Co-Target(s) Information
Target General Information | Top | ||||
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Target ID | T60631 | Target Info | |||
Target Name | Proto-oncogene c-Ret (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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Target Type | Successful Target | ||||
Gene Name | RET | ||||
Biochemical Class | Kinase | ||||
UniProt ID |
Co-Targets of This Target | Top | |||||
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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) | Ponatinib | Drug Info | EC50 = 0.05 nM | [1] | ||
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) | Ponatinib | Drug Info | IC50 = 0.3 nM | Click to Show More | [2] | |
2 | MGCD516 | Drug Info | IC50 = 8 nM | [6] | ||
3 | tamatinib | Drug Info | EC50 = 10 nM | [13] | ||
4 | Regorafenib | Drug Info | IC50 = 82 nM | [23] | ||
5 | Romiplostim | Drug Info | IC50 = 160 nM | [25] | ||
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) | Ponatinib | Drug Info | IC50 = 0.32 nM | Click to Show More | [3] | |
2 | Vandetanib | Drug Info | IC50 = 86 nM | [19] | ||
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) | Ponatinib | Drug Info | IC50 = 0.7 nM | Click to Show More | [4] | |
2 | Regorafenib | Drug Info | IC50 = 1.5 nM | [7] | ||
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) | Ponatinib | Drug Info | IC50 = 1.2 nM | Click to Show More | [5] | |
2 | Regorafenib | Drug Info | IC50 = 1.5 nM | [7] | ||
3 | Romiplostim | Drug Info | IC50 = 68 nM | [21] | ||
4 | Vandetanib | Drug Info | IC50 = 477 nM | [19] | ||
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) | Ponatinib | Drug Info | IC50 = 1.3 nM | [5] | ||
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) | MGCD516 | Drug Info | IC50 = 1.5 nM | [6] | ||
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) | Regorafenib | Drug Info | IC50 = 1.5 nM | Click to Show More | [7] | |
2 | CEP-32496 | Drug Info | IC50 = 82 nM | [22] | ||
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) | Ponatinib | Drug Info | IC50 = 1.5 nM | Click to Show More | [8] | |
2 | Regorafenib | Drug Info | IC50 = 4.2 nM | [10] | ||
3 | MGCD516 | Drug Info | IC50 = 5 nM | [6] | ||
4 | Vandetanib | Drug Info | IC50 = 9 nM | [12] | ||
5 | Romiplostim | Drug Info | IC50 = 12.9 nM | [16] | ||
6 | tamatinib | Drug Info | EC50 = 36 nM | [13] | ||
7 | GSK3179106 | Drug Info | IC50 = 109 nM | [24] | ||
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) | Ponatinib | Drug Info | IC50 = 1.7 nM | Click to Show More | [9] | |
2 | MGCD516 | Drug Info | IC50 = 6 nM | [6] | ||
3 | Regorafenib | Drug Info | IC50 = 6.1 nM | [9] | ||
4 | Romiplostim | Drug Info | IC50 = 35 nM | [19] | ||
5 | Vandetanib | Drug Info | IC50 = 343 nM | [19] | ||
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) | Ponatinib | Drug Info | IC50 = 2.5 nM | Click to Show More | [5] | |
2 | Vandetanib | Drug Info | IC50 = 44 nM | [20] | ||
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) | Ponatinib | Drug Info | IC50 = 2.6 nM | Click to Show More | [5] | |
2 | Romiplostim | Drug Info | IC50 = 200 nM | [27] | ||
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) | MGCD516 | Drug Info | IC50 = 5 nM | [6] | ||
Co-Target Name | Janus kinase 2 (JAK-2) | Successful Target | ||||
UniProt ID | JAK2_HUMAN | |||||
Gene Name | JAK2 | |||||
Synonyms |
Tyrosine-protein kinase JAK2
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Representative Drug(s) | tamatinib | Drug Info | IC50 = 6 nM | [11] | ||
Co-Target Name | BDNF/NT-3 growth factors receptor (TrkB) | Successful Target | ||||
UniProt ID | NTRK2_HUMAN | |||||
Gene Name | NTRK2 | |||||
Synonyms |
Tropomyosin-related kinase B; TrkB tyrosine kinase; Trk-B; TRKB; Neurotrophic tyrosine kinase receptor type 2; GP145-TrkB
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Representative Drug(s) | MGCD516 | Drug Info | IC50 = 9 nM | [6] | ||
Co-Target Name | Tyrosine-protein kinase SYK (SYK) | Successful Target | ||||
UniProt ID | KSYK_HUMAN | |||||
Gene Name | SYK | |||||
Synonyms |
p72-Syk; Spleen tyrosine kinase
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Representative Drug(s) | tamatinib | Drug Info | EC50 = 10 nM | [14] | ||
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) | Vandetanib | Drug Info | IC50 = 11 nM | Click to Show More | [15] | |
2 | Ponatinib | Drug Info | IC50 ~ 1000 nM | [5] | ||
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) | MGCD516 | Drug Info | IC50 = 20 nM | [17] | ||
Co-Target Name | Vascular endothelial growth factor receptor (VEGFR) | Successful Target | ||||
