Co-Target(s) Information
Target General Information | Top | ||||
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Target ID | T77764 | Target Info | |||
Target Name | Aurora B messenger RNA (AURKB mRNA) | ||||
Synonyms |
Serine/threonine-protein kinase aurora-B (mRNA); Serine/threonine-protein kinase 5 (mRNA); Serine/threonine-protein kinase 12 (mRNA); Serine/threonine protein kinase 12 (mRNA); STK5 (mRNA); STK12 (mRNA); Aurora/IPL1-related kinase 2 (mRNA); Aurora-related kinase 2 (mRNA); Aurora-B (mRNA); Aurora-2 kinase (mRNA); Aurora-2 (mRNA); Aurora- and Ipl1-like midbody-associated protein 1 (mRNA); Aurora 1 (mRNA); ARK2 (mRNA); ARK-2 (mRNA); AIRK2 (mRNA); AIM1 (mRNA); AIM-1 (mRNA); AIK2 (mRNA)
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Target Type | Clinical trial Target | ||||
Gene Name | AURKB | ||||
Biochemical Class | mRNA target | ||||
UniProt ID |
Co-Targets of This Target | Top | |||||
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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 | [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) | PHA-739358 | Drug Info | IC50 = 30 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) | PHA-739358 | Drug Info | IC50 = 31 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) | PHA-739358 | Drug Info | IC50 = 47 nM | [2] | ||
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) | PHA-739358 | Drug Info | IC50 = 155 nM | [2] | ||
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 | [2] | ||
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) | PHA-739358 | Drug Info | IC50 = 432 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) | PHA-739358 | Drug Info | IC50 = 669 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) | PHA-739358 | Drug Info | Ki = 2.5 nM | [2] | ||
Co-Target Name | Aurora kinase C (AURKC) | Clinical trial Target | ||||
UniProt ID | AURKC_HUMAN | |||||
Gene Name | 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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Representative Drug(s) | PHA-739358 | Drug Info | IC50 = 61 nM | [2] | ||
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) | PHA-739358 | Drug Info | IC50 = 161 nM | [2] | ||
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 | [2] | ||
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 | [2] |
References | Top | ||||
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REF 1 | 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 2 | 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. |
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