Co-Target(s) Information
Target General Information | Top | ||||
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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 |
Co-Targets of This Target | Top | |||||
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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) | 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) | 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) | 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) | 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) | 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 | ||||
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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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