AZD3458 [Ligand Id: 9997] 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: CHEMBL4126156
There should be some charts here, you may need to enable JavaScript!
  • phosphatidylinositol 3-kinase catalytic subunit type 3/Phosphatidylinositol 3-kinase catalytic subunit type 3 in Human [ChEMBL: CHEMBL1075165] [GtoPdb: 2152] [UniProtKB: Q8NEB9]
There should be some charts here, you may need to enable JavaScript!
  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma in Human [GtoPdb: 2156] [UniProtKB: P48736]
  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform in Mouse [ChEMBL: CHEMBL2189158] [GtoPdb: 2156] [UniProtKB: Q9JHG7]
There should be some charts here, you may need to enable JavaScript!
  • phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 beta/Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing beta polypeptide in Human [ChEMBL: CHEMBL5554] [GtoPdb: 2151] [UniProtKB: O00750]
There should be some charts here, you may need to enable JavaScript!
  • phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 alpha/Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing subunit alpha in Human [ChEMBL: CHEMBL1075102] [GtoPdb: 2150] [UniProtKB: O00443]
There should be some charts here, you may need to enable JavaScript!
  • phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 gamma/Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing subunit gamma in Human [ChEMBL: CHEMBL1163120] [GtoPdb: 2288] [UniProtKB: O75747]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/PI3-kinase p110-delta subunit in Human [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329]
There should be some charts here, you may need to enable JavaScript!
  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/PI3-kinase p110-gamma subunit in Human [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736]
There should be some charts here, you may need to enable JavaScript!
  • P2Y1 receptor/Purinergic receptor P2Y1 in Human [ChEMBL: CHEMBL4315] [GtoPdb: 323] [UniProtKB: P47900]
There should be some charts here, you may need to enable JavaScript!
  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha in Human [GtoPdb: 2153] [UniProtKB: P42336]
There should be some charts here, you may need to enable JavaScript!
  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta in Human [GtoPdb: 2154] [UniProtKB: P42338]
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
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG B 4.5 pIC50 31622.78 nM IC50 J Med Chem (2018) 61: 5435-5441 [PMID:29852070]
phosphatidylinositol 3-kinase catalytic subunit type 3/Phosphatidylinositol 3-kinase catalytic subunit type 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075165] [GtoPdb: 2152] [UniProtKB: Q8NEB9]
ChEMBL Inhibition of PI3KC3 (unknown origin) B 5.1 pIC50 7943.28 nM IC50 J Med Chem (2018) 61: 5435-5441 [PMID:29852070]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma in Human [GtoPdb: 2156] [UniProtKB: P48736]
GtoPdb In a biochemical enzyme activity assay. - 9.1 pIC50 0.79 nM IC50 J Med Chem (2018) 61: 5435-5441 [PMID:29852070]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189158] [GtoPdb: 2156] [UniProtKB: Q9JHG7]
ChEMBL Inhibition of PI3Kgamma in mouse RAW264 cells assessed as reduction in Akt phosphorylation at Ser473 residue preincubated for 15 mins followed by C5a stimulation measured after 3 mins by TR-FRET assay B 8.1 pIC50 7.94 nM IC50 J Med Chem (2018) 61: 5435-5441 [PMID:29852070]
phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 beta/Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing beta polypeptide in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5554] [GtoPdb: 2151] [UniProtKB: O00750]
ChEMBL Inhibition of PI3KC2beta (unknown origin) B 7.5 pIC50 31.62 nM IC50 J Med Chem (2018) 61: 5435-5441 [PMID:29852070]
phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 alpha/Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075102] [GtoPdb: 2150] [UniProtKB: O00443]
ChEMBL Inhibition of PI3KC2alpha (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2018) 61: 5435-5441 [PMID:29852070]
phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 gamma/Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing subunit gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163120] [GtoPdb: 2288] [UniProtKB: O75747]
ChEMBL Inhibition of PI3KC2gamma (unknown origin) B 5.5 pIC50 3162.28 nM IC50 J Med Chem (2018) 61: 5435-5441 [PMID:29852070]
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]
ChEMBL Inhibition of recombinant human 6His-tagged PI3K p110delta/p85alpha using DiC8-PIP2 as substrate preincubated for 10 mins followed by substrate addition measured after 60 mins by ADP-Glo assay B 6.5 pIC50 316.23 nM IC50 J Med Chem (2018) 61: 5435-5441 [PMID:29852070]
GtoPdb In a biochemical enzyme activity assay. - 6.5 pIC50 316 nM IC50 J Med Chem (2018) 61: 5435-5441 [PMID:29852070]
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 in human JeKo1B cells assessed as reduction in AKT phosphorylation at ser473 residue preincubated for 60 mins followed by anti-IgM stimulation measured after 10 mins by TR-FRET assay B 6 pIC50 1000 nM IC50 J Med Chem (2018) 61: 5435-5441 [PMID:29852070]
GtoPdb In a biochemical enzyme activity assay. - 6.5 pIC50 316 nM IC50 J Med Chem (2018) 61: 5435-5441 [PMID:29852070]
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 biochemical enzyme activity assay. - 9.1 pIC50 0.79 nM IC50 J Med Chem (2018) 61: 5435-5441 [PMID:29852070]
ChEMBL Inhibition of recombinant human 6His-tagged PI3Kgamma (144 to 1102 residues) using DiC8-PIP2 as substrate preincubated for 10 mins followed by substrate addition measured after 60 mins by ADP-Glo assay B 9.1 pIC50 <=0.79 nM IC50 J Med Chem (2018) 61: 5435-5441 [PMID:29852070]
P2Y1 receptor/Purinergic receptor P2Y1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4315] [GtoPdb: 323] [UniProtKB: P47900]
ChEMBL Binding affinity to human P2Y1 receptor B 6 pKi <1000 nM Ki J Med Chem (2018) 61: 5435-5441 [PMID:29852070]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha in Human [GtoPdb: 2153] [UniProtKB: P42336]
GtoPdb In a biochemical enzyme activity assay. - 5.1 pIC50 7943 nM IC50 J Med Chem (2018) 61: 5435-5441 [PMID:29852070]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta in Human [GtoPdb: 2154] [UniProtKB: P42338]
GtoPdb In a biochemical enzyme activity assay. - 4.5 pIC50 >31600 nM IC50 J Med Chem (2018) 61: 5435-5441 [PMID:29852070]

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]