dezapelisib [Ligand Id: 9728] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2216863 (Dezapelisib, INCB040093)
  • phosphoinositide-3-kinase regulatory subunit 1/phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha/p85-alpha in Human [ChEMBL: CHEMBL2111367] [GtoPdb: 25032153] [UniProtKB: P27986P42336]
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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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  • phosphoinositide-3-kinase regulatory subunit 1/phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/PI3K p110 beta/p85 alpha in Human [ChEMBL: CHEMBL3038510] [GtoPdb: 25032154] [UniProtKB: P27986P42338]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
phosphoinositide-3-kinase regulatory subunit 1/phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha/p85-alpha in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111367] [GtoPdb: 25032153] [UniProtKB: P27986P42336]
ChEMBL Inhibition of human N-terminal His-tagged PI3Kalpha/p85alpha expressed in Spodoptera frugiperda using phosphatidylinositol as substrate B 5 pIC50 >10000 nM IC50 Eur J Med Chem (2019) 163: 413-427 [PMID:30530193]
GtoPdb - - 6.3 pIC50 >500 nM IC50 WO2011008487. Pyrimidinones as PI3K inhibitors (2011)
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 The same value was obtained using an enzyme activity assay and a scintillation proximity assay. - 7.3 pIC50 <50 nM IC50 WO2011008487. Pyrimidinones as PI3K inhibitors (2011)
ChEMBL Inhibition of PI3Kdelta in B-cells by proliferation assay B 7.3 pIC50 <50 nM IC50 J Med Chem (2012) 55: 8559-8581 [PMID:22924688]
ChEMBL Inhibition of PI3Kdelta B 7.3 pIC50 <50 nM IC50 J Med Chem (2012) 55: 8559-8581 [PMID:22924688]
ChEMBL Inhibition of PI3Kdelta (unknown origin) B 7.51 pIC50 31 nM IC50 Eur J Med Chem (2019) 163: 413-427 [PMID:30530193]
ChEMBL Inhibition of PI3Kdelta in basophil derived from B-cell malignant patient B 7.51 pIC50 31 nM IC50 J Med Chem (2019) 62: 4783-4814 [PMID:30582813]
ChEMBL Inhibition of PI3Kdelta (unknown origin) using D-myophosphatidylinositol 4,5-bisphosphate as substrate incubated for 120 mins by [gamma-33P]ATP based SPA assay B 8.47 pIC50 3.4 nM IC50 ACS Med Chem Lett (2019) 10: 1554-1560 [PMID:31749910]
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 in basophil derived from B-cell malignant patient B 5.64 pIC50 2300 nM IC50 J Med Chem (2019) 62: 4783-4814 [PMID:30582813]
ChEMBL Inhibition of PI3Kgamma (unknown origin) B 5.64 pIC50 2297 nM IC50 Eur J Med Chem (2019) 163: 413-427 [PMID:30530193]
GtoPdb - - 6.3 pIC50 >500 nM IC50 WO2011008487. Pyrimidinones as PI3K inhibitors (2011)
phosphoinositide-3-kinase regulatory subunit 1/phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/PI3K p110 beta/p85 alpha in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038510] [GtoPdb: 25032154] [UniProtKB: P27986P42338]
ChEMBL Inhibition of human full length recombinant N-terminal His-tagged PI3Kbeta/p85alpha expressed in baculovirus infected Sf21 insect cells B 5.43 pIC50 3751 nM IC50 Eur J Med Chem (2019) 163: 413-427 [PMID:30530193]
GtoPdb - - 6.3 pIC50 >500 nM IC50 WO2011008487. Pyrimidinones as PI3K inhibitors (2011)

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]