PI 3-Kg inhibitor [Ligand Id: 6023] 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: CHEMBL568150 (AS-605240)
  • casein kinase 2, alpha prime polypeptide subunit/casein kinase 2, beta polypeptide subunit/casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II in Human [ChEMBL: CHEMBL2095191] [GtoPdb: 1550, 1551, 1549] [UniProtKB: P19784, P67870, P68400]
There should be some charts here, you may need to enable JavaScript!
  • CDGSH iron-sulfur domain-containing protein 1 in Human [ChEMBL: CHEMBL1795168] [UniProtKB: Q9NZ45]
There should be some charts here, you may need to enable JavaScript!
  • CDC like kinase 1/Dual specificity protein kinase CLK1 in Human [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759]
There should be some charts here, you may need to enable JavaScript!
  • dual specificity tyrosine phosphorylation regulated kinase 1A/Dual-specificity tyrosine-phosphorylation regulated kinase 1A in Human [ChEMBL: CHEMBL2292] [GtoPdb: 2009] [UniProtKB: Q13627]
There should be some charts here, you may need to enable JavaScript!
  • dual specificity tyrosine phosphorylation regulated kinase 1B/Dual specificity tyrosine-phosphorylation-regulated kinase 1B in Human [ChEMBL: CHEMBL5543] [GtoPdb: 2010] [UniProtKB: Q9Y463]
There should be some charts here, you may need to enable JavaScript!
  • dual specificity tyrosine phosphorylation regulated kinase 2/Dual-specificity tyrosine-phosphorylation regulated kinase 2 in Human [ChEMBL: CHEMBL4376] [GtoPdb: 2011] [UniProtKB: Q92630]
There should be some charts here, you may need to enable JavaScript!
  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • 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/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
casein kinase 2, alpha prime polypeptide subunit/casein kinase 2, beta polypeptide subunit/casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2095191] [GtoPdb: 1550, 1551, 1549] [UniProtKB: P19784, P67870, P68400]
ChEMBL Inhibition of CK2 (unknown origin) using RRRDDDSDDD-NH2 as susbtrate incubated for 15 mins in presence of [gamma-32P]ATP B 7.7 pIC50 20 nM IC50 Eur J Med Chem (2016) 112: 209-216 [PMID:26896709]
CDGSH iron-sulfur domain-containing protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795168] [UniProtKB: Q9NZ45]
ChEMBL Displacement of [3H]-rosiglitazone from human recombinant C-terminal His-tagged cytosolic domain of mitoNEET (32-108) by scintillation proximity assay B 5.49 pIC50 3260 nM IC50 Bioorg Med Chem Lett (2011) 21: 5498-5501 [PMID:21782425]
CDC like kinase 1/Dual specificity protein kinase CLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759]
ChEMBL Inhibition of recombinant human GST-tagged CLK1 catalytic domain (129 to 484 residues) expressed in Escherichia coli using GRSRSRSRSRSRSRSR as substrate incubated for 15 mins in presence of [gamma-32P]ATP B 7.15 pIC50 70 nM IC50 Eur J Med Chem (2016) 112: 209-216 [PMID:26896709]
dual specificity tyrosine phosphorylation regulated kinase 1A/Dual-specificity tyrosine-phosphorylation regulated kinase 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2292] [GtoPdb: 2009] [UniProtKB: Q13627]
ChEMBL Inhibition of tetracycline-inducible EGFP-DYRK1A (unknown origin) expressed in HEK293 cells coexpressing full length human EGFP-tau protein assessed as reduction in tau-Thr212 phosphorylation incubated overnight by immunofluorescence assay B 5.8 pIC50 1600 nM IC50 Eur J Med Chem (2016) 112: 209-216 [PMID:26896709]
ChEMBL Inhibition of recombinant human N-terminal His6-tagged DYRK1A catalytic domain expressed in Escherichia coli BL21(DE3) cells using KKISGRLSPIMTEQ-NH2 as substrate incubated for 15 mins in presence of [gamma-32P]ATP B 7.52 pIC50 30 nM IC50 Eur J Med Chem (2016) 112: 209-216 [PMID:26896709]
