AURKC
Synonyms
Serine/threonine-protein kinase aurora-C; STK13; Aurora/Ipl1/Eg2 protein 2; Aurora/Ipl1-related kinase 3; Aurora-related kinase 3; Aurora-C; Aurora 3; ARK3; ARK-3; AIRK3; AIK3; AIE2
    Click to Show/Hide
Representative Drug(s) CYC116 Drug Info IC50 = 65 nM Click to Show More [81]
2 Rosiglitazone + metformin Drug Info IC50 = 210 nM [78]
Co-Target Name Checkpoint kinase-1 (CHK1) Clinical trial Target
UniProt ID CHK1_HUMAN
Gene Name CHEK1
Synonyms
Serine/threonine-protein kinase Chk1; Chk1; Cell cycle checkpoint kinase; CHK1 checkpoint homolog
    Click to Show/Hide
Representative Drug(s) Sunitinib Drug Info IC50 = 77.27 nM [31]
Co-Target Name Extracellular signal-regulated kinase 2 (ERK2) Clinical trial Target
UniProt ID MK01_HUMAN
Gene Name MAPK1
Synonyms
PRKM2; PRKM1; P42-MAPK; P42 Mitogen-activated protein kinase; Mitogen-activated protein kinase 2; Mitogen-activated protein kinase 1; MAPK 2; MAPK 1; MAP kinase isoform p42; MAP kinase 2; MAP kinase 1; ERT1; ERK-2
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 109.5 nM [75]
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
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 262 nM [82]
Co-Target Name Cyclin-dependent kinase 2 (CDK2) Clinical trial Target
UniProt ID CDK2_HUMAN
Gene Name CDK2
Synonyms
Sin3 associated polypeptide; SIN3-associated protein; P33 protein kinase; Cell division protein kinase 2; CDKN2
    Click to Show/Hide
Representative Drug(s) CYC116 Drug Info Ki = 390 nM [59]
Co-Target Name Cyclin-dependent kinase 9 (CDK9) Clinical trial Target
UniProt ID CDK9_HUMAN
Gene Name CDK9
Synonyms
Tat-associated kinase complex catalytic subunit; TAK; Similar to cyclin-dependent kinase 9; Serine/threonine-protein kinase PITALRE; Cyclin-dependent protein kinase Cdk9; Cell division protein kinase 9; Cell division cycle 2-like protein kinase 4; CDC2L4; CDC2-related kinase; C-2K
    Click to Show/Hide
Representative Drug(s) CYC116 Drug Info Ki = 480 nM [59]
Co-Target Name Positive transcription elongation factor b (P-TEFb) Clinical trial Target
UniProt ID CDK9_HUMAN-CCNT1_HUMAN
Gene Name CDK9-CCNT1
Synonyms
P-TEFb
    Click to Show/Hide
Representative Drug(s) CYC116 Drug Info Ki = 480 nM [59]
Co-Target Name PAK-4 protein kinase (PAK4) Clinical trial Target
UniProt ID PAK4_HUMAN
Gene Name PAK4
Synonyms
p21-activated kinase 4; Serine/threonine-protein kinase PAK 4; PAK-4; KIAA1142
    Click to Show/Hide
Representative Drug(s) Sunitinib Drug Info Ki = 500 nM [83]
Co-Target Name Ribosomal protein S6 kinase beta-1 (S6K1) Clinical trial Target
UniProt ID KS6B1_HUMAN
Gene Name RPS6KB1
Synonyms
p70-S6K 1; p70 ribosomal S6 kinase alpha; p70 S6KA; p70 S6K-alpha; p70 S6 kinase alpha; Serine/threonine-protein kinase 14A; STK14A; S6K-beta-1; S6K; Ribosomal protein S6 kinase I; P70S6K1; P70-S6K; 70 kDa ribosomal protein S6 kinase 1
    Click to Show/Hide
Representative Drug(s) CYC116 Drug Info Ki = 540 nM [59]
Co-Target Name Casein kinase I alpha (CSNK1A1) Patented-recorded Target
UniProt ID KC1A_HUMAN
Gene Name CSNK1A1
Synonyms
Casein kinase I isoform alpha; CKI-alpha; CK1
    Click to Show/Hide
