mechanistic target of rapamycin kinase | FRAP subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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mechanistic target of rapamycin kinase

Target not currently curated in GtoImmuPdb

Target id: 2109

Nomenclature: mechanistic target of rapamycin kinase

Abbreviated Name: mTOR

Family: FRAP subfamily

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 2549 1p36 MTOR mechanistic target of rapamycin kinase
Mouse - 2549 4 E1 Mtor mechanistic target of rapamycin kinase
Rat - 2549 5 q36 Mtor mechanistic target of rapamycin kinase
Previous and Unofficial Names
FK506 binding protein 12-rapamycin associated protein 2 | FKBP12-rapamycin complex-associated protein 1 | FKBP-rapamycin associated protein | FKBP-rapamycin-associated protein FRAP | RAFT1 | rapamycin and FKBP12 target 1 | rapamycin associated protein FRAP2 | rapamycin target protein 1 | RAPT1 | mammalian target of rapamycin | FK506 binding protein 12-rapamycin associated protein 1 | mechanistic target of rapamycin (serine/threonine kinase) | mechanistic target of rapamycin
Database Links
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Co-crystal structure of the PPIase domain of FKBP51, Rapamycin and the FRB fragment of mTOR
Resolution:  1.45Å
Species:  Human
References:  24
Image of receptor 3D structure from RCSB PDB
Description:  The solution structure of the rapamycin-binding domain of mTOR (FRB)
Resolution:  0.0Å
Species:  Human
References:  36
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of PI3K-gamma in complex with benzothiazole 82.
PDB Id:  3QK0
Ligand:  compound 82 [PMID: 21332118]
Resolution:  2.85Å
Species:  Human
References:  5
Enzyme Reaction
EC Number:

