torin 1 [Ligand Id: 8004] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1256459 (Torin1)
  • protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase in Human [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527]
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  • phosphatidylinositol 3-kinase catalytic subunit type 3/Phosphatidylinositol 3-kinase catalytic subunit type 3 in Human [ChEMBL: CHEMBL1075165] [GtoPdb: 2152] [UniProtKB: Q8NEB9]
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  • phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 beta/Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing beta polypeptide in Human [ChEMBL: CHEMBL5554] [GtoPdb: 2151] [UniProtKB: O00750]
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  • phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 alpha/Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing subunit alpha in Human [ChEMBL: CHEMBL1075102] [GtoPdb: 2150] [UniProtKB: O00443]
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  • phosphoinositide-3-kinase regulatory subunit 1/phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha/p85-alpha in Human [ChEMBL: CHEMBL2111367] [GtoPdb: 25032153] [UniProtKB: P27986P42336]
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha subunit in Human [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336]
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/phosphoinositide-3-kinase regulatory subunit 1/PI3-kinase p110-delta/p85-alpha in Human [ChEMBL: CHEMBL2111432] [GtoPdb: 21552503] [UniProtKB: O00329P27986]
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/PI3-kinase p110-gamma subunit in Human [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736]
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  • phosphatidylinositol 4-kinase alpha/PI4-kinase alpha subunit in Human [ChEMBL: CHEMBL3667] [GtoPdb: 2148] [UniProtKB: P42356]
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  • phosphatidylinositol 4-kinase beta/PI4-kinase beta subunit in Human [ChEMBL: CHEMBL3268] [GtoPdb: 2149] [UniProtKB: Q9UBF8]
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  • CDC42 binding protein kinase alpha/Serine/threonine-protein kinase MRCK-A in Human [ChEMBL: CHEMBL4516] [GtoPdb: 1507] [UniProtKB: Q5VT25]
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  • mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345]
  • mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Mouse [ChEMBL: CHEMBL1255165] [GtoPdb: 2109] [UniProtKB: Q9JLN9]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527]
ChEMBL Inhibition of DNA-PK B 8.2 pIC50 6.34 nM IC50 J. Med. Chem. (2010) 53: 7146-7155 [PMID:20860370]
mechanistic target of rapamycin kinase/mTORC1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4296661] [GtoPdb: 2109] [UniProtKB: P42345Q8N122Q9BVC4]
ChEMBL Inhibition of N-terminally FLAG-tagged mTORC1 (unknown origin) expressed in HEK293T cells using S6K1 or Akt1 as substrate after 20 mins by immunoblotting assay B 8.7 pIC50 2 nM IC50 J Med Chem (2018) 61: 4656-4687 [PMID:29211480]
GtoPdb Assayed using mTORC1 complex - 9.54 pIC50 0.29 nM IC50 J Med Chem (2010) 53: 7146-55 [PMID:20860370]
mechanistic target of rapamycin kinase/mTORC2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4523999] [GtoPdb: 2109] [UniProtKB: P42345Q6R327Q9BPZ7Q9BVC4]
ChEMBL Inhibition of N-terminally FLAG-tagged mTORC2 (unknown origin) expressed in human HeLa cells using S6K1 or Akt1 as substrate after 20 mins by immunoblotting assay B 8 pIC50 10 nM IC50 J Med Chem (2018) 61: 4656-4687 [PMID:29211480]
GtoPdb Assayed using mTORC1 complex - 9.54 pIC50 0.29 nM IC50 J Med Chem (2010) 53: 7146-55 [PMID:20860370]
phosphatidylinositol 3-kinase catalytic subunit type 3/Phosphatidylinositol 3-kinase catalytic subunit type 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075165] [GtoPdb: 2152] [UniProtKB: Q8NEB9]
