Co-Target(s) Information
| Target General Information | Top | ||||
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| Target ID | T97196 | Target Info | |||
| Target Name | ATM serine/threonine kinase (ATM) | ||||
| Synonyms |
Serine-protein kinase ATM; Ataxia telangiectasia mutated; A-T mutated
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| Target Type | Clinical trial Target | ||||
| Gene Name | ATM | ||||
| 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) | AZD0156 | Drug Info | IC50 = 200 nM | [2] | ||
| Co-Target Name | PI3-kinase delta (PIK3CD) | Successful Target | ||||
| UniProt ID | PK3CD_HUMAN | |||||
| Gene Name | PIK3CD | |||||
| Synonyms |
PtdIns-3-kinase subunit p110-delta; PtdIns-3-kinase subunit delta; Phosphoinositide 3-kinase delta; Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit, delta isoform; Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform; Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit delta; PI3Kdelta; PI3K-delta; PI3-kinase subunit delta; PI3-kinase p110 subunit delta; P110delta
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| Representative Drug(s) | AZD0156 | Drug Info | IC50 = 270 nM | [2] | ||
| Co-Target Name | PI3-kinase alpha (PIK3CA) | Successful Target | ||||
| UniProt ID | PK3CA_HUMAN | |||||
| Gene Name | PIK3CA | |||||
| Synonyms |
p110alpha; Serine/threonine protein kinase PIK3CA; PtdIns3kinase subunit p110alpha; PtdIns3kinase subunit alpha; PtdIns-3-kinase subunit p110-alpha; PtdIns-3-kinase subunit alpha; Phosphoinositide3kinase catalytic alpha polypeptide; Phosphoinositide-3-kinase catalytic alpha polypeptide; Phosphatidylinositol 4,5bisphosphate 3kinase catalytic subunit alpha isoform; Phosphatidylinositol 4,5bisphosphate 3kinase 110 kDa catalytic subunit alpha; Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform; Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit alpha; PI3kinase subunit alpha; PI3Kalpha; PI3K-alpha; PI3-kinase subunit alpha
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| Representative Drug(s) | AZD0156 | Drug Info | IC50 = 320 nM | [2] | ||
| Co-Target Name | Serine/threonine-protein kinase ATR (FRP1) | Clinical trial Target | ||||
| UniProt ID | ATR_HUMAN | |||||
| Gene Name | ATR | |||||
| Synonyms |
FRAP-related protein 1; Ataxia telangiectasia and Rad3-related protein
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| Representative Drug(s) | VX-970 | Drug Info | Ki = 0.165 nM | [1] | ||
| 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 | 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 | DNA-dependent protein kinase catalytic (PRKDC) | Clinical trial Target | ||||
| UniProt ID | PRKDC_HUMAN | |||||
| Gene Name | PRKDC | |||||
| Synonyms |
p460; HYRC1; HYRC; DNPK1; DNA-dependent protein kinase catalytic subunit; DNA-PKcs; DNA-PK catalytic subunit
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| Representative Drug(s) | AZD0156 | Drug Info | IC50 = 140 nM | [2] | ||
| 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 | The Identification of Potent, Selective, and Orally Available Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase: The Discovery of AZD0156 (8-{6-[3-(Dimethylamino)propoxy]pyridin-3-yl}-3-methyl-1-(tetrahydro-2 H-pyran-4-yl)-1,3-dihydro-2 H-imidazo[4,5- c]quinolin-2-one). J Med Chem. 2018 May 10;61(9):3823-41. | ||||
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