Download all structure-activity data for this target as a CSV file

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Parameter Reference
PQR620 Hs Inhibition 9.6 pKd 27
pKd 9.6 (Kd 2.7x10-10 M) [27]
Description: Binding affinity constant.
neolymphostin A Hs Inhibition 8.0 pKd 4
pKd 8.0 (Kd 1x10-8 M) [4]
Description: Determined using an active-site dependent competition binding assay.
bimiralisib Hs Inhibition 7.9 pKd
pKd 7.9 (Kd 1.2x10-8 M)
wortmannin Hs Inhibition 5.0 pKd 4
pKd 5.0 (Kd 9.2x10-6 M) [4]
sapanisertib Hs Inhibition 8.9 pKi 14
pKi 8.9 (Ki 1.4x10-9 M) [14]
compound 82 [PMID: 21332118] Hs Inhibition 8.7 pKi 5
pKi 8.7 (Ki 2x10-9 M) [5]
PQR620 Hs Inhibition 8.0 pKi 27
pKi 8.0 (Ki 1.08x10-8 M) [27]
Description: In vitro inhibition constant.
PF-04691502 Hs Inhibition 7.8 pKi 19
pKi 7.8 (Ki 1.6x10-8 M) [19]
apitolisib Hs Inhibition 7.8 pKi 33
pKi 7.8 (Ki 1.7x10-8 M) [33]
omipalisib Hs Inhibition 6.5 – 6.7 pKi 16
pKi 6.5 – 6.7 (Ki 3x10-7 – 1.8x10-7 M) [16]
berzosertib Hs Inhibition <6.0 pKi 7
pKi <6.0 (Ki >1x10-6 M) [7]
eCF309 Hs Inhibition 8.1 pEC50 8
pEC50 8.1 (EC50 9x10-9 M) [8]
Description: In a cell viability assay.
ridaforolimus Hs Inhibition 9.7 pIC50 30
pIC50 9.7 (IC50 2x10-10 M) [30]
Description: Measured as dose-dependent inhibition of phosphorylation of ribosomal protein S6, a signaling protein downstream of mTOR
torin 1 Hs Inhibition 9.5 pIC50 20
pIC50 9.5 (IC50 2.9x10-10 M) [20]
Description: Assayed using mTORC1 complex
AZD8055 Hs Inhibition 9.1 pIC50 26
pIC50 9.1 (IC50 8x10-10 M) [26]
sapanisertib Hs Inhibition 9.0 pIC50 14
pIC50 9.0 (IC50 1x10-9 M) [14]
gedatolisib Hs Inhibition 8.8 pIC50 35
pIC50 8.8 (IC50 1.6x10-9 M) [35]
everolimus Hs Inhibition 8.7 pIC50 32
pIC50 8.7 (IC50 2x10-9 M) [32]
vistusertib Hs Inhibition 8.6 pIC50 26
pIC50 8.6 (IC50 2.8x10-9 M) [26]
Description: Assay using FLAG-tagged human mTOR(1362-2549)
torin 2 Hs Inhibition 8.6 pIC50 21
pIC50 8.6 (IC50 2.81x10-9 M) [21]
panulisib Hs Inhibition 8.4 pIC50 15
pIC50 8.4 (IC50 4.4x10-9 M) [15]
Description: Using a radiometric protein kinase (33PanQinase activity) assay.
WYE-354 Hs Inhibition 8.3 pIC50 38
pIC50 8.3 (IC50 5x10-9 M) [38]
Description: DELFIA assay measuring His6-S6K1 T389 phosphorylation.
dactolisib Hs Inhibition 8.2 pIC50 22
pIC50 8.2 (IC50 6x10-9 M) [22]
Description: Measured as inhibition of downstream mTOR activated p70S6K
PP-242 Hs Inhibition 8.1 pIC50 1
pIC50 8.1 (IC50 8x10-9 M) [1]
CZ415 Hs Inhibition 8.1 pIC50 3
pIC50 8.1 (IC50 8.51x10-9 M) [3]
Description: Assessed in a competition binding assay using a mixed inhibitor lipid kinase matrix.
XL388 Hs Inhibition 8.0 pIC50 34
pIC50 8.0 (IC50 9.9x10-9 M) [34]
PP121 Hs Inhibition 8.0 pIC50 1
pIC50 8.0 (IC50 1x10-8 M) [1]
CC-223 Hs Inhibition 8.0 pIC50 23
pIC50 8.0 (IC50 1x10-8 M) [23]
KU-0063794 Hs Inhibition 8.0 pIC50 10
pIC50 8.0 (IC50 1x10-8 M) [10]
Description: Inhibition of immunoprecipitated mTORC1 (S6K1 as substrate) and mTORC2 (Akt as substrate).
eCF309 Hs Inhibition 7.8 pIC50 8
pIC50 7.8 (IC50 1.5x10-8 M) [8]
Description: In a biochemical assys using recombinant wild type enzyme.
PI-103 Hs Inhibition 7.5 pIC50 28
pIC50 7.5 (IC50 3x10-8 M) [28]
VS-5584 Hs Inhibition 7.4 pIC50 12
pIC50 7.4 (IC50 3.7x10-8 M) [12]
compound 11j [PMID: 23021994] Hs Inhibition 7.3 pIC50 11
pIC50 7.3 (IC50 5x10-8 M) [11]
GDC0084 Hs Inhibition 7.2 pIC50 13
pIC50 7.2 (IC50 7x10-8 M) [13]
LY3023414 Hs Inhibition 6.8 pIC50 2
pIC50 6.8 (IC50 1.65x10-7 M) [2]
temsirolimus Hs Inhibition 5.8 pIC50 17
pIC50 5.8 (IC50 1.76x10-6 M) [17]
MEN1611 Hs Inhibition 5.8 pIC50 25
pIC50 5.8 (IC50 1.6x10-6 M) [25]
STK16-IN-1 Hs Inhibition 5.3 pIC50 18
pIC50 5.3 (IC50 5.56x10-6 M) [18]
Description: In an in vitro enzymatic assay.
serabelisib Hs Inhibition >5.0 pIC50 29
pIC50 >5.0 (IC50 <1x10-5 M) [29]
RapaLink-1 Hs Inhibition - - 31
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
Reference: 6,37

Key to terms and symbols Click column headers to sort
Target used in screen: MTOR
Ligand Sp. Type Action Affinity Parameter
PP-242 Hs Inhibitor Inhibition 8.5 pKd
PI-103 Hs Inhibitor Inhibition 7.9 pKd
pictilisib Hs Inhibitor Inhibition 6.7 pKd
TG-100-115 Hs Inhibitor Inhibition 6.2 pKd
ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
erlotinib Hs Inhibitor Inhibition <5.5 pKd
GSK690693 Hs Inhibitor Inhibition <5.5 pKd
masitinib Hs Inhibitor Inhibition <5.5 pKd
A-674563 Hs Inhibitor Inhibition <5.5 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

Reference: 9...