Representative Drug(s) Sunitinib Drug Info IC50 < 1 nM Click to Show More [10]
2 CEP-11981 Drug Info IC50 = 48 nM [24]
3 Drug Info IC50 = 250 nM [10]
Co-Target Name Discoidin domain-containing receptor 2 (DDR2) Patented-recorded Target
UniProt ID DDR2_HUMAN
Gene Name DDR2
Synonyms
Tyrosine-protein kinase TYRO10; Receptor protein-tyrosine kinase TKT; Neurotrophic tyrosine kinase, receptor-related 3; Discoidin domain-containing receptor tyrosine kinase 2; Discoidin domain receptor 2; DDR2; CD167 antigen-like family member B
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 7 nM Click to Show More [84]
2 CP-547632 Drug Info IC50 = 24 nM [84]
Co-Target Name Ribosomal protein S6 kinase alpha-1 (RSK1) Patented-recorded Target
UniProt ID KS6A1_HUMAN
Gene Name RPS6KA1
Synonyms
p90S6K; p90RSK1; p90-RSK 1; S6K-alpha-1; Ribosomal S6 kinase 1; RSK-1; MAPKAPK1A; MAPKAPK-1a; MAPKAP kinase 1a; MAPK-activated protein kinase 1a; MAP kinase-activated protein kinase 1a; 90 kDa ribosomal protein S6 kinase 1
    Click to Show/Hide
Representative Drug(s) Sunitinib Drug Info IC50 = 131.3 nM [31]
Co-Target Name Ribosomal protein S6 kinase alpha-3 (RSK3) Patented-recorded Target
UniProt ID KS6A3_HUMAN
Gene Name RPS6KA3
Synonyms
pp90RSK2; p90RSK3; p90-RSK 3; S6K-alpha-3; Ribosomal S6 kinase 2; RSK2; RSK-2; MAPKAPK1B; MAPKAPK-1b; MAPKAP kinase 1b; MAPK-activated protein kinase 1b; MAP kinase-activated protein kinase 1b; Insulin-stimulated protein kinase 1; ISPK1; ISPK-1; 90 kDa ribosomal protein S6 kinase 3
    Click to Show/Hide
Representative Drug(s) Sunitinib Drug Info IC50 = 183.9 nM [31]
Co-Target Name Hematopoietic cell kinase (HCK) Patented-recorded Target
UniProt ID HCK_HUMAN
Gene Name HCK
Synonyms
p61Hck; p59Hck; p59-HCK/p60-HCK; Tyrosine-protein kinase HCK; Hemopoietic cell kinase
    Click to Show/Hide
Representative Drug(s) Sunitinib Drug Info IC50 = 190 nM Click to Show More [10]
2 Drug Info IC50 = 530 nM [10]
Co-Target Name Cyclin-dependent kinase 8 (CDK8) Patented-recorded Target
UniProt ID CDK8_HUMAN
Gene Name CDK8
Synonyms
Protein kinase K35; Mediator of RNA polymerase II transcription subunit CDK8; Mediator complex subunit CDK8; Cell division protein kinase 8
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 199 nM [85]
Co-Target Name Polo-like kinase 4 (PLK4) Literature-reported Target
UniProt ID PLK4_HUMAN
Gene Name PLK4
Synonyms
Serine/threonine-protein kinase Sak; Serine/threonine-protein kinase PLK4; Serine/threonine-protein kinase 18; STK18; SAK; PLK-4
    Click to Show/Hide
Representative Drug(s) Axitinib Drug Info Ki = 4.2 nM [86]
Co-Target Name NIMA-related kinase 2 (NEK2) Literature-reported Target
UniProt ID NEK2_HUMAN
Gene Name NEK2
Synonyms
Serine/threonine-protein kinase Nek2; NimA-related protein kinase 2; NimA-like protein kinase 1; Never in mitosis A-related kinase 2; NLK1; NEK2A; HSPK 21
    Click to Show/Hide
Representative Drug(s) HKI-272 Drug Info IC50 = 274 nM [87]
Co-Target Name Serine/threonine-protein kinase A-Raf (ARAF) Co-Target
UniProt ID ARAF_HUMAN
Gene Name ARAF
Synonyms
Proto-oncogene A-Raf; Proto-oncogene A-Raf-1; Proto-oncogene Pks
