PP121 [Ligand Id: 8013] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1081312
  • protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase in Human [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527]
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  • EPH receptor B4/Ephrin type-B receptor 4 in Human [ChEMBL: CHEMBL5147] [GtoPdb: 1833] [UniProtKB: P54760]
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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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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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  • phosphatidylinositol 4-kinase beta/PI4-kinase beta subunit in Human [ChEMBL: CHEMBL3268] [GtoPdb: 2149] [UniProtKB: Q9UBF8]
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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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  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
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  • HCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase HCK in Human [ChEMBL: CHEMBL3234] [GtoPdb: 2032] [UniProtKB: P08631]
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  • ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
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  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
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  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
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  • platelet derived growth factor receptor alpha in Human [GtoPdb: 1803] [UniProtKB: P16234]
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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 - - 7.22 pIC50 60 nM IC50 Nat Chem Biol (2008) 4: 691-9 [PMID:18849971]
ChEMBL Inhibition of DNA-PK by radioactive phosphotransfer assay in presence of 10 uM ATP B 7.22 pIC50 60 nM IC50 Nat. Chem. Biol. (2008) 4: 691-699 [PMID:18849971]
EPH receptor B4/Ephrin type-B receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5147] [GtoPdb: 1833] [UniProtKB: P54760]
ChEMBL Inhibition of recombinant EphB4R by radioactive phosphotransfer assay in presence of 10 uM ATP B 6.72 pIC50 190 nM IC50 Nat. Chem. Biol. (2008) 4: 691-699 [PMID:18849971]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibition of recombinant EGFR by radioactive phosphotransfer assay in presence of 10 uM ATP B 6.59 pIC50 260 nM IC50 Nat. Chem. Biol. (2008) 4: 691-699 [PMID:18849971]
ChEMBL Inhibition of EGFR (unknown origin) B 6.59 pIC50 260 nM IC50 MedChemComm (2012) 3: 1337-1355
GtoPdb - - 6.59 pIC50 260 nM IC50 Nat Chem Biol (2008) 4: 691-9 [PMID:18849971]
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]
GtoPdb - - 7.28 pIC50 52 nM IC50 Nat Chem Biol (2008) 4: 691-9 [PMID:18849971]
ChEMBL Inhibition of PI3K p110-alpha B 7.28 pIC50 52 nM IC50 J. Med. Chem. (2010) 53: 1413-1437 [PMID:20166671]
ChEMBL Inhibition of recombinant PI3Kalpha by radioactive phosphotransfer assay in presence of 10 uM ATP B 7.28 pIC50 52 nM IC50 Nat. Chem. Biol. (2008) 4: 691-699 [PMID:18849971]
ChEMBL Inhibition of PI3Kalpha (unknown origin) B 7.28 pIC50 52 nM IC50 MedChemComm (2012) 3: 1337-1355
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]
GtoPdb - - 5.85 pIC50 1400 nM IC50 Nat Chem Biol (2008) 4: 691-9 [PMID:18849971]
ChEMBL Inhibition of recombinant PI3Kbeta by radioactive phosphotransfer assay in presence of 10 uM ATP B 5.85 pIC50 1400 nM IC50 Nat. Chem. Biol. (2008) 4: 691-699 [PMID:18849971]
ChEMBL Inhibition of PI3Kbeta (unknown origin) B 5.85 pIC50 1400 nM IC50 MedChemComm (2012) 3: 1337-1355
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]
GtoPdb - - 6.82 pIC50 150 nM IC50 Nat Chem Biol (2008) 4: 691-9 [PMID:18849971]
ChEMBL Inhibition of recombinant PI3Kdelta by radioactive phosphotransfer assay in presence of 10 uM ATP B 6.82 pIC50 150 nM IC50 Nat. Chem. Biol. (2008) 4: 691-699 [PMID:18849971]
ChEMBL Inhibition of PI3Kdelta (unknown origin) B 6.82 pIC50 150 nM IC50 MedChemComm (2012) 3: 1337-1355