UniProt ID | VGFR1_HUMAN; VGFR2_HUMAN; VGFR3_HUMAN | |||||
Gene Name | NO-GeName | |||||
Representative Drug(s) | Vandetanib | Drug Info | IC50 = 25 nM | [18] | ||
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) | CEP-32496 | Drug Info | Ki = 187.8 nM | [26] | ||
Co-Target Name | Tyrosine-protein kinase Lyn (JTK8) | Clinical trial Target | ||||
UniProt ID | LYN_HUMAN | |||||
Gene Name | LYN | |||||
Synonyms |
p56Lyn; p53Lyn; V-yes-1 Yamaguchi sarcoma viral related oncogene homolog; Lck/Yes-related novel protein tyrosine kinase
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Representative Drug(s) | Ponatinib | Drug Info | IC50 = 0.24 nM | Click to Show More | [8] | |
2 | tamatinib | Drug Info | IC50 = 732 nM | [11] | ||
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 | [28] | ||
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) | Regorafenib | Drug Info | IC50 = 1.5 nM | Click to Show More | [7] | |
2 | Romiplostim | Drug Info | IC50 = 8 nM | [29] | ||
3 | Ponatinib | Drug Info | IC50 = 20.9 nM | [5] | ||
4 | Vandetanib | Drug Info | IC50 = 22 nM | [31] | ||
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) | Regorafenib | Drug Info | IC50 = 1.5 nM | [7] | ||
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) | Regorafenib | Drug Info | IC50 = 1.5 nM | Click to Show More | [7] | |
2 | Vandetanib | Drug Info | IC50 = 567 nM | [19] | ||
Co-Target Name | Fibroblast growth factor receptor 4 (FGFR4) | Clinical trial Target | ||||
UniProt ID | FGFR4_HUMAN | |||||
Gene Name | FGFR4 | |||||
Synonyms |
TKF; JTK2; FGFR-4; CD334
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Representative Drug(s) | Ponatinib | Drug Info | IC50 = 7.1 nM | [5] | ||
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) | Ponatinib | Drug Info | IC50 = 9.4 nM | [5] | ||
Co-Target Name | Stress-activated protein kinase JNK1 (JNK1) | Clinical trial Target | ||||
UniProt ID | MK08_HUMAN | |||||
Gene Name | MAPK8 | |||||
Synonyms |
Stress-activated protein kinase 1c; SAPK1c; PRKM8; Mitogen-activated protein kinase 8; MAPK 8; MAP kinase 8; JNK-46; C-Jun N-terminal kinase 1
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Representative Drug(s) | tamatinib | Drug Info | EC50 = 10 nM | [14] | ||
Co-Target Name | Receptor-interacting protein 1 (RIPK1) | Clinical trial Target | ||||
UniProt ID | RIPK1_HUMAN | |||||
Gene Name | RIPK1 | |||||
Synonyms |
Receptor-interacting serine/threonine-protein kinase 1; RIP1; RIP-1; RIP; Cell death protein RIP
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Representative Drug(s) | Ponatinib | Drug Info | IC50 = 12 nM | [30] | ||
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) | Romiplostim | Drug Info | IC50 = 50 nM | Click to Show More | [19] | |
2 | Vandetanib | Drug Info | IC50 = 233 nM | [19] | ||
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) | Romiplostim | Drug Info | IC50 = 84 nM | [19] | ||
Co-Target Name | Stress-activated protein kinase JNK2 (JNK2) | Patented-recorded Target | ||||
UniProt ID | MK09_HUMAN | |||||
Gene Name | MAPK9 | |||||
Synonyms |
Stress-activated protein kinase 1a; SAPK1a; PRKM9; Mitogen-activated protein kinase 9; Mitogen-activated protein kinase 8-interacting protein 2; MAPK 9; MAP kinase 9; Jun-N-terminal kinase 2; JNK-interacting protein 2; JNK-55; JNK MAP kinase scaffold protein 2; JIP-2; Islet-brain-2; IB-2; C-jun-amino-terminal kinase interacting protein 2; C-Jun N-terminal kinase 2
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Representative Drug(s) | tamatinib | Drug Info | EC50 = 10 nM | [14] | ||
Co-Target Name | Tyrosine-protein kinase ZAP-70 (ZAP-70) | Patented-recorded Target | ||||
UniProt ID | ZAP70_HUMAN | |||||
Gene Name | ZAP70 | |||||
Synonyms |
Syk-related tyrosine kinase; SRK; 70 kDa zeta-chain associated protein
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Representative Drug(s) | tamatinib | Drug Info | IC50 = 42 nM | [11] | ||
Co-Target Name | Serine/threonine-protein kinase RIPK2 (RIPK2) | Co-Target | ||||
UniProt ID | RIPK2_HUMAN | |||||
Gene Name | RIPK2 | |||||
Synonyms |
Receptor-interacting serine/threonine-protein kinase 2; CARD-containing interleukin-1 beta-converting enzyme-associated kinase; CARD-containing IL-1 beta ICE-kinase; RIP-like-interacting CLARP kinase; Receptor-interacting protein 2; RIP-2; Tyrosine-protein kinase RIPK2
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Representative Drug(s) | Ponatinib | Drug Info | IC50 = 1 nM | [30] | ||
Co-Target Name | Receptor-interacting serine/threonine-protein kinase 3 (RIPK3) | Co-Target | ||||
UniProt ID | RIPK3_HUMAN | |||||
