SAR405 [Ligand Id: 9353] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3622372
  • 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-phosphate 3-kinase catalytic subunit type 2 gamma/Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing subunit gamma in Human [ChEMBL: CHEMBL1163120] [GtoPdb: 2288] [UniProtKB: O75747]
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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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  • mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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]
GtoPdb - - 8.82 pKd 1.52 nM Kd Nat Chem Biol (2014) 10: 1013-9 [PMID:25326666]
ChEMBL Inhibition of Vps34 in human HeLa cells expressing GFP-FYVE B 7.57 pIC50 27 nM IC50 J Med Chem (2018) 61: 4656-4687 [PMID:29211480]
ChEMBL Inhibition of recombinant human Vps34 by TR-FRET analysis B 8.92 pIC50 1.2 nM IC50 J Med Chem (2015) 58: 7611-7633 [PMID:26086931]
ChEMBL Inhibition of Vps34 (unknown origin) B 8.92 pIC50 1.2 nM IC50 J Med Chem (2017) 60: 47-65 [PMID:27644332]
ChEMBL Inhibition of Vps34 (unknown origin) B 8.92 pIC50 1.2 nM IC50 J Med Chem (2018) 61: 4656-4687 [PMID:29211480]
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) B 5 pIC50 >10000 nM IC50 J Med Chem (2017) 60: 47-65 [PMID:27644332]
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 PI3KC2alpha (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2017) 60: 47-65 [PMID:27644332]
phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 gamma/Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing subunit gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163120] [GtoPdb: 2288] [UniProtKB: O75747]
ChEMBL Inhibition of PI3KC2gamma (unknown origin) B 5 pIC50 >10000 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 recombinant human PI3Kalpha by TR-FRET analysis B 5 pIC50 >10000 nM IC50 J Med Chem (2015) 58: 7611-7633 [PMID:26086931]
ChEMBL Inhibition of PI3K p110alpha (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2018) 61: 4656-4687 [PMID:29211480]
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 recombinant human PI3Kbeta by TR-FRET analysis B 5 pIC50 >10000 nM IC50 J Med Chem (2015) 58: 7611-7633 [PMID:26086931]
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 recombinant human PI3Kdelta by TR-FRET analysis B 5 pIC50 >10000 nM IC50 J Med Chem (2015) 58: 7611-7633 [PMID:26086931]
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 recombinant human PI3Kgamma by TR-FRET analysis B 5 pIC50 >10000 nM IC50 J Med Chem (2015) 58: 7611-7633 [PMID:26086931]
mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345]
ChEMBL Inhibition of recombinant human mTOR by TR-FRET analysis B 5 pIC50 >10000 nM IC50 J Med Chem (2015) 58: 7611-7633 [PMID:26086931]

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]