Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T97592 Target Info
Target Name Aurora kinase C (AURKC)
Synonyms
Serine/threonine-protein kinase aurora-C; STK13; Aurora/Ipl1/Eg2 protein 2; Aurora/Ipl1-related kinase 3; Aurora-related kinase 3; Aurora-C; Aurora 3; ARK3; ARK-3; AIRK3; AIK3; AIE2
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Target Type Clinical trial Target
Gene Name AURKC
Biochemical Class Kinase
UniProt ID
AURKC_HUMAN
Co-Targets of This Target  Top
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) ABT-348 Drug Info Ki = 0.7943 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) ABT-348 Drug Info IC50 = 2 nM Click to Show More [2]
2 PHA-739358 Drug Info IC50 = 432 nM [5]
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) ABT-348 Drug Info IC50 = 3 nM Click to Show More [3]
2 PHA-739358 Drug Info IC50 = 155 nM [5]
Co-Target Name Platelet-derived growth factor receptor beta (PDGFRB) Successful Target
UniProt ID PGFRB_HUMAN
Gene Name PDGFRB
Synonyms
Platelet-derived growth factor receptor 1; PDGFR1; PDGFR-beta; PDGFR-1; PDGFR; PDGF-R-beta; CD140b antigen; CD140b; CD140 antigen-like family member B; Beta-type platelet-derived growth factor receptor; Beta-PDGFR; Beta platelet-derived growth factor receptor
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Representative Drug(s) ABT-348 Drug Info IC50 = 3 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) PHA-739358 Drug Info IC50 = 5 nM Click to Show More [4]
2 ABT-348 Drug Info IC50 = 12 nM [3]
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) ABT-348 Drug Info IC50 = 7 nM Click to Show More [3]
2 PHA-739358 Drug Info IC50 = 31 nM [5]
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) PHA-739358 Drug Info IC50 = 30 nM [5]
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) PHA-739358 Drug Info IC50 = 47 nM Click to Show More [5]
2 GSK1070916 Drug Info IC50 = 76 nM [6]
3 ABT-348 Drug Info IC50 = 188 nM [3]
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) ABT-348 Drug Info IC50 = 110 nM [3]
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) ABT-348 Drug Info IC50 = 363 nM [3]
Co-Target Name Tyrosine-protein kinase Kit (KIT) Successful Target
UniProt ID KIT_HUMAN
Gene Name KIT
Synonyms
v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog; p145 c-kit; Proto-oncogene tyrosine-protein kinase Kit; Proto-oncogene c-Kit; Piebald trait protein; PBT; Mast/stem cell growth factor receptor Kit; CD117 antigen; CD117; C-kit
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Representative Drug(s) PHA-739358 Drug Info IC50 = 407 nM [5]
Co-Target Name Rho-associated protein kinase 1 (ROCK1) Successful Target
UniProt ID ROCK1_HUMAN
Gene Name ROCK1
Synonyms
Rok; Rho-associated, coiled-coil containing protein kinase 1; Rho-associated kinase 1; Rho kinase; ROCK1; ROCK; P160ROCK; P160(rock); P160 ROCK-1; Let-502 kinase
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Representative Drug(s) ABT-348 Drug Info IC50 = 456 nM [3]
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) ABT-348 Drug Info IC50 = 539 nM [3]
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) PHA-739358 Drug Info IC50 = 669 nM [5]
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) ABT-348 Drug Info IC50 = 1000 nM [3]
Co-Target Name Aurora kinase B (AURKB) Clinical trial Target
UniProt ID AURKB_HUMAN
Gene Name AURKB
Synonyms
Serine/threonine-protein kinase aurora-B; Serine/threonine-protein kinase 5; Serine/threonine-protein kinase 12; Serine/threonine protein kinase 12; STK5; STK12; Aurora/IPL1-related kinase 2; Aurora-related kinase 2; Aurora-B; Aurora-2 kinase; Aurora-2; Aurora- and Ipl1-like midbody-associated protein 1; Aurora 1; ARK2; ARK-2; AIRK2; AIM1; AIM-1; AIK2
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Representative Drug(s) GSK1070916 Drug Info Ki = 0.38 nM Click to Show More [6]