Gene Name | RIPK3 | |||||
Synonyms |
RIP-like protein kinase 3; Receptor-interacting protein 3; RIP-3
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Representative Drug(s) | Ponatinib | Drug Info | IC50 = 1.6 nM | [30] | ||
Co-Target Name | Mitogen-activated protein kinase 1 (MAPK1) | Co-Target | ||||
UniProt ID | MK01_HUMAN | |||||
Gene Name | MAPK1 | |||||
Synonyms |
MAP kinase 1; MAPK 1; ERT1; Extracellular signal-regulated kinase 2; ERK-2; MAP kinase isoform p42; p42-MAPK; Mitogen-activated protein kinase 2; MAP kinase 2; MAPK 2
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Representative Drug(s) | tamatinib | Drug Info | EC50 = 10 nM | [14] | ||
Co-Target Name | Mitogen-activated protein kinase 3 (MAPK3) | Co-Target | ||||
UniProt ID | MK03_HUMAN | |||||
Gene Name | MAPK3 | |||||
Synonyms |
MAP kinase 3; MAPK 3; ERT2; Extracellular signal-regulated kinase 1; ERK-1; Insulin-stimulated MAP2 kinase; MAP kinase isoform p44; p44-MAPK; Microtubule-associated protein 2 kinase; p44-ERK1
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Representative Drug(s) | tamatinib | Drug Info | EC50 = 10 nM | [14] | ||
Co-Target Name | Tyrosine-protein kinase ABL2 (ABL2) | Co-Target | ||||
UniProt ID | ABL2_HUMAN | |||||
Gene Name | ABL2 | |||||
Synonyms |
Abelson murine leukemia viral oncogene homolog 2; Abelson tyrosine-protein kinase 2; Abelson-related gene protein; Tyrosine-protein kinase ARG
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Representative Drug(s) | Ponatinib | Drug Info | IC50 = 40 nM | [32] |
References | Top | ||||
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REF 1 | 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 2 | Inhibitors of Stat5 protein signalling. Medchemcomm. 2012;3:22-7. | ||||
REF 3 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. J Med Chem. 2013 Feb 14;56(3):879-94. | ||||
REF 4 | Novel benzothiazinones (BTOs) as allosteric modulator or substrate competitive inhibitor of glycogen synthase kinase 3beta (GSK-3beta) with cellular activity of promoting glucose uptake. Bioorg Med Chem Lett. 2014 Dec 15;24(24):5639-43. | ||||
REF 5 | Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors. Eur J Med Chem. 2017 Jan 27;126:122-32. | ||||
REF 6 | Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application. J Med Chem. 2019 Feb 28;62(4):1731-1760. | ||||
REF 7 | 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 8 | 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 9 | Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT. J Med Chem. 2017 Nov 9;60(21):8801-15. | ||||
REF 10 | Design, synthesis and docking study of novel picolinamide derivatives as anticancer agents and VEGFR-2 inhibitors. Eur J Med Chem. 2019 Apr 15;168:315-329. | ||||
REF 11 | Syk inhibitors with high potency in presence of blood. Bioorg Med Chem Lett. 2014 May 15;24(10):2278-82. | ||||
REF 12 | Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors. J Med Chem. 2005 Mar 10;48(5):1610-9. | ||||
REF 13 | Discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase. J Med Chem. 2014 May 8;57(9):3856-73. | ||||
REF 14 | Discovery and development of spleen tyrosine kinase (SYK) inhibitors. J Med Chem. 2012 Apr 26;55(8):3614-43. | ||||
REF 15 | 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 16 | The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents. Bioorg Med Chem. 2015 May 15;23(10):2408-23. | ||||
REF 17 | 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 18 | Novel 4-anilinoquinazolines with C-7 basic side chains: design and structure activity relationship of a series of potent, orally active, VEGF receptor tyrosine kinase inhibitors. J Med Chem. 2002 Mar 14;45(6):1300-12. | ||||
REF 19 | Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93. | ||||
REF 20 | Discovery of biarylaminoquinazolines as novel tubulin polymerization inhibitors. J Med Chem. 2014 Jun 12;57(11):4598-605. | ||||
REF 21 | Synthesis of hybrid anticancer agents based on kinase and histone deacetylase inhibitors. Medchemcomm. 2014;5:1829-33. | ||||
REF 22 | Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E. J Med Chem. 2012 Feb 9;55(3):1082-105. | ||||
REF 23 | 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 24 | Discovery of a First-in-Class Gut-Restricted RET Kinase Inhibitor as a Clinical Candidate for the Treatment of IBS. ACS Med Chem Lett. 2018 May 24;9(7):623-8. | ||||
REF 25 | 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 26 | 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 27 | 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. | ||||
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