amdizalisib [Ligand Id: 11699] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4438249 (Amdizalisib, Hmpl-689, HMPL-689)
  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/phosphoinositide-3-kinase regulatory subunit 1/PI3-kinase p110-delta/p85-alpha in Human [ChEMBL: CHEMBL2111432] [GtoPdb: 21552503] [UniProtKB: O00329P27986]
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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-4,5-bisphosphate 3-kinase catalytic subunit beta in Human [GtoPdb: 2154] [UniProtKB: P42338]
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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 delta/phosphoinositide-3-kinase regulatory subunit 1/PI3-kinase p110-delta/p85-alpha in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111432] [GtoPdb: 21552503] [UniProtKB: O00329P27986]
GtoPdb - - 9.52 pIC50 0.3 nM IC50 WO2016045591A1. Novel imidazopyridazine compounds and their use (2016)
ChEMBL Inhibition of N-terminal His6-tagged recombinant full length human p110delta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells after 80 mins by fluorescence polarization assay B 9.52 pIC50 0.3 nM IC50 J Med Chem (2019) 62: 4783-4814 [PMID:30582813]
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]
GtoPdb - - 7.42 pIC50 38 nM IC50 WO2016045591A1. Novel imidazopyridazine compounds and their use (2016)
ChEMBL Inhibition of recombinant N-terminal His-tagged full length human PI3Kgamma expressed in baculovirus expression system after 80 mins by fluorescence polarization assay B 7.42 pIC50 38 nM IC50 J Med Chem (2019) 62: 4783-4814 [PMID:30582813]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta in Human [GtoPdb: 2154] [UniProtKB: P42338]
GtoPdb - - 7.06 pIC50 87 nM IC50 WO2016045591A1. Novel imidazopyridazine compounds and their use (2016)

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]