Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T92057 Target Info
Target Name Erbb4 tyrosine kinase receptor (Erbb-4)
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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Target Type Successful Target
Gene Name ERBB4
Biochemical Class Kinase
UniProt ID
ERBB4_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) CI-1033 Drug Info Ki = 0.11 nM Click to Show More [1]
2 Dacomitinib Drug Info IC50 = 1.8 nM [2]
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) CI-1033 Drug Info IC50 = 5 nM Click to Show More [3]
2 Dacomitinib Drug Info IC50 = 45.7 nM [4]
Co-Target Name LCK tyrosine protein kinase (LCK) Successful Target
UniProt ID LCK_HUMAN
Gene Name LCK
Synonyms
p56-LCK; Tyrosine-protein kinase Lck; T cell-specific protein-tyrosine kinase; Proto-oncogene tyrosine-protein kinase LCK; Proto-oncogene Lck; Protein YT16; Lymphocyte cell-specific protein-tyrosine kinase; Leukocyte C-terminal Src kinase; LSK; LCK p59-Fyn; LCK Protooncogene Syn
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Representative Drug(s) Dacomitinib Drug Info IC50 = 94 nM [5]
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) Dacomitinib Drug Info IC50 = 110 nM [5]
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) CI-1033 Drug Info IC50 = 185 nM [6]
Co-Target Name Ubiquitin-protein ligase E3 Mdm2 (MDM2) Clinical trial Target
UniProt ID MDM2_HUMAN
Gene Name MDM2
Synonyms
RING-type E3 ubiquitin transferase Mdm2; P53-binding protein Mdm2; Oncoprotein Mdm2; MDM2 protein; Hdm2; E3 ubiquitin-protein ligase Mdm2; Double minute 2 protein
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Representative Drug(s) RG7388 Drug Info IC50 = 6 nM [7]
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) CI-1033 Drug Info IC50 = 29 nM [6]
Co-Target Name Tyrosine-protein kinase BMX (BMX) Patented-recorded Target
UniProt ID BMX_HUMAN
Gene Name BMX
Synonyms
NTK38; Epithelial and endothelial tyrosine kinase; ETK; Cytoplasmic tyrosine-protein kinase BMX; Bone marrow tyrosine kinase gene in chromosome X protein
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Representative Drug(s) CI-1033 Drug Info IC50 = 62 nM [6]
Co-Target Name Tumour suppressor p53-E3 ubiquitinprotein ligase Mdm2 (TP53-MDM2) Co-Target
UniProt ID P53_HUMAN-MDM2_HUMAN
Gene Name TP53-MDM2
Representative Drug(s) RG7388 Drug Info IC50 = 9 nM [8]
References  Top
REF 1 Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants. J Med Chem. 2016 Mar 10;59(5):2005-24.
REF 2 Structure-activity study of quinazoline derivatives leading to the discovery of potent EGFR-T790M inhibitors. Eur J Med Chem. 2015 Sep 18;102:445-63.
REF 3 Irreversible protein kinase inhibitors: balancing the benefits and risks. J Med Chem. 2012 Jul 26;55(14):6243-62.
REF 4 Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry. Eur J Med Chem. 2019 May 15;170:55-72.
REF 5 Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family. J Med Chem. 2016 Sep 8;59(17):8103-24.
REF 6 Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase. Bioorg Med Chem Lett. 2008 Nov 15;18(22):5916-9.
REF 7 Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development. J Med Chem. 2013 Jul 25;56(14):5979-83.
REF 8 Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy. Bioorg Med Chem. 2014 Aug 1;22(15):4001-9.

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