PI 3-Kg inhibitor [Ligand Id: 6023] activity data from GtoPdb and ChEMBL

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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: 155015511549] [UniProtKB: P19784P67870P68400]
  • This target only has 0 pki data point
1 CHEMBL568150_lig_chart_1 Casein kinase II Human
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  • CDGSH iron-sulfur domain-containing protein 1 in Human [ChEMBL: CHEMBL1795168] [UniProtKB: Q9NZ45]
  • This target only has 0 pki data point
2 CHEMBL568150_lig_chart_2 CDGSH iron-sulfur domain-containing protein 1 Human
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  • dual specificity tyrosine phosphorylation regulated kinase 1A/Dual-specificity tyrosine-phosphorylation regulated kinase 1A in Human [ChEMBL: CHEMBL2292] [GtoPdb: 2009] [UniProtKB: Q13627]
  • This target only has 0 pki data point
3 CHEMBL568150_lig_chart_3 Dual-specificity tyrosine-phosphorylation regulated kinase 1A Human
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  • dual specificity tyrosine phosphorylation regulated kinase 1B/Dual specificity tyrosine-phosphorylation-regulated kinase 1B in Human [ChEMBL: CHEMBL5543] [GtoPdb: 2010] [UniProtKB: Q9Y463]
  • This target only has 0 pki data point
4 CHEMBL568150_lig_chart_4 Dual specificity tyrosine-phosphorylation-regulated kinase 1B Human
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  • dual specificity tyrosine phosphorylation regulated kinase 2/Dual-specificity tyrosine-phosphorylation regulated kinase 2 in Human [ChEMBL: CHEMBL4376] [GtoPdb: 2011] [UniProtKB: Q92630]
  • This target only has 0 pki data point
5 CHEMBL568150_lig_chart_5 Dual-specificity tyrosine-phosphorylation regulated kinase 2 Human
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  • CDC like kinase 1/Dual specificty protein kinase CLK1 in Human [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759]
  • This target only has 0 pki data point
6 CHEMBL568150_lig_chart_6 Dual specificty protein kinase CLK1 Human
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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
  • This target only has 0 pki data point
7 CHEMBL568150_lig_chart_7 Epidermal growth factor receptor erbB1 Human
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  • Monoamine oxidase B in Human [ChEMBL: CHEMBL2039] [GtoPdb: 2490] [UniProtKB: P27338]
  • This target only has 0 pki data point
8 CHEMBL568150_lig_chart_8 Monoamine oxidase B Human
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha subunit in Human [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336]
  • This target only has 0 pki data point
9 CHEMBL568150_lig_chart_9 PI3-kinase p110-alpha subunit Human
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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]
  • This target only has 0 pki data point
10 CHEMBL568150_lig_chart_10 PI3-kinase p110-beta subunit Human
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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]
  • This target only has 0 pki data point
11 CHEMBL568150_lig_chart_11 PI3-kinase p110-delta subunit Human
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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]
  • This target only has 0 pki data point
12 CHEMBL568150_lig_chart_12 PI3-kinase p110-gamma subunit Human
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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: 155015511549] [UniProtKB: P19784P67870P68400]
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]
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]
CDC like kinase 1/Dual specificty 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]
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
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) 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
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]
GtoPdb - - 8.1 pIC50 8 nM IC50 Nat. Med. (2005) 11: 936-43 [PMID:16127437]

ChEMBL data shown on this page come from version 27:

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]