pilaralisib [Ligand Id: 7963] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3218575 (SAR-245408, XL-147)
  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha subunit in Human [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336]
  • This target only has 0 pki data point
1 CHEMBL3218575_lig_chart_1 PI3-kinase p110-alpha subunit Human
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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]
  • This target only has 0 pki data point
2 CHEMBL3218575_lig_chart_2 PI3-kinase p110-beta subunit Human
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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]
  • This target only has 0 pki data point
3 CHEMBL3218575_lig_chart_3 PI3-kinase p110-delta subunit Human
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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]
  • This target only has 0 pki data point
4 CHEMBL3218575_lig_chart_4 PI3-kinase p110-gamma subunit Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 of PI3Kalpha (unknown origin) B 7.41 pIC50 39 nM IC50 MedChemComm (2012) 3: 1337-1355
GtoPdb - - 7.41 pIC50 39 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]
ChEMBL Inhibition of PI3Kbeta (unknown origin) B 6.42 pIC50 383 nM IC50 MedChemComm (2012) 3: 1337-1355
GtoPdb - - 6.42 pIC50 383 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 - - 7.44 pIC50 36 nM IC50 Medchemcomm (2012) 3: 1337-1355
ChEMBL Inhibition of PI3Kdelta (unknown origin) B 7.44 pIC50 36 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 PI3Kgamma (unknown origin) B 7.64 pIC50 23 nM IC50 MedChemComm (2012) 3: 1337-1355
GtoPdb - - 7.64 pIC50 23 nM IC50 Medchemcomm (2012) 3: 1337-1355

ChEMBL data shown on this page come from version 27:

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]