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 recombinant PI3Kgamma by radioactive phosphotransfer assay in presence of 10 uM ATP B 5.96 pIC50 1100 nM IC50 Nat. Chem. Biol. (2008) 4: 691-699 [PMID:18849971]
ChEMBL Inhibition of PI3Kgamma (unknown origin) B 5.96 pIC50 1100 nM IC50 MedChemComm (2012) 3: 1337-1355
GtoPdb - - 5.96 pIC50 1100 nM IC50 Nat Chem Biol (2008) 4: 691-9 [PMID:18849971]
phosphatidylinositol 4-kinase beta/PI4-kinase beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3268] [GtoPdb: 2149] [UniProtKB: Q9UBF8]
ChEMBL Inhibition of recombinant PI4Kbeta by radioactive phosphotransfer assay in presence of 10 uM ATP B 7.22 pIC50 60 nM IC50 Nat. Chem. Biol. (2008) 4: 691-699 [PMID:18849971]
ATR serine/threonine kinase/Serine-protein kinase ATR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5024] [GtoPdb: 1935] [UniProtKB: Q13535]
ChEMBL Inhibition of human recombinant FLAG-tagged full length ATR expressed in mammalian cell line co-expressing human recombinant cMyc-tagged full length ATRIP B 5.85 pIC50 1420 nM IC50 Bioorg Med Chem Lett (2017) 27: 750-754 [PMID:28131712]
mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345]
GtoPdb - - 8 pIC50 10 nM IC50 Nat Chem Biol (2008) 4: 691-9 [PMID:18849971]
ChEMBL Inhibition of mTOR B 8 pIC50 10 nM IC50 J. Med. Chem. (2010) 53: 1413-1437 [PMID:20166671]
ChEMBL Inhibition of recombinant mTOR by radioactive phosphotransfer assay in presence of 10 uM ATP B 8 pIC50 <10 nM IC50 Nat. Chem. Biol. (2008) 4: 691-699 [PMID:18849971]
ChEMBL Inhibition of mTOR (unknown origin) B 8 pIC50 10 nM IC50 MedChemComm (2012) 3: 1337-1355
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
GtoPdb - - 7.74 pIC50 18 nM IC50 Nat Chem Biol (2008) 4: 691-9 [PMID:18849971]
ChEMBL Inhibition of recombinant c-Abl by radioactive phosphotransfer assay in presence of 10 uM ATP B 7.74 pIC50 18 nM IC50 Nat. Chem. Biol. (2008) 4: 691-699 [PMID:18849971]
ChEMBL Inhibition of ABL (unknown origin) B 7.74 pIC50 18 nM IC50 MedChemComm (2012) 3: 1337-1355
ChEMBL Inhibition of ABL1 at 1 uM after 60 mins by FRET assay in presence of 10 uM ATP B 8.7 pIC50 2 nM IC50 Nat. Chem. Biol. (2008) 4: 691-699 [PMID:18849971]
HCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase HCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3234] [GtoPdb: 2032] [UniProtKB: P08631]
ChEMBL Inhibition of recombinant HCK by radioactive phosphotransfer assay in presence of 10 uM ATP B 8.1 pIC50 8 nM IC50 Nat. Chem. Biol. (2008) 4: 691-699 [PMID:18849971]
ChEMBL Inhibition of HCK (unknown origin) B 8.1 pIC50 8 nM IC50 MedChemComm (2012) 3: 1337-1355
GtoPdb - - 8.1 pIC50 8 nM IC50 Nat Chem Biol (2008) 4: 691-9 [PMID:18849971]
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
ChEMBL Inhibition of Ret B 9 pIC50 <1 nM IC50 Nat. Chem. Biol. (2008) 4: 691-699 [PMID:18849971]
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
GtoPdb - - 7.85 pIC50 14 nM IC50 Nat Chem Biol (2008) 4: 691-9 [PMID:18849971]
ChEMBL Inhibition of Src B 7.85 pIC50 14 nM IC50 J. Med. Chem. (2010) 53: 1413-1437 [PMID:20166671]
ChEMBL Inhibition of recombinant c-Src by radioactive phosphotransfer assay in presence of 10 uM ATP B 7.85 pIC50 14 nM IC50 Nat. Chem. Biol. (2008) 4: 691-699 [PMID:18849971]
ChEMBL Inhibition of Src (unknown origin) B 7.85 pIC50 14 nM IC50 MedChemComm (2012) 3: 1337-1355
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
ChEMBL Inhibition of VEGFR2-mediated proliferation of HUVEC in VEGF-supplemented medium at 0.04 to 10 uM after 24 hrs by fluorescence assay B 7.39 pIC50 41 nM IC50 Nat. Chem. Biol. (2008) 4: 691-699 [PMID:18849971]
GtoPdb - - 7.92 pIC50 12 nM IC50 Nat Chem Biol (2008) 4: 691-9 [PMID:18849971]
ChEMBL Inhibition of VEGFR2 B 7.92 pIC50 12 nM IC50 J. Med. Chem. (2010) 53: 1413-1437 [PMID:20166671]
ChEMBL Inhibition of recombinant VEGFR2 by radioactive phosphotransfer assay in presence of 10 uM ATP B 7.92 pIC50 12 nM IC50 Nat. Chem. Biol. (2008) 4: 691-699 [PMID:18849971]
platelet derived growth factor receptor alpha in Human [GtoPdb: 1803] [UniProtKB: P16234]
GtoPdb - - 8.7 pIC50 2 nM IC50 Nat Chem Biol (2008) 4: 691-9 [PMID:18849971]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]