2 ABT-348 Drug Info IC50 = 2 nM [3]
3 AMG 900 Drug Info IC50 = 4 nM [7]
4 PHA-739358 Drug Info IC50 = 79 nM [8]
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) PHA-739358 Drug Info Ki = 2.5 nM Click to Show More [5]
2 AMG 900 Drug Info IC50 = 5 nM [7]
3 ABT-348 Drug Info IC50 = 12 nM [3]
4 GSK1070916 Drug Info Ki = 490 nM [6]
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) ABT-348 Drug Info Ki = 3.162 nM [1]
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) ABT-348 Drug Info IC50 = 32 nM Click to Show More [3]
2 GSK1070916 Drug Info IC50 = 42 nM [6]
Co-Target Name Angiopoietin 1 receptor (TEK) Clinical trial Target
UniProt ID TIE2_HUMAN
Gene Name 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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Representative Drug(s) GSK1070916 Drug Info IC50 = 59 nM [6]
Co-Target Name Vascular endothelial growth factor receptor 3 (FLT-4) Clinical trial Target
UniProt ID VGFR3_HUMAN
Gene Name FLT4
Synonyms
VEGFR3; VEGFR-3; VEGF-3 receptor; Tyrosine-protein kinase receptor FLT4; Fms-like tyrosine kinase 4
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Representative Drug(s) GSK1070916 Drug Info IC50 = 74 nM Click to Show More [6]
2 PHA-739358 Drug Info IC50 = 161 nM [5]
Co-Target Name Cyclin-dependent kinase 2 (CDK2) Clinical trial Target
UniProt ID CDK2_HUMAN
Gene Name CDK2
Synonyms
Sin3 associated polypeptide; SIN3-associated protein; P33 protein kinase; Cell division protein kinase 2; CDKN2
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Representative Drug(s) PHA-739358 Drug Info IC50 = 462 nM [5]
Co-Target Name Salt-inducible kinase 1 (SIK1) Literature-reported Target
UniProt ID SIK1_HUMAN
Gene Name SIK1
Synonyms
Serine/threonine-protein kinase SNF1LK; Serine/threonine-protein kinase SNF1-like kinase 1; Serine/threonine-protein kinase SIK1; SNF1LK; SIK-1; SIK
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Representative Drug(s) GSK1070916 Drug Info IC50 = 70 nM [6]
Co-Target Name STE20-related serine/threonine-protein kinase (SLK) Literature-reported Target
UniProt ID SLK_HUMAN
Gene Name SLK
Synonyms
hSLK; STE20-related kinase; STE20-like kinase
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Representative Drug(s) PHA-739358 Drug Info IC50 = 621 nM [5]
Co-Target Name Aurora kinase B-Inner centromere protein complex (AURKB-INCENP) Co-Target
UniProt ID AURKB_HUMAN-INCE_HUMAN
Gene Name AURKB-INCENP
Representative Drug(s) GSK1070916 Drug Info Ki = 0.38 nM [7]
Co-Target Name Aurora kinase A-Targeting protein for Xklp2 complex (AURKA-TPX2) Co-Target
UniProt ID AURKA_HUMAN-TPX2_HUMAN
Gene Name AURKA-TPX2
Representative Drug(s) GSK1070916 Drug Info Ki = 490 nM [7]
References  Top
REF 1 Targeted kinase selectivity from kinase profiling data. ACS Med Chem Lett. 2012 Mar 14;3(5):383-6.
REF 2 Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases. Bioorg Med Chem Lett. 2012 Jul 15;22(14):4750-5.
REF 3 Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families. Bioorg Med Chem Lett. 2012 May 1;22(9):3208-12.
REF 4 A type-II kinase inhibitor capable of inhibiting the T315I "gatekeeper" mutant of Bcr-Abl. J Med Chem. 2010 Aug 12;53(15):5439-48.
REF 5 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: identification of a potent Aurora kinase inhibitor with a favorable antitumor kinase inhibition profile. J Med Chem. 2006 Nov 30;49(24):7247-51.
REF 6 Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase. J Med Chem. 2010 May 27;53(10):3973-4001.
REF 7 A comprehensive review on Aurora kinase: Small molecule inhibitors and clinical trial studies. Eur J Med Chem. 2017 Nov 10;140:1-19.
REF 8 Discovery and development of aurora kinase inhibitors as anticancer agents. J Med Chem. 2009 May 14;52(9):2629-51.

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