Co-Target(s) Information
Target General Information | Top | ||||
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Target ID | T97155 | Target Info | |||
Target Name | Serine/threonine-protein kinase ATR (FRP1) | ||||
Synonyms |
FRAP-related protein 1; Ataxia telangiectasia and Rad3-related protein
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Target Type | Clinical trial Target | ||||
Gene Name | ATR | ||||
Biochemical Class | Kinase | ||||
UniProt ID |
Co-Targets of This Target | Top | |||||
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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) | VX-970 | Drug Info | Ki = 18 nM | [1] | ||
Co-Target Name | Glycogen synthase kinase-3 alpha (GSK-3A) | Successful Target | ||||
UniProt ID | GSK3A_HUMAN | |||||
Gene Name | GSK3A | |||||
Synonyms |
Serine/threonineprotein kinase GSK3A; Serine/threonine-protein kinase GSK3A; Glycogen synthase kinase3 alpha; Glycogen synthase kinase 3; GSK3 alpha; GSK-3 alpha; GSK-3
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Representative Drug(s) | VX-970 | Drug Info | Ki = 33 nM | [1] | ||
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) | VX-970 | Drug Info | Ki = 39 nM | [1] | ||
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) | VX-970 | Drug Info | Ki = 59 nM | [1] | ||
Co-Target Name | Janus kinase 2 (JAK-2) | Successful Target | ||||
UniProt ID | JAK2_HUMAN | |||||
Gene Name | JAK2 | |||||
Synonyms |
Tyrosine-protein kinase JAK2
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Representative Drug(s) | VX-970 | Drug Info | Ki = 150 nM | [1] | ||
Co-Target Name | Tyrosine-protein kinase SYK (SYK) | Successful Target | ||||
UniProt ID | KSYK_HUMAN | |||||
Gene Name | SYK | |||||
Synonyms |
p72-Syk; Spleen tyrosine kinase
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Representative Drug(s) | VX-970 | Drug Info | Ki = 190 nM | [1] | ||
Co-Target Name | Serine/threonine-protein kinase mTOR (mTOR) | Successful Target | ||||
UniProt ID | MTOR_HUMAN | |||||
Gene Name | MTOR | |||||
Synonyms |
Target of rapamycin; TOR kinase; Rapamycin target protein 1; Rapamycin target protein; Rapamycin and FKBP12 target 1; RAPT1; RAFT1; Mechanistic target of rapamycin; Mammalian target of rapamycin; FRAP2; FRAP1; FRAP; FKBP12-rapamycin complex-associated protein; FKBP-rapamycin associated protein; FK506-binding protein 12-rapamycin complex-associated protein 1
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Representative Drug(s) | AZD6738 | Drug Info | IC50 = 370 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) | VX-970 | Drug Info | Ki = 8 nM | [1] | ||
Co-Target Name | Mixed lineage kinase 1 (MAP3K9) | Clinical trial Target | ||||
UniProt ID | M3K9_HUMAN | |||||
Gene Name | MAP3K9 | |||||
Synonyms |
PRKE1; Mitogen-activated protein kinase kinase kinase 9; MLK1
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Representative Drug(s) | VX-970 | Drug Info | Ki = 15 nM | [1] | ||
Co-Target Name | Tyrosine-protein kinase Mer (MERTK) | Clinical trial Target | ||||
UniProt ID | MERTK_HUMAN | |||||
Gene Name | MERTK | |||||
Synonyms |
Receptor tyrosine kinase MerTK; Proto-oncogene c-Mer
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Representative Drug(s) | VX-970 | Drug Info | Ki = 30 nM | [1] | ||
Co-Target Name | ATM serine/threonine kinase (ATM) | Clinical trial Target | ||||
UniProt ID | ATM_HUMAN | |||||
Gene Name | ATM | |||||
Synonyms |
Serine-protein kinase ATM; Ataxia telangiectasia mutated; A-T mutated
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Representative Drug(s) | VX-970 | Drug Info | Ki = 44 nM | [1] | ||
Co-Target Name | Glycogen synthase kinase-3 beta (GSK-3B) | Clinical trial Target | ||||
UniProt ID | GSK3B_HUMAN | |||||
Gene Name | GSK3B | |||||
Synonyms |
Serine/threonine-protein kinase GSK3B; GSK-3 beta
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Representative Drug(s) | VX-970 | Drug Info | Ki = 140 nM | [1] | ||
Co-Target Name | Dual-specificity tyrosine-phosphorylation regulated kinase 2 (DYRK2) | Patented-recorded Target | ||||
UniProt ID | DYRK2_HUMAN | |||||
Gene Name | DYRK2 | |||||
Synonyms |
Dual specificity tyrosine-phosphorylation-regulated kinase 2
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Representative Drug(s) | VX-970 | Drug Info | Ki = 26 nM | [1] | ||
Co-Target Name | PI3K p110 alpha/p85 alpha (PIK3CA/PIK3R1) | Co-Target | ||||
UniProt ID | PK3CA_HUMAN-P85A_HUMAN | |||||
Gene Name | PIK3CA-PIK3R1 | |||||
Representative Drug(s) | VX-970 | Drug Info | Ki = 140 nM | [1] |
References | Top | ||||
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REF 1 | Rational Design of 5-(4-(Isopropylsulfonyl)phenyl)-3-(3-(4-((methylamino)methyl)phenyl)isoxazol-5-yl)pyrazin-2-amine (VX-970, M6620): Optimization of Intra- and Intermolecular Polar Interactions of a New Ataxia Telangiectasia Mutated and Rad3-Related (ATR) Kinase Inhibitor. J Med Chem. 2019 Jun 13;62(11):5547-5561. | ||||
REF 2 | Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. J Med Chem. 2018 Nov 21;61(22):9889-9907. |
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