Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T14597 Target Info
Target Name Erbb2 tyrosine kinase receptor (HER2)
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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Target Type Successful Target
Gene Name ERBB2
Biochemical Class Kinase
UniProt ID
ERBB2_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) HM-78136B Drug Info IC50 = 0.078 nM Click to Show More [1]
2 HKI-272 Drug Info IC50 = 0.08 nM [2]
3 CI-1033 Drug Info Ki = 0.11 nM [3]
4 BIBW 2992 Drug Info IC50 = 0.19 nM [4]
5 TAK-285 Drug Info IC50 = 1 nM [5]
6 Dacomitinib Drug Info IC50 = 1.8 nM [6]
7 Lapatinib Drug Info IC50 = 1.8 nM [7]
8 CUDC-101 Drug Info IC50 = 2.4 nM [8]
9 AZD8931 Drug Info IC50 = 4 nM [9]
10 Varlitinib Drug Info IC50 = 7 nM [11]
11 BMS-599626 Drug Info IC50 = 32 nM [16]
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) Varlitinib Drug Info IC50 = 4 nM Click to Show More [10]
2 CI-1033 Drug Info IC50 = 10 nM [13]
3 Dacomitinib Drug Info IC50 = 74 nM [17]
4 BMS-599626 Drug Info IC50 = 190 nM [19]
5 TAK-285 Drug Info IC50 = 260 nM [20]
6 Lapatinib Drug Info IC50 ~ 1000 nM [21]
Co-Target Name Histone deacetylase (HDAC) Successful Target
UniProt ID HDAC1_HUMAN; HDAC2_HUMAN; HDAC3_HUMAN; HDAC4_HUMAN; HDAC5_HUMAN; HDAC6_HUMAN; HDAC7_HUMAN; HDAC8_HUMAN; HDAC9_HUMAN; HDA10_HUMAN; HDA11_HUMAN
Gene Name NO-GeName
Synonyms
Human histone deacetylase
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Representative Drug(s) CUDC-101 Drug Info IC50 = 4.4 nM [8]
Co-Target Name Histone deacetylase 1 (HDAC1) Successful Target
UniProt ID HDAC1_HUMAN
Gene Name HDAC1
Synonyms
RPD3L1; HD1
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Representative Drug(s) CUDC-101 Drug Info IC50 = 4.5 nM [8]
Co-Target Name Inosine-5'-monophosphate dehydrogenase (IMPDH) Successful Target
UniProt ID IMDH1_HUMAN; IMDH2_HUMAN
Gene Name NO-GeName
Representative Drug(s) Merimepodib Drug Info IC50 = 7 nM [12]
Co-Target Name Inosine-5'-monophosphate dehydrogenase 2 (IMPDH2) Successful Target
UniProt ID IMDH2_HUMAN
Gene Name IMPDH2
Synonyms
IMPDH-II; IMPDH 2; IMPD2; IMPD 2; IMP dehydrogenase 2
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Representative Drug(s) Merimepodib Drug Info IC50 = 10 nM [14]
Co-Target Name Farnesoid X-activated receptor (FXR) Successful Target
UniProt ID NR1H4_HUMAN
Gene Name NR1H4
Synonyms
Retinoid X receptor-interacting protein 14; RXR-interacting protein 14; RIP14; Nuclear receptor subfamily 1 group H member 4; HRR1; Farnesol receptor HRR-1; FXR; Bile acid receptor; BAR
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Representative Drug(s) Bevacizumab + Trastuzumab Drug Info IC50 = 18.3 nM [15]
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 [17]
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 [17]
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 [18]
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) CUDC-101 Drug Info IC50 = 849 nM Click to Show More [8]
2 HKI-272 Drug Info IC50 = 858.2 nM [2]
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 [22]
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) AZD8931 Drug Info IC50 = 4 nM [23]
Co-Target Name Histone deacetylase 6 (HDAC6) Clinical trial Target
UniProt ID HDAC6_HUMAN
Gene Name HDAC6
Synonyms
KIAA0901; JM21; HD6
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Representative Drug(s) CUDC-101 Drug Info IC50 = 5.1 nM [8]
Co-Target Name Histone deacetylase 3 (HDAC3) Clinical trial Target
UniProt ID HDAC3_HUMAN
Gene Name HDAC3
Synonyms
SMAP45; RPD32; RPD3-2; HD3
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Representative Drug(s) CUDC-101 Drug Info IC50 = 9.1 nM [8]
Co-Target Name Histone deacetylase 2 (HDAC2) Clinical trial Target
UniProt ID HDAC2_HUMAN
Gene Name HDAC2
Synonyms
HD2
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Representative Drug(s) CUDC-101 Drug Info IC50 = 12.6 nM [8]
Co-Target Name Histone deacetylase 4 (HDAC4) Clinical trial Target
UniProt ID HDAC4_HUMAN
Gene Name HDAC4
Synonyms
KIAA0288; HD4
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Representative Drug(s) CUDC-101 Drug Info IC50 = 13.2 nM [8]
Co-Target Name G-protein coupled bile acid receptor 1 (GPBAR1) Clinical trial Target
UniProt ID GPBAR_HUMAN
Gene Name GPBAR1
Synonyms
hGPCR19; hBG37; TGR5; Membrane-type receptor for bile acids; M-BAR; G-protein coupled receptor GPCR19; BG37
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Representative Drug(s) Bevacizumab + Trastuzumab Drug Info EC50 = 580 nM [24]
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) CUDC-101 Drug Info IC50 = 840 nM [8]
Co-Target Name Histone deacetylase 5 (HDAC5) Patented-recorded Target
UniProt ID HDAC5_HUMAN
Gene Name HDAC5
Synonyms
KIAA0600; HD5; Antigen NY-CO-9
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Representative Drug(s) CUDC-101 Drug Info IC50 = 11.4 nM [8]
Co-Target Name Histone deacetylase 10 (HDAC10) Patented-recorded Target
UniProt ID HDA10_HUMAN
