nemiralisib [Ligand Id: 9425] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2216859 (GSK-2269557 FREE BASE, GSK2269557A, GSK-2269557A, GSK-2269557, Nemiralisib)
  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha subunit in Human [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336]
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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]
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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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  • Kv11.1 in Human [GtoPdb: 572] [UniProtKB: Q12809]
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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]
GtoPdb In a homogeneous time-resolved fluorescence (HTRF) assay - 5.3 pIC50 5011 nM IC50 J Med Chem (2015) 58: 7381-99 [PMID:26301626]
ChEMBL Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by HTRF method B 5.3 pIC50 5011.87 nM IC50 J Med Chem (2018) 61: 11061-11073 [PMID:30532965]
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 In a homogeneous time-resolved fluorescence (HTRF) assay - 5.8 pIC50 1584 nM IC50 J Med Chem (2015) 58: 7381-99 [PMID:26301626]
ChEMBL Inhibition of PI3Kbeta (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by HTRF method B 5.8 pIC50 1584.89 nM IC50 J Med Chem (2018) 61: 11061-11073 [PMID:30532965]
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]
ChEMBL Inhibition of PI3Kdelta (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by HTRF method B 9.9 pKi 0.13 nM Ki J Med Chem (2018) 61: 11061-11073 [PMID:30532965]
ChEMBL Inhibition of PI3Kdelta B 7 pIC50 <100 nM IC50 J. Med. Chem. (2012) 55: 8559-8581 [PMID:22924688]
GtoPdb In a homogeneous time-resolved fluorescence (HTRF) assay in the presence of 2mM ATP. - 9.9 pIC50 0.13 nM IC50 J Med Chem (2015) 58: 7381-99 [PMID:26301626]
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 In a homogeneous time-resolved fluorescence (HTRF) assay - 5.2 pIC50 6310 nM IC50 J Med Chem (2015) 58: 7381-99 [PMID:26301626]
ChEMBL Inhibition of PI3Kgamma (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by HTRF method B 5.2 pIC50 6309.57 nM IC50 J Med Chem (2018) 61: 11061-11073 [PMID:30532965]
Kv11.1 in Human [GtoPdb: 572] [UniProtKB: Q12809]
GtoPdb - - 5.5 pIC50 3162 nM IC50 J Med Chem (2015) 58: 7381-99 [PMID:26301626]

ChEMBL data shown on this page come from version 28:

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]