PIK-93 [Ligand Id: 6062] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1229535
  • protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase in Human [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527]
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  • phosphatidylinositol 3-kinase catalytic subunit type 3/Phosphatidylinositol 3-kinase catalytic subunit type 3 in Human [ChEMBL: CHEMBL1075165] [GtoPdb: 2152] [UniProtKB: Q8NEB9]
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  • 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]
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  • 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]
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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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  • phosphatidylinositol 4-kinase alpha/PI4-kinase alpha subunit in Human [ChEMBL: CHEMBL3667] [GtoPdb: 2148] [UniProtKB: P42356]
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  • phosphatidylinositol 4-kinase beta/PI4-kinase beta subunit in Human [ChEMBL: CHEMBL3268] [GtoPdb: 2149] [UniProtKB: Q9UBF8]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527]
ChEMBL Inhibition of human DNA-PK by non-radiometric ADP-Glo assay B 7.19 pIC50 64 nM IC50 ACS Med Chem Lett (2015) 6: 3-6 [PMID:25589915]
ChEMBL Inhibition of DNA-PK (unknown origin) B 7.19 pIC50 64 nM IC50 J Med Chem (2017) 60: 47-65 [PMID:27644332]
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 full length human recombinant VPS34 (unknown origin) using phosphatidylinositol and gamma-32P-ATP incubated for 20 mins by TLC assay or high-throughput membrane capture assay B 6.49 pIC50 320 nM IC50 J Med Chem (2017) 60: 47-65 [PMID:27644332]
ChEMBL Inhibition of GST-tagged recombinant human full length VPS34 expressed in baculovirus preincubated for 15 mins followed by addition of cold ATP/gamma32P-ATP measured after 1 hr in presence of MnCl2 B 6.51 pIC50 307 nM IC50 J Med Chem (2016) 59: 1830-1839 [PMID:26885694]
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) expressed in HEK293 cells using phosphatidylinositol and gamma-32P-ATP incubated for 20 mins by TLC assay or high-throughput membrane capture assay B 4.85 pIC50 14000 nM IC50 J Med Chem (2017) 60: 47-65 [PMID:27644332]
ChEMBL Inhibition of human PI3KC2beta by non-radiometric ADP-Glo assay B 6.85 pIC50 140 nM IC50 ACS Med Chem Lett (2015) 6: 3-6 [PMID:25589915]
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 human PI3KC2alpha by non-radiometric ADP-Glo assay B 4.8 pIC50 16000 nM IC50 ACS Med Chem Lett (2015) 6: 3-6 [PMID:25589915]
ChEMBL Inhibition of PI3KC2alpha (unknown origin) expressed in HEK293 cells using phosphatidylinositol and gamma-32P-ATP incubated for 20 mins by TLC assay or high-throughput membrane capture assay B 4.8 pIC50 16000 nM IC50 J Med Chem (2017) 60: 47-65 [PMID:27644332]
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 7.41 pIC50 39 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 6.23 pIC50 590 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 PI3Kdelta (unknown origin) B 6.92 pIC50 120 nM IC50 Medchemcomm (2012) 3: 1337-1355
ChEMBL Inhibition of histidine-tagged recombinant human full length PI3Kdelta expressed in baculovirus preincubated for 15 mins followed by addition of cold ATP/gamma32P-ATP measured after 20 mins in presence of MgCl2 B 7.11 pIC50 77 nM IC50 J Med Chem (2016) 59: 1830-1839 [PMID:26885694]
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) B 8.15 pKi 7 nM Ki J Med Chem (2015) 58: 517-521 [PMID:24754609]
ChEMBL Inhibition of histidine-tagged recombinant human full length PI3Kgamma expressed in insect cells preincubated for 15 mins followed by addition of cold ATP/gamma32P-ATP measured after 15 mins in presence of MgCl2 B 7.77 pIC50 17 nM IC50 J Med Chem (2016) 59: 1830-1839 [PMID:26885694]
ChEMBL Inhibition of PI3Kgamma (unknown origin) B 7.8 pIC50 16 nM IC50 Medchemcomm (2012) 3: 1337-1355
ChEMBL Inhibition of human PI3KCgamma by non-radiometric ADP-Glo assay B 7.8 pIC50 16 nM IC50 ACS Med Chem Lett (2015) 6: 3-6 [PMID:25589915]
ChEMBL Inhibition of PI3Kgamma (unknown origin) using phosphatidylinositol and gamma-32P-ATP incubated for 20 mins by TLC assay or high-throughput membrane capture assay B 7.8 pIC50 16 nM IC50 J Med Chem (2017) 60: 47-65 [PMID:27644332]
phosphatidylinositol 4-kinase alpha/PI4-kinase alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3667] [GtoPdb: 2148] [UniProtKB: P42356]
ChEMBL Inhibition of PI4K3alpha (unknown origin) B 5.96 pIC50 1100 nM IC50 J Med Chem (2018) 61: 6705-6723 [PMID:29952567]
phosphatidylinositol 4-kinase beta/PI4-kinase beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3268] [GtoPdb: 2149] [UniProtKB: Q9UBF8]
ChEMBL Inhibition of PI4K3beta in human PBMC assessed as reduction in mitomycin-C treated human RPMI1788 cells-stimulated lymphocyte proliferation by measuring reduction in [3H]thymidine incorporation preincubated for 5 days followed by [3H]thymidine addition measured after 18 hrs by liquid scintillation counting method B 7.55 pIC50 28 nM IC50 J Med Chem (2018) 61: 6705-6723 [PMID:29952567]
GtoPdb - - 7.72 pIC50 19 nM IC50 Cell (2006) 125: 733-47 [PMID:16647110];
Mol Biol Cell (2008) 19: 711-21 [PMID:18077555]
ChEMBL Inhibition of PI4K3beta (unknown origin) B 7.72 pIC50 19 nM IC50 J Med Chem (2018) 61: 6705-6723 [PMID:29952567]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]