PP121 [Ligand Id: 8013] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL1081312 |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
| 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 |
| 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] |
| 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 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]
