AS-252424 [Ligand Id: 10578] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL379156
  • 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]
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  • mitogen-activated protein kinase kinase 7/Dual specificity mitogen-activated protein kinase kinase 7 in Human [ChEMBL: CHEMBL3530] [GtoPdb: 2068] [UniProtKB: O14733]
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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]
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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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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 human CK2 B 7.7 pIC50 20 nM IC50 J. Med. Chem. (2006) 49: 3857-3871 [PMID:16789742]
mitogen-activated protein kinase kinase 7/Dual specificity mitogen-activated protein kinase kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3530] [GtoPdb: 2068] [UniProtKB: O14733]
ChEMBL Inhibition of human MKK7beta B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2006) 49: 3857-3871 [PMID:16789742]
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 human PI3Kalpha B 6.03 pIC50 940 nM IC50 J. Med. Chem. (2006) 49: 3857-3871 [PMID:16789742]
ChEMBL Inhibition of PI3Kalpha (unknown origin) by lipid kinase assay B 6.03 pIC50 940 nM IC50 MedChemComm (2012) 3: 1337-1355
GtoPdb - - 6.03 pIC50 935 nM IC50 J. Med. Chem. (2006) 49: 3857-71 [PMID:16789742]
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 human PI3Kbeta B 4.7 pIC50 20000 nM IC50 J. Med. Chem. (2006) 49: 3857-3871 [PMID:16789742]
ChEMBL Inhibition of PI3Kbeta (unknown origin) by lipid kinase assay B 4.7 pIC50 20000 nM IC50 MedChemComm (2012) 3: 1337-1355
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 human PI3Kdelta B 4.7 pIC50 20000 nM IC50 J. Med. Chem. (2006) 49: 3857-3871 [PMID:16789742]
ChEMBL Inhibition of PI3Kdelta (unknown origin) by lipid kinase assay B 4.7 pIC50 20000 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]
GtoPdb - - 7.48 pIC50 33 nM IC50 J. Med. Chem. (2006) 49: 3857-71 [PMID:16789742]
ChEMBL Inhibition of PI3Kgamma (unknown origin) assessed as decrease in fluorescence intensity using phosphorylated substrate B 7.48 pIC50 33 nM IC50 Eur. J. Med. Chem. (2014) 84: 454-465 [PMID:25050878]
ChEMBL Inhibition of human PI3Kgamma B 7.52 pIC50 30 nM IC50 J. Med. Chem. (2006) 49: 3857-3871 [PMID:16789742]
ChEMBL Inhibition of recombinant human PI3Kgamma by HTRF assay B 7.52 pIC50 30 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 6586-6590 [PMID:21925880]
ChEMBL Inhibition of PI3Kgamma (unknown origin) by lipid kinase assay B 7.52 pIC50 30 nM IC50 MedChemComm (2012) 3: 1337-1355

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]