torin 2 [Ligand Id: 8839] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1765602
  • 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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  • ATM serine/threonine kinase/Serine-protein kinase ATM in Human [ChEMBL: CHEMBL3797] [GtoPdb: 1934] [UniProtKB: Q13315]
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  • ATR serine/threonine kinase/Serine-protein kinase ATR in Human [ChEMBL: CHEMBL5024] [GtoPdb: 1935] [UniProtKB: Q13535]
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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]
GtoPdb - - 9.3 pIC50 0.5 nM IC50 J Med Chem (2011) 54: 1473-80 [PMID:21322566]
ChEMBL Inhibition of DNA-PK B 9.3 pIC50 0.5 nM IC50 J Med Chem (2011) 54: 1473-1480 [PMID:21322566]
ChEMBL Inhibition of DNAPK in human HCT116 cells assessed as after 1 hr by Western blot analysis B 6.93 pEC50 118 nM EC50 J Med Chem (2018) 61: 4656-4687 [PMID:29211480]
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 pIC50 <10 nM IC50 J Med Chem (2018) 61: 4656-4687 [PMID:29211480]
GtoPdb - - 8.55 pIC50 2.81 nM IC50 J Med Chem (2011) 54: 1473-80 [PMID:21322566]
ChEMBL Inhibition of mTORC1 in human HCT116 cells assessed as reduction in T389 phosphorylation on RPS6KB1 after 1 hr by Western blot analysis B 9.6 pEC50 0.25 nM EC50 J Med Chem (2018) 61: 4656-4687 [PMID:29211480]
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 - - 8.55 pIC50 2.81 nM IC50 J Med Chem (2011) 54: 1473-80 [PMID:21322566]
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 hVPS34 B 8.07 pIC50 8.58 nM IC50 J Med Chem (2011) 54: 1473-1480 [PMID:21322566]
GtoPdb - - 8.07 pIC50 8.58 nM IC50 J Med Chem (2011) 54: 1473-80 [PMID:21322566]
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]
GtoPdb - - 7.61 pIC50 24.5 nM IC50 J Med Chem (2011) 54: 1473-80 [PMID:21322566]
ChEMBL Inhibition of PI3K-C2beta B 7.61 pIC50 24.5 nM IC50 J Med Chem (2011) 54: 1473-1480 [PMID:21322566]
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]
GtoPdb - - 7.55 pIC50 28.1 nM IC50 J Med Chem (2011) 54: 1473-80 [PMID:21322566]
ChEMBL Inhibition of PI3K-C2alpha B 7.55 pIC50 28.1 nM IC50 J Med Chem (2011) 54: 1473-1480 [PMID:21322566]
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 P110 alpha/p85alpha B 8.33 pIC50 4.68 nM IC50 J Med Chem (2011) 54: 1473-1480 [PMID:21322566]
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 Inhibition of PI3Kalpha in human PC3 cells expressing Akt1 S473D mutant assessed as phosphorylation of Akt Thr308 by immunoblotting B 6.7 pEC50 200 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/P85alpha B 7.76 pIC50 17.5 nM IC50 J Med Chem (2011) 54: 1473-1480 [PMID:21322566]
GtoPdb - - 8.25 pIC50 5.67 nM IC50 J Med Chem (2011) 54: 1473-80 [PMID:21322566]
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 8.25 pIC50 5.67 nM IC50 J Med Chem (2011) 54: 1473-1480 [PMID:21322566]
phosphatidylinositol 4-kinase alpha/PI4-kinase alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3667] [GtoPdb: 2148] [UniProtKB: P42356]
ChEMBL Inhibition of PI4K alpha B 5 pIC50 >10000 nM IC50 J Med Chem (2011) 54: 1473-1480 [PMID:21322566]
phosphatidylinositol 4-kinase beta/PI4-kinase beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3268] [GtoPdb: 2149] [UniProtKB: Q9UBF8]
ChEMBL Inhibition of PI4K beta B 7.74 pIC50 18.3 nM IC50 J Med Chem (2011) 54: 1473-1480 [PMID:21322566]
GtoPdb - - 7.74 pIC50 18.3 nM IC50 J Med Chem (2011) 54: 1473-80 [PMID:21322566]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Gametocytocidal activity against Plasmodium falciparum after 72 hrs by Alamar Blue assay F 8.1 pIC50 8 nM IC50 Bioorg Med Chem Lett (2016) 26: 2907-2911 [PMID:27156776]
ATM serine/threonine kinase/Serine-protein kinase ATM in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3797] [GtoPdb: 1934] [UniProtKB: Q13315]
ChEMBL Inhibition of ATM in human HCT116 cells assessed as after 1 hr by Western blot analysis B 7.55 pEC50 28 nM EC50 J Med Chem (2018) 61: 4656-4687 [PMID:29211480]
ATR serine/threonine kinase/Serine-protein kinase ATR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5024] [GtoPdb: 1935] [UniProtKB: Q13535]
ChEMBL Inhibition of ATR in human HCT116 cells assessed as after 1 hr by Western blot analysis B 7.46 pEC50 35 nM EC50 J Med Chem (2018) 61: 4656-4687 [PMID:29211480]
mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345]
GtoPdb - - 8.55 pIC50 2.81 nM IC50 J Med Chem (2011) 54: 1473-80 [PMID:21322566]
ChEMBL Inhibition of mTOR (unknown origin) B 9.6 pIC50 0.25 nM IC50 Bioorg Med Chem (2018) 26: 4537-4543 [PMID:30077608]
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 9.6 pEC50 0.25 nM EC50 J Med Chem (2011) 54: 1473-1480 [PMID:21322566]

ChEMBL data shown on this page come from version 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]