Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T75243 Target Info
Target Name Serine/threonine-protein kinase mTOR (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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Target Type Successful Target
Gene Name MTOR
Biochemical Class Kinase
UniProt ID
MTOR_HUMAN
Co-Targets of This Target  Top
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) PF-05212384 Drug Info IC50 = 0.4 nM Click to Show More [1]
2 PF-04691502 Drug Info Ki = 0.57 nM [2]
3 BEZ235 Drug Info IC50 = 4 nM [1]
4 BGT226 Drug Info IC50 = 4 nM [3]
5 GDC-0980/RG7422 Drug Info IC50 = 4.8 nM [4]
6 VS-5584 Drug Info IC50 = 16 nM [8]
7 PQR309 Drug Info Ki = 17 nM [9]
8 INK128 Drug Info Ki = 28 nM [11]
9 SAR245409 Drug Info IC50 = 39 nM [7]
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) BEZ235 Drug Info IC50 = 5 nM Click to Show More [5]
2 PF-05212384 Drug Info IC50 = 6 nM [6]
3 GDC-0980/RG7422 Drug Info IC50 = 6.7 nM [4]
4 VS-5584 Drug Info IC50 = 37 nM [8]
5 SAR245409 Drug Info IC50 = 43 nM [7]
6 PQR309 Drug Info IC50 = 451 nM [12]
Co-Target Name PI3-kinase gamma (PIK3CG) Successful Target
UniProt ID PK3CG_HUMAN
Gene Name PIK3CG
Synonyms
p120-PI3K; p110gamma; Serine/threonine protein kinase PIK3CG; PtdIns-3-kinase subunit p110-gamma; PtdIns-3-kinase subunit gamma; PtdIns-3-kinase p110; Phosphoinositol-3 kinase; Phosphoinositide-3-kinase catalytic gamma polypeptide; Phosphoinositide 3-Kinase gamma; Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit, gamma isoform; Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform; Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit gamma; PI3Kgamma; PI3K-gamma; PI3K; PI3-kinase subunit gamma; PI3-kinase p110 subunit gamma
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Representative Drug(s) BEZ235 Drug Info IC50 = 5 nM Click to Show More [3]
2 PF-05212384 Drug Info IC50 = 5.4 nM [6]
3 SAR245409 Drug Info IC50 = 9 nM [7]
4 GDC-0980/RG7422 Drug Info IC50 = 14 nM [4]
5 VS-5584 Drug Info IC50 = 25 nM [8]
6 BGT226 Drug Info IC50 = 38 nM [3]
7 PQR309 Drug Info IC50 = 708 nM [12]
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 [10]
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 [10]
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 [10]
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 [10]
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) GDC-0980/RG7422 Drug Info IC50 = 134 nM Click to Show More [4]
2 VX-970 Drug Info Ki = 190 nM [10]
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 [10]
Co-Target Name Transformation-sensitive protein p120 (TRPA1) Successful Target
UniProt ID TRPA1_HUMAN
Gene Name TRPA1
Synonyms
TRPA1; Ankyrin-like with transmembrane domains protein 1; ANKTM1
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Representative Drug(s) Salirasib Drug Info EC50 = 800 nM [13]
Co-Target Name Janus kinase 3 (JAK-3) Successful Target
UniProt ID JAK3_HUMAN
Gene Name JAK3
Synonyms
Tyrosine-protein kinase JAK3; Leukocyte janus kinase; L-JAK
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Representative Drug(s) BEZ235 Drug Info IC50 = 1000 nM [14]
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 [10]
Co-Target Name PI3-kinase beta (PIK3CB) Clinical trial Target
UniProt ID PK3CB_HUMAN
Gene Name PIK3CB
Synonyms
p110beta; PtdIns3kinase subunit p110beta; PtdIns3kinase subunit beta; PtdIns-3-kinase subunit p110-beta; PtdIns-3-kinase subunit beta; Phosphatidylinositol 4,5bisphosphate 3kinase catalytic subunitbeta isoform; Phosphatidylinositol 4,5bisphosphate 3kinase 110 kDa catalyticsubunit beta; Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform; Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit beta; PIK3C1; PI3kinase subunit beta; PI3Kbeta; PI3K-beta; PI3-kinase subunit beta