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 7.1 nM [88]
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) Lenvatinib Drug Info IC50 = 10 nM Click to Show More [14]
2 Cabozantinib Drug Info IC50 = 190 nM [45]
3 Vandetanib Drug Info IC50 = 400 nM [45]
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) Lenvatinib Drug Info IC50 = 10 nM Click to Show More [14]
2 Cabozantinib Drug Info IC50 = 889 nM [92]
Co-Target Name Proto oncogene c Ret-Nuclear receptor coactivator 4 fusion protein (RET-NCOA4) Co-Target
UniProt ID RET_HUMAN-NCOA4_HUMAN
Gene Name RET-NCOA4
Representative Drug(s) Lenvatinib Drug Info IC50 = 10 nM [14]
Co-Target Name Nuclear receptor subfamily 2 group C member 2 (NR2C2) Co-Target
UniProt ID NR2C2_HUMAN
Gene Name NR2C2
Synonyms
Orphan nuclear receptor TAK1; Orphan nuclear receptor TR4; Testicular receptor 4
    Click to Show/Hide
Representative Drug(s) CEP-11981 Drug Info IC50 = 14 nM [24]
Co-Target Name Serine/threonine-protein kinase MST2 (STK3) Co-Target
UniProt ID STK3_HUMAN
Gene Name STK3
Synonyms
Serine/threonine-protein kinase 3; Mammalian STE20-like protein kinase 2; MST-2; STE20-like kinase MST2; Serine/threonine-protein kinase Krs-1
    Click to Show/Hide
Representative Drug(s) CEP-11981 Drug Info IC50 = 21 nM [24]
Co-Target Name Cyclin dependent kinase 8-Cyclin C complex (CDK8-CCNC) Co-Target
UniProt ID CDK8_HUMAN-CCNC_HUMAN
Gene Name CDK8-CCNC
Representative Drug(s) Drug Info IC50 = 32.5 nM [89]
Co-Target Name Carbonic anhydrase VA (CA5A) Co-Target
UniProt ID CAH5A_HUMAN
Gene Name CA5A
Synonyms
Carbonic anhydrase 5A, mitochondrial; Carbonate dehydratase VA; CA-VA
    Click to Show/Hide
Representative Drug(s) Lenvatinib Drug Info Ki = 132.7 nM [90]
Co-Target Name Cyclin-dependent kinase 19 (CDK19) Co-Target
UniProt ID CDK19_HUMAN
Gene Name CDK19
Synonyms
CDC2-related protein kinase 6; Cell division cycle 2-like protein kinase 6; Cell division protein kinase 19; Cyclin-dependent kinase 11; Death-preventing kinase
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 206 nM [85]
Co-Target Name Cyclin dependent kinase 2-G1/S specific cyclin E1 complex (CDK2-CCNE1) Co-Target
UniProt ID CDK2_HUMAN-CCNE1_HUMAN
Gene Name CDK2-CCNE1
Representative Drug(s) CYC116 Drug Info Ki = 390 nM [59]
Co-Target Name Serine/threonine-protein kinase PAK 5 (PAK5) Co-Target
UniProt ID PAK5_HUMAN
Gene Name PAK5
Synonyms
p21-activated kinase 5; PAK-5; p21-activated kinase 7; PAK-7
    Click to Show/Hide
Representative Drug(s) Sunitinib Drug Info Ki = 500 nM [83]
Co-Target Name Serine/threonine-protein kinase PAK 6 (PAK6) Co-Target
UniProt ID PAK6_HUMAN
Gene Name PAK6
Synonyms
PAK-5; p21-activated kinase 6; PAK-6
    Click to Show/Hide
Representative Drug(s) Sunitinib Drug Info Ki = 500 nM [83]
Co-Target Name Pirin (PIR) Co-Target
UniProt ID PIR_HUMAN
Gene Name PIR
Synonyms
Probable quercetin 2,3-dioxygenase PIR; Probable quercetinase
    Click to Show/Hide
Representative Drug(s) PLX-4720 Drug Info IC50 = 670 nM [91]
References  Top
REF 1 Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cyst... Bioorg Med Chem. 2007 Jun 1;15(11):3635-48.
