IC-87114 [Ligand Id: 9376] 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: CHEMBL1213082
  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha subunit in Human [ChEMBL: CHEMBL4005] [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/PI3-kinase p110-beta subunit in Human [ChEMBL: CHEMBL3145] [GtoPdb: 2154] [UniProtKB: P42338]
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!
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 4 pIC50 >100000 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 4.12 pIC50 75000 nM IC50 Medchemcomm (2012) 3: 1337-1355
ChEMBL Inhibition of p110beta B 4.8 pIC50 16000 nM IC50 Nat Chem Biol (2010) 6: 117-124 [PMID:20081827]
ChEMBL Inhibition of PI3Kbeta in presence of 10 uM ATP B 4.8 pIC50 16000 nM IC50 J Med Chem (2012) 55: 8559-8581 [PMID:22924688]
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 - - 7.7 pKi ~20 nM Ki Chem Biol (2005) 12: 621-37 [PMID:15975507]
ChEMBL Inhibition of human recombinant full length N-terminal His6-tagged PI3K p110delta/p85alpha expressed in baculovirus infected Sf9 insect cells using PI:PS as substrate after 60 mins by ADP-Glo assay B 7.7 pKi 19.95 nM Ki J Med Chem (2017) 60: 4304-4315 [PMID:28489362]
ChEMBL Inhibition of human recombinant full length N-terminal His6-tagged PI3K p110delta/p85alpha expressed in baculovirus infected Sf9 insect cells using PI:PS as substrate after 60 mins by ADP-Glo assay B 7.9 pKi 12.59 nM Ki J Med Chem (2017) 60: 4304-4315 [PMID:28489362]
GtoPdb - - 6.3 pIC50 500 nM IC50 J Immunol (2003) 170: 2647-54 [PMID:12594293]
ChEMBL Inhibition of full length recombinant human N-terminal His6-tagged PI3K p110delta/human p85alpha expressed in baculovirus infected sf21 cells using PIP2 as substrate preincubated for 30 mins followed by substrate addition by HTRF assay B 6.89 pIC50 130 nM IC50 ACS Med Chem Lett (2017) 8: 118-123 [PMID:28105286]
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 p110delta B 7.7 pKi 20 nM Ki Chem Biol (2005) 12: 621-637 [PMID:15975507]
GtoPdb - - 7.7 pKi ~20 nM Ki Chem Biol (2005) 12: 621-37 [PMID:15975507]
GtoPdb - - 6.3 pIC50 500 nM IC50 J Immunol (2003) 170: 2647-54 [PMID:12594293]
ChEMBL Inhibition of PI3Kdelta (unknown origin) B 6.3 pIC50 500 nM IC50 Medchemcomm (2012) 3: 1337-1355
ChEMBL Inhibition of PI3Kdelta in presence of 200 uM ATP B 6.3 pIC50 500 nM IC50 J Med Chem (2012) 55: 8559-8581 [PMID:22924688]
ChEMBL Inhibition of PI3K-delta (unknown origin) by cell free biochemical assay B 6.8 pIC50 160 nM IC50 Bioorg Med Chem Lett (2018) 28: 1005-1010 [PMID:29486969]
ChEMBL Inhibition of p110delta B 6.89 pIC50 130 nM IC50 Nat Chem Biol (2010) 6: 117-124 [PMID:20081827]
ChEMBL Inhibition of PI3Kdelta in presence of 10 uM ATP B 6.89 pIC50 130 nM IC50 J Med Chem (2012) 55: 8559-8581 [PMID:22924688]
ChEMBL Inhibition of PI3K-delta (unknown origin) expressed in baculovirus infected Sf9 insect cells after 10 mins in presence of [gamma-32P]ATP by radioligand binding assay B 6.89 pIC50 130 nM IC50 Bioorg Med Chem Lett (2018) 28: 1005-1010 [PMID:29486969]
ChEMBL Inhibition of PI3Kdelta in human PBMC assessed as reduction in anti-human CD28 antibody stimulated IL-6 secretion levels after 72 hrs by ELISA B 7.3 pIC50 50.12 nM IC50 J Med Chem (2017) 60: 4304-4315 [PMID:28489362]
ChEMBL Inhibition of PI3Kdelta in human PBMC assessed as reduction in anti-human CD28 antibody stimulated IL-6 secretion levels after 72 hrs by ELISA B 7.6 pIC50 25.12 nM IC50 J Med Chem (2017) 60: 4304-4315 [PMID:28489362]
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 PI3K-gamma (unknown origin) by cell free biochemical assay B 4.15 pIC50 70000 nM IC50 Bioorg Med Chem Lett (2018) 28: 1005-1010 [PMID:29486969]
ChEMBL Inhibition of p110gamma B 4.21 pIC50 61000 nM IC50 Nat Chem Biol (2010) 6: 117-124 [PMID:20081827]
ChEMBL Inhibition of PI3Kgamma in presence of 10 uM ATP B 4.21 pIC50 61000 nM IC50 J Med Chem (2012) 55: 8559-8581 [PMID:22924688]
ChEMBL Inhibition of PI3Kgamma (unknown origin) B 4.54 pIC50 29000 nM IC50 Medchemcomm (2012) 3: 1337-1355

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]