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Representative Drug(s) BEZ235 Drug Info IC50 = 6 nM Click to Show More [3]
2 PF-05212384 Drug Info IC50 = 6 nM [6]
3 GDC-0980/RG7422 Drug Info IC50 = 27 nM [4]
4 BGT226 Drug Info IC50 = 63 nM [3]
5 VS-5584 Drug Info IC50 = 68 nM [8]
6 SAR245409 Drug Info IC50 = 113 nM [7]
7 PQR309 Drug Info IC50 = 661 nM [12]
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) BEZ235 Drug Info IC50 = 7 nM Click to Show More [15]
2 VX-970 Drug Info Ki = 44 nM [10]
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 Click to Show More [10]
2 CC-223 Drug Info IC50 = 651 nM [17]
Co-Target Name RAC-alpha serine/threonine-protein kinase (AKT1) Clinical trial Target
UniProt ID AKT1_HUMAN
Gene Name AKT1
Synonyms
RAC-PK-alpha; RAC; Proto-oncogene c-Akt; Protein kinase B alpha; PKB alpha
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Representative Drug(s) PF-04691502 Drug Info IC50 = 13 nM [16]
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 Click to Show More [10]
2 GDC-0980/RG7422 Drug Info IC50 = 232 nM [4]
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) CC-223 Drug Info IC50 = 28 nM [17]
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 [10]
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 [10]
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 [10]
Co-Target Name Tyrosine-protein kinase Fgr (FGR) Literature-reported Target
UniProt ID FGR_HUMAN
Gene Name FGR
Synonyms
p58c-Fgr; p58-Fgr; p55-Fgr; SRC2; Proto-oncogene c-Fgr; Gardner-Rasheed feline sarcoma viral (v-fgr) oncogene homolog
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Representative Drug(s) GDC-0980/RG7422 Drug Info IC50 = 697 nM [4]
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) BEZ235 Drug Info IC50 = 4 nM Click to Show More [18]
2 PQR309 Drug Info Ki = 17 nM [20]
3 VX-970 Drug Info Ki = 140 nM [10]
Co-Target Name PI3K p110 beta/p85 alpha (PIK3CB/PIK3R1) Co-Target
UniProt ID PK3CB_HUMAN-P85A_HUMAN
Gene Name PIK3CB-PIK3R1
Representative Drug(s) BEZ235 Drug Info IC50 = 16.23 nM [19]
Co-Target Name PI3K p110 delta/p85 alpha (PIK3CD/PIK3R1) Co-Target
UniProt ID PK3CD_HUMAN-P85A_HUMAN
Gene Name PIK3CD-PIK3R1
Representative Drug(s) BEZ235 Drug Info IC50 = 22 nM [3]
Co-Target Name Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit alpha (PIK3C2A) Co-Target
UniProt ID P3C2A_HUMAN
Gene Name PIK3C2A
Synonyms
PI3K-C2-alpha; PtdIns-3-kinase C2 subunit alpha; Phosphoinositide 3-kinase-C2-alpha
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Representative Drug(s) BEZ235 Drug Info IC50 = 34 nM [21]
Co-Target Name Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta (PIK3C2B) Co-Target
UniProt ID P3C2B_HUMAN
Gene Name PIK3C2B
Synonyms
PI3K-C2-beta; PtdIns-3-kinase C2 subunit beta; C2-PI3K; Phosphoinositide 3-kinase-C2-beta
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Representative Drug(s) BEZ235 Drug Info IC50 = 44 nM Click to Show More [21]
2 GDC-0980/RG7422 Drug Info IC50 = 794 nM [4]
Co-Target Name PI3K-gamma/PI3K regulatory subunit 5 (PIK3CG-PIK3R5) Co-Target
UniProt ID PK3CG_HUMAN-PI3R5_HUMAN
Gene Name PIK3CG-PIK3R5
Representative Drug(s) BEZ235 Drug Info IC50 = 72 nM [22]
Co-Target Name Phosphatidylinositol 3-kinase catalytic subunit type 3 (PIK3C3) Co-Target
UniProt ID PK3C3_HUMAN
Gene Name PIK3C3
Synonyms
PI3-kinase type 3; PI3K type 3; PtdIns-3-kinase type 3; Phosphatidylinositol 3-kinase p100 subunit; Phosphoinositide-3-kinase class 3; hVps34
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Representative Drug(s) BEZ235 Drug Info IC50 = 450 nM [21]
References  Top
REF 1 Small molecules targeting phosphoinositide 3-kinases. Medchemcomm. 2012;3:1337-55.
