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: 2503, 2153] [UniProtKB: P27986, P42336]
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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: 2155, 2503] [UniProtKB: O00329, P27986]
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/PI3-kinase p110-delta subunit in Human [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329]
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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]
ChEMBL Selectivity interaction (SelectScreen Kinase Profiling (biochemical enzymatic kinase assays)) EUB0000092b PRKDC B 8.2 pIC50 6.34 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
mechanistic target of rapamycin kinase/mTORC1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4296661] [GtoPdb: 2109] [UniProtKB: P42345, Q8N122, Q9BVC4]
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]
ChEMBL Inhibition of mTORC1 (unknown origin) B 9.54 pIC50 0.29 nM IC50 Eur J Med Chem (2023) 246: 114971-114971 [PMID:36462440]
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: P42345, Q6R327, Q9BPZ7, Q9BVC4]
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]
ChEMBL Inhibition of mTORC2 (unknown origin) B 8.7 pIC50 2 nM IC50 Eur J Med Chem (2023) 246: 114971-114971 [PMID:36462440]
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]
ChEMBL Selectivity interaction (SelectScreen Kinase Profiling (biochemical enzymatic kinase assays)) EUB0000092b PIK3C3 B 6.27 pIC50 533 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
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]
ChEMBL Selectivity interaction (SelectScreen Kinase Profiling (biochemical enzymatic kinase assays)) EUB0000092b PIK3C2B B 6.26 pIC50 549 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
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]
ChEMBL Selectivity interaction (SelectScreen Kinase Profiling (biochemical enzymatic kinase assays)) EUB0000092b PIK3C2A B 6.75 pIC50 176 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
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: 2503, 2153] [UniProtKB: P27986, P42336]
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 Selectivity interaction (Competition-binding assay (DiscoverX)) EUB0000092b PIK3CA B 7.64 pKd 23 nM Kd Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Binding affinity to PIK3CA I800L mutant B 7.85 pKd 14 nM Kd J Med Chem (2010) 53: 7146-7155 [PMID:20860370]
ChEMBL Selectivity interaction (Competition-binding assay (DiscoverX)) EUB0000092b PIK3CA B 7.85 pKd 14 nM Kd Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Selectivity interaction (SelectScreen Kinase Profiling (biochemical enzymatic kinase assays)) EUB0000092b PIK3CA B 6.6 pIC50 250 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
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: 2155, 2503] [UniProtKB: O00329, P27986]
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 delta/PI3-kinase p110-delta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329]
ChEMBL Selectivity interaction (SelectScreen Kinase Profiling (biochemical enzymatic kinase assays)) EUB0000092b PIK3CD B 6.25 pIC50 564 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
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]
ChEMBL Selectivity interaction (SelectScreen Kinase Profiling (biochemical enzymatic kinase assays)) EUB0000092b PIK3CG B 6.77 pIC50 171 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
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]
ChEMBL Selectivity interaction (SelectScreen Kinase Profiling (biochemical enzymatic kinase assays)) EUB0000092b PI4KA B 5 pIC50 >10000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
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]
ChEMBL Selectivity interaction (SelectScreen Kinase Profiling (biochemical enzymatic kinase assays)) EUB0000092b PI4KB B 5.18 pIC50 6680 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
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]
ChEMBL Selectivity interaction (Competition-binding assay (DiscoverX)) EUB0000092b CDC42BPA B 5 pKd 10000 nM Kd Selectivity Literature for EUbOPEN Chemogenomic Library
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 Selectivity interaction (Competition-binding assay (DiscoverX)) EUB0000092b MTOR B 9.38 pKd 0.42 nM Kd Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of human mTOR B 8.36 pIC50 4.32 nM IC50 J Med Chem (2010) 53: 7146-7155 [PMID:20860370]
ChEMBL Selectivity interaction (SelectScreen Kinase Profiling (biochemical enzymatic kinase assays)) EUB0000092b MTOR B 8.36 pIC50 4.32 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (Immunoblotting (phosphorylation of S6K1 Thr-389 in p53xe2x88x92/xe2x88x92 MEFs cells)) EUB0000092b MTOR F 8.7 pIC50 2 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Biochemical interaction: (Lanthascreen time-resolved FRET assay (Invitrogen)) EUB0000092b MTOR B 9.38 pIC50 0.42 nM IC50 Affinity Biochemical Literature for EUbOPEN Chemogenomic Library
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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]