KU-0063794 [Ligand Id: 9360] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1078983 (AZD-2014) |
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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] |
| 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] |
| 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 33:
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]
