Co-Target(s) Information
Target General Information | Top | ||||
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Target ID | T92144 | Target Info | |||
Target Name | Angiopoietin 1 receptor (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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Target Type | Clinical trial Target | ||||
Gene Name | TEK | ||||
Biochemical Class | Kinase | ||||
UniProt ID |
Co-Targets of This Target | Top | |||||
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Co-Target Name | NT-3 growth factor receptor (TrkC) | Successful Target | ||||
UniProt ID | NTRK3_HUMAN | |||||
Gene Name | NTRK3 | |||||
Synonyms |
TrkC tyrosine kinase; Trk-C; TRKC; Neurotrophic tyrosine kinase receptor type 3; NT3 growth factor receptor; GP145TrkC; GP145-TrkC
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Representative Drug(s) | Altiratinib | Drug Info | IC50 = 0.83 nM | [1] | ||
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) | Altiratinib | Drug Info | IC50 = 0.85 nM | Click to Show More | [1] | |
2 | CEP-11981 | Drug Info | IC50 = 3 nM | [2] | ||
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) | Altiratinib | Drug Info | IC50 = 2.7 nM | [1] | ||
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) | CEP-11981 | Drug Info | IC50 = 4 nM | Click to Show More | [2] | |
2 | Altiratinib | Drug Info | IC50 = 9.2 nM | [3] | ||
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) | Altiratinib | Drug Info | IC50 = 4.6 nM | Click to Show More | [1] | |
2 | CEP-11981 | Drug Info | IC50 = 5 nM | [2] | ||
Co-Target Name | Proto-oncogene c-Ret (RET) | Successful Target | ||||
UniProt ID | RET_HUMAN | |||||
Gene Name | 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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Representative Drug(s) | CEP-11981 | Drug Info | IC50 = 5 nM | [2] | ||
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) | CEP-11981 | Drug Info | IC50 = 13 nM | [2] | ||
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) | CEP-11981 | Drug Info | IC50 = 37 nM | [2] | ||
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) | CEP-11981 | Drug Info | IC50 = 71 nM | [2] | ||
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) | CEP-11981 | Drug Info | IC50 = 93 nM | [2] | ||
Co-Target Name | ALK tyrosine kinase receptor (ALK) | Successful Target | ||||
UniProt ID | ALK_HUMAN | |||||
Gene Name | ALK | |||||
Synonyms |
CD246; Anaplastic lymphoma kinase
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Representative Drug(s) | CEP-11981 | Drug Info | IC50 = 132 nM | [2] | ||
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) | CEP-11981 | Drug Info | IC50 = 246 nM | [2] | ||
Co-Target Name | Adenosine A2a receptor (ADORA2A) | Successful Target | ||||
UniProt ID | AA2AR_HUMAN | |||||
Gene Name | ADORA2A | |||||
Synonyms |
Adenosine receptor A2a; ADORA2; A2a Adenosine receptor; A(2A) adenosine receptor
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Representative Drug(s) | CEP-11981 | Drug Info | Ki = 500 nM | [2] | ||
Co-Target Name | Yes tyrosine kinase (YES) | Clinical trial Target | ||||
UniProt ID | YES_HUMAN | |||||
Gene Name | YES1 | |||||
Synonyms |
p61-Yes; Yes p59-Fyn; Yes Protooncogene Syn; Tyrosine-protein kinase Yes; Proto-oncogene c-Yes
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Representative Drug(s) | DCC-2036 | Drug Info | IC50 = 1.5 nM | [4] | ||
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) | CEP-11981 | Drug Info | IC50 = 3 nM | [2] | ||
Co-Target Name | Aurora kinase A (AURKA) | Clinical trial Target | ||||
UniProt ID | AURKA_HUMAN | |||||
Gene Name | AURKA | |||||
Synonyms |
hARK1; Serine/threonine-protein kinase aurora-A; Serine/threonine-protein kinase 6; Serine/threonine-protein kinase 15; Serine/threonine kinase 15; STK6; STK15; IAK1; Breast tumor-amplified kinase; BTAK; Aurora/IPL1-related kinase 1; Aurora-related kinase 1; Aurora-A; Aurora 2; AYK1; AURA; ARK1; ARK-1; AIRK1; AIK
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Representative Drug(s) | CEP-11981 | Drug Info | IC50 = 42 nM | [2] | ||
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) | CEP-11981 | Drug Info | IC50 = 78 nM | [2] | ||
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) | CEP-11981 | Drug Info | IC50 = 89 nM | [2] | ||
Co-Target Name | Serine/threonine-protein kinase Chk2 (RAD53) | Clinical trial Target | ||||
UniProt ID | CHK2_HUMAN | |||||
Gene Name | CHEK2 | |||||
Synonyms |
hCds1; Hucds1; Checkpoint kinase 2; Cds1 homolog; Cds1; CHK2 checkpoint homolog; CHK2
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Representative Drug(s) | CEP-11981 | Drug Info | IC50 = 140 nM | [2] | ||
Co-Target Name | Casein kinase I alpha (CSNK1A1) | Patented-recorded Target | ||||
UniProt ID | KC1A_HUMAN | |||||
Gene Name | CSNK1A1 | |||||
Synonyms |
Casein kinase I isoform alpha; CKI-alpha; CK1
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Representative Drug(s) | CEP-11981 | Drug Info | IC50 = 48 nM | [2] | ||
Co-Target Name | Nuclear receptor subfamily 2 group C member 2 (NR2C2) | Co-Target | ||||
UniProt ID | NR2C2_HUMAN | |||||
Gene Name | NR2C2 | |||||
Synonyms |
Orphan nuclear receptor TAK1; Orphan nuclear receptor TR4; Testicular receptor 4
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Representative Drug(s) | CEP-11981 | Drug Info | IC50 = 14 nM | [2] | ||
Co-Target Name | Serine/threonine-protein kinase MST2 (STK3) | Co-Target | ||||
UniProt ID | STK3_HUMAN | |||||
Gene Name | STK3 | |||||
Synonyms |
Serine/threonine-protein kinase 3; Mammalian STE20-like protein kinase 2; MST-2; STE20-like kinase MST2; Serine/threonine-protein kinase Krs-1
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Representative Drug(s) | CEP-11981 | Drug Info | IC50 = 21 nM | [2] |
References | Top | ||||
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REF 1 | The "Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules. J Med Chem. 2016 Oct 13;59(19):8712-56. | ||||
REF 2 | Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one (CEP-11981): a novel oncology therapeutic agent. J Med Chem. 2012 Jan 26;55(2):903-13. | ||||
REF 3 | 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 4 | Identification of potent Yes1 kinase inhibitors using a library screening approach. Bioorg Med Chem Lett. 2013 Aug 1;23(15):4398-403. |
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