PP121 [Ligand Id: 8013] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1081312 |
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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] |
| 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 in 4EBP1 phosphorylation at Thr37/46 by AlphaLISA assay | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2023) 66: 149-169 [PMID:36533617] |
| ChEMBL | Inhibition of mTORC1 in human MDA-MB-468 cells assessed as reduction in P70S6K phosphorylation at Thr389 by AlphaLISA assay | B | 7.07 | pIC50 | 86 | nM | IC50 | J Med Chem (2023) 66: 149-169 [PMID:36533617] |
| GtoPdb | - | - | 8 | pIC50 | 10 | 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 |
| ChEMBL | Inhibition of mTOR (unknown origin) using U-Light-4E-BP1 peptide as a substrate in the presence of ATP incubated for 30 mins by Lance ultra assay | B | 8 | pIC50 | 10 | nM | IC50 | Eur J Med Chem (2021) 225: 113824-113824 [PMID:34509167] |
| ChEMBL | Inhibition of recombinant mTOR (unknown origin) using 4EBP1 as substrate in presence of [gamma-32P]ATP by radiometric scintillation assay | B | 8 | pIC50 | 10 | nM | IC50 | Eur J Med Chem (2020) 208: 112820-112820 [PMID:32966896] |
| 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 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]