dual specificity tyrosine phosphorylation regulated kinase 1B/Dual specificity tyrosine-phosphorylation-regulated kinase 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5543] [GtoPdb: 2010] [UniProtKB: Q9Y463]
ChEMBL Inhibition of full length recombinant human GST-tagged DYRK1B expressed in insect cells using KKISGRLSPIMTEQ-NH2 as substrate incubated for 15 mins in presence of [gamma-32P]ATP B 7.1 pIC50 80 nM IC50 Eur J Med Chem (2016) 112: 209-216 [PMID:26896709]
dual specificity tyrosine phosphorylation regulated kinase 2/Dual-specificity tyrosine-phosphorylation regulated kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4376] [GtoPdb: 2011] [UniProtKB: Q92630]
ChEMBL Inhibition of recombinant human N-terminal GST-tagged DYRK2 expressed in Escherichia coli BL21(DE3) cells using KKISGRLSPIMTEQ-NH2 as substrate incubated for 15 mins in presence of [gamma-32P]ATP B 7 pIC50 100 nM IC50 Eur J Med Chem (2016) 112: 209-216 [PMID:26896709]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibition of EGFR (unknown origin) incubated for 15 mins in presence of [gamma-32P]ATP B 5 pIC50 >10000 nM IC50 Eur J Med Chem (2016) 112: 209-216 [PMID:26896709]
Monoamine oxidase B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2039] [GtoPdb: 2490] [UniProtKB: P27338]
ChEMBL Inhibition of human recombinant MAO-B after 15 mins B 4.89 pIC50 13000 nM IC50 Bioorg Med Chem Lett (2010) 20: 5295-5298 [PMID:20650633]
ChEMBL Inhibition of human recombinant MAOB by amplex red assay B 4.89 pIC50 13000 nM IC50 Bioorg Med Chem Lett (2011) 21: 4798-4803 [PMID:21742494]
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 - - 7.22 pIC50 60 nM IC50 Nat Med (2005) 11: 936-43 [PMID:16127437]
ChEMBL Inhibition of PI3Kalpha (unknown origin) by lipid kinase assay B 7.22 pIC50 60 nM IC50 Medchemcomm (2012) 3: 1337-1355
ChEMBL Inhibition of PI3Kalpha (unknown origin) B 7.22 pIC50 60 nM IC50 Eur J Med Chem (2019) 163: 413-427 [PMID:30530193]
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 5.57 pIC50 2700 nM IC50 Eur J Med Chem (2019) 163: 413-427 [PMID:30530193]
ChEMBL Inhibition of PI3Kbeta (unknown origin) by lipid kinase assay B 6.57 pIC50 270 nM IC50 Medchemcomm (2012) 3: 1337-1355
GtoPdb - - 6.57 pIC50 270 nM IC50 Nat Med (2005) 11: 936-43 [PMID:16127437]
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 - - 6.52 pIC50 300 nM IC50 Nat Med (2005) 11: 936-43 [PMID:16127437]
ChEMBL Inhibition of PI3Kdelta (unknown origin) by lipid kinase assay B 6.52 pIC50 300 nM IC50 Medchemcomm (2012) 3: 1337-1355
ChEMBL Inhibition of PI3Kdelta (unknown origin) B 6.52 pIC50 300 nM IC50 Eur J Med Chem (2019) 163: 413-427 [PMID:30530193]
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 human recombinant GST-tagged PI3Kgamma incubated for 180 mins using [33P]gamma-ATP by scintillation proximity assay B 8.05 pIC50 9 nM IC50 Bioorg Med Chem (2015) 23: 2953-2974 [PMID:25890697]
ChEMBL Inhibition of PI3Kgamma (unknown origin) by lipid kinase assay B 8.1 pIC50 8 nM IC50 Medchemcomm (2012) 3: 1337-1355
ChEMBL Inhibition of human recombinant N-terminal GST-tagged PI3K-gamma (39 to 1102 residues) expressed n baculovirus infected TN5 cells using phosphatidylinositol as substrate by scintillation proximity assay in presence of {33P]gammaATP B 8.1 pIC50 8 nM IC50 Eur J Med Chem (2016) 112: 209-216 [PMID:26896709]
ChEMBL Inhibition of PI3Kgamma (unknown origin) B 8.1 pIC50 8 nM IC50 Eur J Med Chem (2019) 163: 413-427 [PMID:30530193]
ChEMBL Inhibition of human recombinant PI3Kgamma using phosphatidylinositol as substrate in presence of [gamma33P]ATP by scintillation proximity assay B 8.1 pIC50 8 nM IC50 Eur J Med Chem (2023) 246: 114971-114971 [PMID:36462440]
GtoPdb - - 8.1 pIC50 8 nM IC50 Nat Med (2005) 11: 936-43 [PMID:16127437]

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]