REF 2 Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants including T315I for chronic myeloid leukemia. Eur J Med Chem. 2018 Dec 5;160:61-81.
REF 3 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 4 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 5 Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma. ACS Med Chem Lett. 2015 Aug 3;6(9):961-5.
REF 6 Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design. J Med Chem. 2013 Jul 25;56(14):5757-72.
REF 7 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 8 Design and synthesis of orally bioavailable benzimidazoles as Raf kinase inhibitors. J Med Chem. 2008 Nov 27;51(22):7049-52.
REF 9 Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors. Bioorg Med Chem Lett. 2009 Jan 1;19(1):21-6.
REF 10 Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol. 2008 Nov;4(11):691-9.
REF 11 Combining structure- and property-based optimization to identify selective FLT3-ITD inhibitors with good antitumor efficacy in AML cell inoculated mouse xenograft model. Eur J Med Chem. 2019 Aug 15;176:248-267.
REF 12 Design, synthesis and biological evaluation of 4-aminopyrimidine-5-cabaldehyde oximes as dual inhibitors of c-Met and VEGFR-2. Bioorg Med Chem. 2016 Aug 15;24(16):3353-8.
REF 13 Novel potent substituted 4-amino-2-thiopyrimidines as dual VEGFR-2 and BRAF kinase inhibitors. Eur J Med Chem. 2019 Oct 1;179:707-722.
REF 14 Progress in Discovery of KIF5B-RET Kinase Inhibitors for the Treatment of Non-Small-Cell Lung Cancer. J Med Chem. 2015 May 14;58(9):3672-81.
REF 15 Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives. J Med Chem. 2010 Nov 25;53(22):8140-9.
REF 16 The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2012 Aug 1;22(15):4979-85.
REF 17 Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel... J Med Chem. 2003 Mar 27;46(7):1116-9.
REF 18 Design, synthesis and biological evaluation of deuterated Tivozanib for improving pharmacokinetic properties. Bioorg Med Chem Lett. 2015 Jun 1;25(11):2425-8.
REF 19 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 20 Design, synthesis and biological evaluation of indolin-2-one-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase3 (FLT3). Eur J Med Chem. 2017 Feb 15;127:72-86.
REF 21 Conformation-specific effects of Raf kinase inhibitors. J Med Chem. 2012 Sep 13;55(17):7332-41.
REF 22 Expanding the structural diversity of diarylureas as multi-target tyrosine kinase inhibitors. Bioorg Med Chem. 2016 Feb 15;24(4):750-8.
REF 23 Discovery of novel selective inhibitors for EGFR-T790M/L858R. Bioorg Med Chem Lett. 2012 Feb 1;22(3):1365-70.
REF 24 Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one (CEP-11981): a novel oncology therapeutic agent. J Med Chem. 2012 Jan 26;55(2):903-13.
REF 25 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 26 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 27 Discovery of N-[5-({2-[(cyclopropylcarbonyl)amino]imidazo[1,2-b]pyridazin-6-yl}oxy)-2-methylphenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide (TAK-593), a highly potent VEGFR2 kinase inhibitor. Bioorg Med Chem. 2013 Apr 15;21(8):2333-45.
REF 28 Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT. J Med Chem. 2017 Nov 9;60(21):8801-15.