Key to terms and symbols Click column headers to sort
Target used in screen: mTOR-FKBP12/nd
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
sirolimus Hs Inhibitor Inhibition -17.0 4.0
PI-103 Hs Inhibitor Inhibition -12.0 7.0
Akt inhibitor X Hs Inhibitor Inhibition 70.0 98.0
CGP74514A Hs Inhibitor Inhibition 70.0 109.0
AG 9 Hs Inhibitor Inhibition 70.0 101.0
AG 1295 Hs Inhibitor Inhibition 70.0 83.0
Gö 6976 Hs Inhibitor Inhibition 72.0 99.0
CGP53353 Hs Inhibitor Inhibition 73.0 85.0
MEK inhibitor I Hs Inhibitor Inhibition 74.0 95.0
PDGF RTK inhibitor Hs Inhibitor Inhibition 75.0 111.0
Target used in screen: mTOR/nd
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
LY 294002 Hs Inhibitor Inhibition 24.0 27.0
PI 3-Kg inhibitor Hs Inhibitor Inhibition 46.0 51.0
PI-103 Hs Inhibitor Inhibition 49.0 35.0
PKR inhibitor, negative control Hs Inhibitor Inhibition 51.0 64.0
sirolimus Hs Inhibitor Inhibition 57.0 51.0
PKR inhibitor Hs Inhibitor Inhibition 73.0 73.0
isogranulatimide Hs Inhibitor Inhibition 75.0 71.0
GSK-3 inhibitor IX Hs Inhibitor Inhibition 76.0 76.0
AG 1024 Hs Inhibitor Inhibition 77.0 86.0
DMBI Hs Inhibitor Inhibition 78.0 101.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Clinically-Relevant Mutations and Pathophysiology
Click column headers to sort
Type Species Amino acid change Nucleotide change Description Reference
Nonsense Human M2327I Activating mutation in the kinase domain of mTOR, which could theoretically confer a growth advantage in transformed cancer cells. 31
Clinically-Relevant Mutations and Pathophysiology Comments
Hyperactivation of mTOR kinase by single amino acid mutations such as M2327I (which has been identified in drug-naive patients) can reduce sensitivity to ATP-competitive mTOR inhibitors in vitro [31].


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13. Heffron TP, Ndubaku CO, Salphati L, Alicke B, Cheong J, Drobnick J, Edgar K, Gould SE, Lee LB, Lesnick JD et al.. (2016) Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR. ACS Med Chem Lett, 7 (4): 351-6. [PMID:27096040]

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17. Kong F, Zhu T, Yu K, Pagano TG, Desai P, Radebaugh G, Fawzi M. (2011) Isolation and structure of homotemsirolimuses A, B, and C. J. Nat. Prod., 74 (4): 547-53. [PMID:21438579]

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21. Liu Q, Wang J, Kang SA, Thoreen CC, Hur W, Ahmed T, Sabatini DM, Gray NS. (2011) Discovery of 9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a potent, selective, and orally available mammalian target of rapamycin (mTOR) inhibitor for treatment of cancer. J. Med. Chem., 54 (5): 1473-80. [PMID:21322566]

22. Maira SM, Stauffer F, Brueggen J, Furet P, Schnell C, Fritsch C, Brachmann S, Chène P, De Pover A, Schoemaker K et al.. (2008) Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity. Mol. Cancer Ther., 7 (7): 1851-63. [PMID:18606717]

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How to cite this page

FRAP subfamily: mechanistic target of rapamycin kinase. Last modified on 30/11/2018. Accessed on 23/05/2019. IUPHAR/BPS Guide to PHARMACOLOGY,