REF 2 Highly Selective and Potent Thiophenes as PI3K Inhibitors with Oral Antitumor Activity. ACS Med Chem Lett. 2011 Sep 19;2(11):809-13.
REF 3 Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3Kdelta. Bioorg Med Chem. 2018 Aug 15;26(15):4537-43.
REF 4 Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer. J Med Chem. 2011 Nov 10;54(21):7579-87.
REF 5 Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kdelta selective inhibitors. Bioorg Med Chem Lett. 2019 Jun 1;29(11):1313-1319.
REF 6 Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor. J Med Chem. 2010 Mar 25;53(6):2636-45.
REF 7 Phosphatidylinositol 3 kinase (PI3K) inhibitors as new weapon to combat cancer. Eur J Med Chem. 2019 Dec 1;183:111718.
REF 8 Phosphatidylinositol 3-Kinase (PI3K) and phosphatidylinositol 3-kinase-related kinase (PIKK) inhibitors: importance of the morpholine ring. J Med Chem. 2015 Jan 8;58(1):41-71.
REF 9 (S)-4-(Difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine (PQR530), a Potent, Orally Bioavailable, and Brain-Penetrable Dual Inhibitor of Class I PI3K and mTOR Kinase. J Med Chem. 2019 Jul 11;62(13):6241-6261.
REF 10 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 11 Impact of Minor Structural Modifications on Properties of a Series of mTOR Inhibitors. ACS Med Chem Lett. 2019 Oct 4;10(11):1561-1567.
REF 12 5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology. J Med Chem. 2017 Sep 14;60(17):7524-7538.
REF 13 N-Cinnamoylanthranilates as human TRPA1 modulators: Structure-activity relationships and channel binding sites. Eur J Med Chem. 2019 May 15;170:141-156.
REF 14 Selectivity data: assessment, predictions, concordance, and implications. J Med Chem. 2013 Sep 12;56(17):6991-7002.
REF 15 Optimization of a Novel Series of Ataxia-Telangiectasia Mutated Kinase Inhibitors as Potential Radiosensitizing Agents. J Med Chem. 2016 Jan 28;59(2):559-77.
REF 16 Structure-based design, SAR analysis and antitumor activity of PI3K/mTOR dual inhibitors from 4-methylpyridopyrimidinone series. Bioorg Med Chem Lett. 2013 May 1;23(9):2787-92.
REF 17 Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. J Med Chem. 2015 Jul 9;58(13):5323-33.
REF 18 6-Aryl substituted 4-(4-cyanomethyl) phenylamino quinazolines as a new class of isoform-selective PI3K-alpha inhibitors. Eur J Med Chem. 2016 Oct 21;122:731-743.
REF 19 Discovery of a series of N-(5-(quinolin-6-yl)pyridin-3-yl)benzenesulfonamides as PI3K/mTOR dual inhibitors. Eur J Med Chem. 2017 Feb 15;127:509-520.
REF 20 A Conformational Restriction Strategy for the Identification of a Highly Selective Pyrimido-pyrrolo-oxazine mTOR Inhibitor. J Med Chem. 2019 Sep 26;62(18):8609-8630.
REF 21 Class II Phosphoinositide 3-Kinases as Novel Drug Targets. J Med Chem. 2017 Jan 12;60(1):47-65.
REF 22 Synthesis and anticancer effects evaluation of 1-alkyl-3-(6-(2-methoxy-3-sulfonylaminopyridin-5-yl)benzo[d]thiazol-2-yl)urea as anticancer agents with low toxicity. Bioorg Med Chem. 2015 Oct 1;23(19):6477-85.

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