REF 29 Identification of new potent phthalazine derivatives with VEGFR-2 and EGFR kinase inhibitory activity. Eur J Med Chem. 2016 Nov 10;123:191-201.
REF 30 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 31 Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors. Eur J Med Chem. 2011 Sep;46(9):4311-23.
REF 32 Discovery of dual Axl/VEGF-R2 inhibitors as potential anti-angiogenic and anti-metastatic drugs for cancer chemotherapy. Bioorg Med Chem Lett. 2017 Aug 15;27(16):3766-71.
REF 33 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 34 Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors. J Med Chem. 2012 Dec 27;55(24):10797-822.
REF 35 AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective. J Med Chem. 2016 Apr 28;59(8):3593-608.
REF 36 Design and discovery of 4-anilinoquinazoline-urea derivatives as dual TK inhibitors of EGFR and VEGFR-2. Eur J Med Chem. 2017 Jan 5;125:245-54.
REF 37 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 38 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 39 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 40 Selectivity data: assessment, predictions, concordance, and implications. J Med Chem. 2013 Sep 12;56(17):6991-7002.
REF 41 Metabolic chiral inversion of brivanib and its relevance to safety and pharmacology. Drug Metab Dispos. 2012 Dec;40(12):2374-80.
REF 42 Design, synthesis and in vitro evaluation of 6-amide-2-aryl benzoxazole/benzimidazole derivatives against tumor cells by inhibiting VEGFR-2 kinase. Eur J Med Chem. 2019 Oct 1;179:147-165.
REF 43 Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93.
REF 44 Discovery of biarylaminoquinazolines as novel tubulin polymerization inhibitors. J Med Chem. 2014 Jun 12;57(11):4598-605.
REF 45 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 46 5-Substituted pyrido[2,3-d]pyrimidine, an inhibitor against three receptor tyrosine kinases. Bioorg Med Chem Lett. 2009 Feb 1;19(3):745-50.
REF 47 Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors. J Med Chem. 2012 Jun 28;55(12):5749-59.
REF 48 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 49 Synthesis of hybrid anticancer agents based on kinase and histone deacetylase inhibitors. Medchemcomm. 2014;5:1829-33.
REF 50 Radioiodinated sunitinib as a potential radiotracer for imaging angiogenesis-radiosynthesis and first radiopharmacological evaluation of 5-[125I]Iodo-sunitinib. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2850-5.
REF 51 Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. J Med Chem. 2019 Dec 26;62(24):11135-11150.
REF 52 Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors. Bioorg Med Chem. 2010 Feb 15;18(4):1482-96.
REF 53 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 54 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 55 Vegfrecine, an inhibitor of VEGF receptor tyrosine kinases isolated from the culture broth of Streptomyces sp. J Nat Prod. 2013 Apr 26;76(4):715-9.
REF 56 Prediction of Thorough QT study results using action potential simulations based on ion channel screens. J Pharmacol Toxicol Methods. Nov-Dec 2014;70(3):246-54.
REF 57 Chemical modulation of receptor signaling inhibits regenerative angiogenesis in adult zebrafish. Nat Chem Biol. 2006 May;2(5):265-73.
REF 58 Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching. Bioorg Med Chem Lett. 2003 Sep 15;13(18):2967-71.
REF 59 Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors. J Med Chem. 2010 Jun 10;53(11):4367-78.
REF 60 A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proc Natl Acad Sci U S A. 2007 Dec 18;104(51):20523-8.
REF 61 Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. J Med Chem. 2016 Apr 28;59(8):3886-905.
REF 62 Recent developments in small molecule therapies for renal cell carcinoma. Eur J Med Chem. 2017 Dec 15;142:383-92.
REF 63 Discovery of novel anti-angiogenesis agents. Part 6: Multi-targeted RTK inhibitors. Eur J Med Chem. 2017 Feb 15;127:275-85.
REF 64 Discovery of novel anti-angiogenesis agents. Part 10: Multi-target inhibitors of VEGFR-2, Tie-2 and EphB4 incorporated with 1,2,3-triazol. Eur J Med Chem. 2019 Feb 1;163:1-9.