ChEMBL Inhibition of human hVPS34 B 6.27 pIC50 533 nM IC50 J. Med. Chem. (2010) 53: 7146-7155 [PMID:20860370]
phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 beta/Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing beta polypeptide in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5554] [GtoPdb: 2151] [UniProtKB: O00750]
ChEMBL Inhibition of PI3K-C2 beta B 6.26 pIC50 549 nM IC50 J. Med. Chem. (2010) 53: 7146-7155 [PMID:20860370]
phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 alpha/Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075102] [GtoPdb: 2150] [UniProtKB: O00443]
ChEMBL Inhibition of PI3K-C2 alpha B 6.75 pIC50 176 nM IC50 J. Med. Chem. (2010) 53: 7146-7155 [PMID:20860370]
phosphoinositide-3-kinase regulatory subunit 1/phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha/p85-alpha in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111367] [GtoPdb: 25032153] [UniProtKB: P27986P42336]
ChEMBL Inhibition of P110alpha/p85-alpha B 6.6 pIC50 250 nM IC50 J. Med. Chem. (2010) 53: 7146-7155 [PMID:20860370]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336]
ChEMBL Binding affinity to PIK3CA B 7.64 pKd 23 nM Kd J. Med. Chem. (2010) 53: 7146-7155 [PMID:20860370]
ChEMBL Binding affinity to PIK3CA I800L mutant B 7.85 pKd 14 nM Kd J. Med. Chem. (2010) 53: 7146-7155 [PMID:20860370]
ChEMBL Inhibition of PI3Kalpha in human PC3 cells expressing Akt1 S473D mutant assessed as phosphorylation of Akt Thr308 by immunoblotting B 5.74 pEC50 1800 nM EC50 J. Med. Chem. (2011) 54: 1473-1480 [PMID:21322566]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/phosphoinositide-3-kinase regulatory subunit 1/PI3-kinase p110-delta/p85-alpha in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111432] [GtoPdb: 21552503] [UniProtKB: O00329P27986]
ChEMBL Inhibition of P110delta/p85-alpha B 6.25 pIC50 564 nM IC50 J. Med. Chem. (2010) 53: 7146-7155 [PMID:20860370]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/PI3-kinase p110-gamma subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736]
ChEMBL Inhibition of P110gamma B 6.77 pIC50 171 nM IC50 J. Med. Chem. (2010) 53: 7146-7155 [PMID:20860370]
phosphatidylinositol 4-kinase alpha/PI4-kinase alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3667] [GtoPdb: 2148] [UniProtKB: P42356]
ChEMBL Inhibition of PI4Kalpha B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2010) 53: 7146-7155 [PMID:20860370]
phosphatidylinositol 4-kinase beta/PI4-kinase beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3268] [GtoPdb: 2149] [UniProtKB: Q9UBF8]
ChEMBL Inhibition of PI4Kbeta B 5.18 pIC50 6680 nM IC50 J. Med. Chem. (2010) 53: 7146-7155 [PMID:20860370]
CDC42 binding protein kinase alpha/Serine/threonine-protein kinase MRCK-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4516] [GtoPdb: 1507] [UniProtKB: Q5VT25]
ChEMBL Binding affinity to MRCKA B 5 pKd 10000 nM Kd J. Med. Chem. (2010) 53: 7146-7155 [PMID:20860370]
mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345]
ChEMBL Binding affinity to mTOR B 9.38 pKd 0.42 nM Kd J. Med. Chem. (2010) 53: 7146-7155 [PMID:20860370]
ChEMBL Inhibition of human mTOR B 8.36 pIC50 4.32 nM IC50 J. Med. Chem. (2010) 53: 7146-7155 [PMID:20860370]
ChEMBL Inhibition of human mTOR complex 1 after 30 mins by FRET assay B 9.54 pIC50 0.29 nM IC50 J. Med. Chem. (2010) 53: 7146-7155 [PMID:20860370]
GtoPdb Assayed using mTORC1 complex - 9.54 pIC50 0.29 nM IC50 J Med Chem (2010) 53: 7146-55 [PMID:20860370]
mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1255165] [GtoPdb: 2109] [UniProtKB: Q9JLN9]
ChEMBL Inhibition of mTOR in p53-deficient MEF assessed as phosphorylation of S6K1 at Thr389 by immunoblotting B 8.7 pIC50 2 nM IC50 J. Med. Chem. (2010) 53: 7146-7155 [PMID:20860370]
ChEMBL Inhibition of mTOR in p53-deficient MEF assessed as phosphorylation of S6K1 at Thr389 by immunoblotting B 8.7 pEC50 2 nM EC50 J. Med. Chem. (2011) 54: 1473-1480 [PMID:21322566]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]