KU-0063794 [Ligand Id: 9360] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1078983 (AZD-2014)
  • protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase in Human [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527]
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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 beta/PI3-kinase p110-beta subunit in Human [ChEMBL: CHEMBL3145] [GtoPdb: 2154] [UniProtKB: P42338]
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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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  • 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]
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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 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2009) 19: 5950-5953 [PMID:19762236]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG B 5.08 pIC50 8300 nM IC50 Bioorg Med Chem Lett (2013) 23: 1212-1216 [PMID:23375793]
mechanistic target of rapamycin kinase/mTORC1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4296661] [GtoPdb: 2109] [UniProtKB: P42345, Q8N122, Q9BVC4]
ChEMBL Inhibition of mTORC1 in human MDA-MB-468 cells assessed as reduction of pS6 phosphorylation at Ser235/236 after 2 hrs B 6.18 pIC50 660 nM IC50 Bioorg Med Chem Lett (2013) 23: 1212-1216 [PMID:23375793]
GtoPdb Inhibition of immunoprecipitated mTORC1 (S6K1 as substrate) and mTORC2 (Akt as substrate). - 8 pIC50 10 nM IC50 Biochem J (2009) 421: 29-42 [PMID:19402821]
ChEMBL Inhibition of mTORC1 in HEK293 cells using GST-tagged S6K1 or Akt1 as substrate after 30 mins by immunoblotting assay B 8 pIC50 10 nM IC50 J Med Chem (2018) 61: 4656-4687 [PMID:29211480]
ChEMBL Inhibition of mTORC1 in human HEK293 cells assessed as decrease in phosphorylated S6K level incubated for 30 mins by immunoblot assay B 8 pIC50 10 nM IC50 Eur J Med Chem (2020) 208: 112820-112820 [PMID:32966896]
mechanistic target of rapamycin kinase/mTORC2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4523999] [GtoPdb: 2109] [UniProtKB: P42345, Q6R327, Q9BPZ7, Q9BVC4]
GtoPdb Inhibition of immunoprecipitated mTORC1 (S6K1 as substrate) and mTORC2 (Akt as substrate). - 8 pIC50 10 nM IC50 Biochem J (2009) 421: 29-42 [PMID:19402821]
ChEMBL Inhibition of mTORC2 in HEK293 cells using GST-tagged S6K1 or Akt1 as substrate after 30 mins by immunoblotting assay B 8 pIC50 10 nM IC50 J Med Chem (2018) 61: 4656-4687 [PMID:29211480]
ChEMBL Inhibition of mTORC2 in human HEK293 cells assessed as decrease in phosphorylated Akt level incubated for 30 mins by immunoblot assay B 8 pIC50 10 nM IC50 Eur J Med Chem (2020) 208: 112820-112820 [PMID:32966896]
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 PI3K-alpha-mediated PIP2 phosphorylation after 20 mins by alphascreen competition assay B 5.05 pIC50 8900 nM IC50 Bioorg Med Chem Lett (2009) 19: 5950-5953 [PMID:19762236]
ChEMBL Inhibition of PI3Kalpha (unknown origin) using lipid PIP2 as substrate B 5.05 pIC50 8900 nM IC50 Bioorg Med Chem Lett (2013) 23: 1212-1216 [PMID:23375793]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/PI3-kinase p110-beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3145] [GtoPdb: 2154] [UniProtKB: P42338]
ChEMBL Inhibition PI3K-beta-mediated PIP2 phosphorylation after 20 mins by alphascreen competition assay B 4.52 pIC50 >30000 nM IC50 Bioorg Med Chem Lett (2009) 19: 5950-5953 [PMID:19762236]
ChEMBL Inhibition of PI3Kbeta (unknown origin) using lipid PIP2 as substrate B 4.52 pIC50 >30000 nM IC50 Bioorg Med Chem Lett (2013) 23: 1212-1216 [PMID:23375793]
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 Inhibition PI3K-delta-mediated PIP2 phosphorylation after 20 mins by alphascreen competition assay B 5.28 pIC50 >5300 nM IC50 Bioorg Med Chem Lett (2009) 19: 5950-5953 [PMID:19762236]
ChEMBL Inhibition of PI3Kdelta (unknown origin) using lipid PIP2 as substrate B 5.28 pIC50 5300 nM IC50 Bioorg Med Chem Lett (2013) 23: 1212-1216 [PMID:23375793]
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 PI3K-gamma-mediated PIP2 phosphorylation after 20 mins by alphascreen competition assay B 4.52 pIC50 >30000 nM IC50 Bioorg Med Chem Lett (2009) 19: 5950-5953 [PMID:19762236]
ChEMBL Inhibition of PI3Kgamma (unknown origin) using lipid PIP2 as substrate B 4.52 pIC50 >30000 nM IC50 Bioorg Med Chem Lett (2013) 23: 1212-1216 [PMID:23375793]
ATR serine/threonine kinase/Serine-protein kinase ATR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5024] [GtoPdb: 1935] [UniProtKB: Q13535]
ChEMBL Inhibition of ATR B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2009) 19: 5950-5953 [PMID:19762236]
mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345]
ChEMBL Inhibition of mTORC2 in human U87MG cells assessed as phosphorylated AKT (Ser473) level after 2 hrs by Western blotting B 6.82 pIC50 150 nM IC50 Bioorg Med Chem Lett (2009) 19: 5950-5953 [PMID:19762236]
ChEMBL Inhibition of mTORC1 in human U87MG cells assessed as phosphorylated S6 ribosomal protein (Ser235/236) level after 2 hrs by Western blotting B 7 pIC50 100 nM IC50 Bioorg Med Chem Lett (2009) 19: 5950-5953 [PMID:19762236]
GtoPdb Inhibition of immunoprecipitated mTORC1 (S6K1 as substrate) and mTORC2 (Akt as substrate). - 8 pIC50 10 nM IC50 Biochem J (2009) 421: 29-42 [PMID:19402821]
ChEMBL Inhibition of mTOR (unknown origin) B 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (2021) 47: 128204-128204 [PMID:34139324]
ChEMBL Inhibition of recombinant FLAG-tagged mTOR expressed in HEK293 cells using biotinylated p70S6K substrate after 2 hrs by alphascreen competition assay B 8.52 pIC50 3 nM IC50 Bioorg Med Chem Lett (2009) 19: 5950-5953 [PMID:19762236]
ChEMBL Inhibition of recombinant FLAG-tagged mTOR (1362 to 2549) (unknown origin) expressed in HEK293 cells B 8.6 pIC50 2.5 nM IC50 Bioorg Med Chem Lett (2013) 23: 1212-1216 [PMID:23375793]

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]