REF 65 Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3732-7.
REF 66 Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors. Bioorg Med Chem. 2010 Jul 1;18(13):4674-86.
REF 67 Evolution in medicinal chemistry of sorafenib derivatives for hepatocellular carcinoma. Eur J Med Chem. 2019 Oct 1;179:916-935.
REF 68 Dual Leucine Zipper Kinase Inhibitors for the Treatment of Neurodegeneration. J Med Chem. 2018 Sep 27;61(18):8078-87.
REF 69 New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven a... J Med Chem. 2000 Jun 15;43(12):2310-23.
REF 70 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 71 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 72 The development of CNS-active LRRK2 inhibitors using property-directed optimisation. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3690-6.
REF 73 Discovery and evaluation of 3-phenyl-1H-5-pyrazolylamine-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3). Bioorg Med Chem. 2011 Jul 15;19(14):4173-82.
REF 74 Design and synthesis of dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole oximes as potent dual inhibitors of TIE-2 and VEGF-R2 receptor tyrosine kinases. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1916-21.
REF 75 Design and synthesis of potent 1,2,4-trisubstituted imidazolinone derivatives with dual p38alphaMAPK and ERK1/2 inhibitory activity. Eur J Med Chem. 2015 Apr 13;94:397-404.
REF 76 ortho-Substituted azoles as selective and dual inhibitors of VEGF receptors 1 and 2. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1369-75.
REF 77 Selectively nonselective kinase inhibition: striking the right balance. J Med Chem. 2010 Feb 25;53(4):1413-37.
REF 78 The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.
REF 79 Synthesis and Structure-Activity Relationships of 3,5-Disubstituted-pyrrolo[2,3- b]pyridines as Inhibitors of Adaptor-Associated Kinase 1 with Antiviral Activity. J Med Chem. 2019 Jun 27;62(12):5810-5831.
REF 80 Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-... J Med Chem. 2006 Apr 6;49(7):2143-6.
REF 81 Discovery and development of aurora kinase inhibitors as anticancer agents. J Med Chem. 2009 May 14;52(9):2629-51.
REF 82 Design and synthesis of novel 6-hydroxy-4-methoxy-3-methylbenzofuran-7-carboxamide derivatives as potent Mnks inhibitors by fragment-based drug design. Bioorg Med Chem. 2018 Sep 1;26(16):4602-14.
REF 83 Discovery of indolin-2-one derivatives as potent PAK4 inhibitors: Structure-activity relationship analysis, biological evaluation and molecular docking study. Bioorg Med Chem. 2017 Jul 1;25(13):3500-11.
REF 84 Identification of type II and III DDR2 inhibitors. J Med Chem. 2014 May 22;57(10):4252-62.
REF 85 Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?. J Med Chem. 2018 Jun 28;61(12):5073-92.
REF 86 Drug discovery using spirooxindole cores: Success and Challenges [corrected]. Eur J Med Chem. 2015 May 5;95:35-40.
REF 87 Therapeutic melting pot of never in mitosis gene a related kinase 2 (Nek2): a perspective on Nek2 as an oncology target and recent advancements in Nek2 small molecule inhibition. J Med Chem. 2014 Jul 24;57(14):5835-44.
REF 88 Discovery of potent Pan-Raf inhibitors with increased solubility to overcome drug resistance. Eur J Med Chem. 2019 Feb 1;163:243-255.
REF 89 Design and Development of a Series of Potent and Selective Type II Inhibitors of CDK8. ACS Med Chem Lett. 2016 Apr 5;7(6):595-600.
REF 90 A computer-assisted discovery of novel potential anti-obesity compounds as selective carbonic anhydrase VA inhibitors. Eur J Med Chem. 2019 Nov 1;181:111565.
REF 91 Privileged Structures and Polypharmacology within and between Protein Families. ACS Med Chem Lett. 2018 Nov 16;9(12):1199-1204.
REF 92 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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