Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T92494 Target Info
Target Name Eukaryotic elongation factor 2 kinase (eEF-2K)
Synonyms
eEF-2K; eEF-2 kinase; Calcium/calmodulin-dependent eukaryotic elongation factor 2 kinase
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Target Type Successful Target
Gene Name EEF2K
Biochemical Class Kinase
UniProt ID
EF2K_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) Lapatinib Drug Info IC50 = 1.8 nM [1]
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) Lapatinib Drug Info IC50 = 2.7 nM [2]
Co-Target Name Fyn tyrosine protein kinase (FYN) Successful Target
UniProt ID FYN_HUMAN
Gene Name FYN
Synonyms
Tyrosine-protein kinase Fyn; Src-like kinase; SLK; Proto-oncogene tyrosine-protein kinase Fyn; Proto-oncogene c-Fyn; Proto-oncogene Syn; Fyn p59-Fyn; Fyn Protooncogene Syn
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Representative Drug(s) Lapatinib Drug Info Ki ~ 398.11 nM [3]
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) Lapatinib Drug Info Ki ~ 630.96 nM [3]
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) Lapatinib Drug Info Ki ~ 630.96 nM [3]
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) Lapatinib Drug Info IC50 ~ 1000 nM [4]
Co-Target Name Insulin-like growth factor I receptor (IGF1R) Successful Target
UniProt ID IGF1R_HUMAN
Gene Name IGF1R
Synonyms
Type 1 insulin-like growth factor receptor; Insulin-like growth factor 1 receptor; IGF-IR; IGF-I receptor; IGF-1R; IGF-1 receptor; CD221 antigen; CD221
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Representative Drug(s) Lapatinib Drug Info Ki ~ 1000 nM [3]
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) Lapatinib Drug Info IC50 = 1000 nM [5]
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) Lapatinib Drug Info Ki ~ 398.11 nM [3]
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) Lapatinib Drug Info IC50 ~ 1000 nM [4]
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) Lapatinib Drug Info Ki ~ 794.33 nM [3]
References  Top
REF 1 Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2019 Jun 15;29(12):1435-1439.
REF 2 Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates. Eur J Med Chem. 2014 Nov 24;87:631-42.
REF 3 PubChem BioAssay: 2017 update. Nucleic Acids Res. 2017 Jan 4;45(D1):D955-D963.
REF 4 Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases. J Med Chem. 2012 Mar 22;55(6):2846-57.
REF 5 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.

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