Gene Name HDAC10
Synonyms
Polyamine deacetylase HDAC10; HD10
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Representative Drug(s) CUDC-101 Drug Info IC50 = 26.1 nM [8]
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 [18]
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 [18]
Co-Target Name Histone deacetylase 9 (HDAC9) Patented-recorded Target
UniProt ID HDAC9_HUMAN
Gene Name HDAC9
Synonyms
MITR; MEF2-interacting transcription repressor MITR; KIAA0744; Histone deacetylase-related protein; Histone deacetylase 7B; HDRP; HDAC7B; HDAC7; HD9; HD7b
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Representative Drug(s) CUDC-101 Drug Info IC50 = 67.2 nM [8]
Co-Target Name Histone deacetylase 8 (HDAC8) Patented-recorded Target
UniProt ID HDAC8_HUMAN
Gene Name HDAC8
Synonyms
Histone deacetylase-8; HDACL1; HD8; CDA07
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Representative Drug(s) CUDC-101 Drug Info IC50 = 79.8 nM [8]
Co-Target Name Histone deacetylase 7 (HDAC7) Patented-recorded Target
UniProt ID HDAC7_HUMAN
Gene Name HDAC7
Synonyms
Histone deacetylase 7A; HDAC7A; HD7a; HD7
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Representative Drug(s) CUDC-101 Drug Info IC50 = 373 nM [8]
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
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Representative Drug(s) HKI-272 Drug Info IC50 = 274 nM [25]
Co-Target Name HLA class I histocompatibility antigen A-3 (HLA-A) Co-Target
UniProt ID HLAA_HUMAN
Gene Name HLA-A
Synonyms
HLA class I histocompatibility antigen, A alpha chain; Human leukocyte antigen A; HLA-A
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Representative Drug(s) Nelipepimut S Drug Info IC50 = 33.27 nM [26]
References  Top
REF 1 Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. J Med Chem. 2019 Nov 27;62(22):10108-10123.
REF 2 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 3 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 4 Design, synthesis and biological evaluation of novel 4-anilinoquinazolines with C-6 urea-linked side chains as inhibitors of the epidermal growth factor receptor. Bioorg Med Chem. 2013 Dec 15;21(24):7988-98.
REF 5 Targeting EGFR/HER2 tyrosine kinases with a new potent series of 6-substituted 4-anilinoquinazoline hybrids: Design, synthesis, kinase assay, cell-based assay, and molecular docking. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5147-54.
REF 6 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 7 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 8 Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer. J Med Chem. 2010 Mar 11;53(5):2000-9.
REF 9 Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma. J Med Chem. 2019 May 9;62(9):4772-4778.
REF 10 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 11 Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy. Bioorg Med Chem. 2017 Jan 1;25(1):27-37.
REF 12 New dermatological agents for the treatment of psoriasis. J Med Chem. 2001 Feb 1;44(3):281-97.
REF 13 Irreversible protein kinase inhibitors: balancing the benefits and risks. J Med Chem. 2012 Jul 26;55(14):6243-62.
REF 14 Discovery of N-[2-[2-[[3-methoxy-4-(5-oxazolyl)phenyl]amino]-5-oxazolyl]phenyl]-N-methyl-4- morpholineacetamide as a novel and potent inhibitor of inosine monophosphate dehydrogenase with excellent in vivo activity. J Med Chem. 2002 May 23;45(11):2127-30.
REF 15 Identification of trisubstituted-pyrazol carboxamide analogs as novel and potent antagonists of farnesoid X receptor. Bioorg Med Chem. 2014 Jun 1;22(11):2919-38.
REF 16 Novel pyrrolo[2,1-f][1,2,4]triazin-4-amines: Dual inhibitors of EGFR and HER2 protein tyrosine kinases. Bioorg Med Chem Lett. 2011 Jan 15;21(2):781-5.
REF 17 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 18 Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase. Bioorg Med Chem Lett. 2008 Nov 15;18(22):5916-9.
REF 19 Discovery and preclinical evaluation of [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic acid, (3S)-3-morpholinylmethyl ester (BMS-599626), a selective and orally efficacious inhibitor of human epidermal growth factor receptor 1 and 2 kinases. J Med Chem. 2009 Nov 12;52(21):6527-30.
REF 20 Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold. J Med Chem. 2011 Dec 8;54(23):8030-50.
REF 21 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 22 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 23 Discovery of AZD8931, an Equipotent, Reversible Inhibitor of Signaling by EGFR, HER2, and HER3 Receptors. ACS Med Chem Lett. 2013 May 31;4(8):742-6.
REF 24 Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies. J Med Chem. 2008 Mar 27;51(6):1831-41.
REF 25 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 26 Toward the quantitative prediction of T-cell epitopes: coMFA and coMSIA studies of peptides with affinity for the class I MHC molecule HLA-A*0201. J Med Chem. 2001 Oct 25;44(22):3572-81.

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