taselisib [Ligand Id: 7794] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2387080 (GDC-0032, RG-7604, Taselisib)
  • 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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  • 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
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 DNA-dependent protein kinase (unknown origin) B 5.32 pIC50 >4800 nM IC50 J Med Chem (2013) 56: 4597-4610 [PMID:23662903]
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 human VPS34 B 6.43 pIC50 374 nM IC50 J Med Chem (2013) 56: 4597-4610 [PMID:23662903]
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 6.53 pIC50 292 nM IC50 J Med Chem (2013) 56: 4597-4610 [PMID:23662903]
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 (2013) 56: 4597-4610 [PMID:23662903]
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 PI3K alpha (unknown origin) using PIP2 as substrate by fluorescence polarization assay B 9.52 pKi 0.3 nM Ki J Med Chem (2016) 59: 985-1002 [PMID:26741947]
ChEMBL Inhibition of PI3Kalpha (unknown origin) assessed as 3,4,5-inositoltriphosphate formation after 30 mins by fluorescence polarization assay B 9.54 pKi 0.29 nM Ki J Med Chem (2013) 56: 4597-4610 [PMID:23662903]
GtoPdb - - 9.54 pKi 0.29 nM Ki J Med Chem (2013) 56: 4597-610 [PMID:23662903]
GtoPdb - - 10.05 pKi 0.09 nM Ki US20170015678. Benzoxazepin oxazolidinone compounds and methods of use (2017)
ChEMBL Inhibition of PI3Kalpha in human PC3 cells assessed as reduction of AKT phosphorylation B 7.51 pIC50 31 nM IC50 J Med Chem (2013) 56: 4597-4610 [PMID:23662903]
ChEMBL Inhibition of PI3Kalpha in human MCF7-neo/Her2 cells assessed as reduction of AKT phosphorylation at S473 B 8.4 pIC50 4 nM IC50 J Med Chem (2013) 56: 4597-4610 [PMID:23662903]
ChEMBL Inhibition of PI3K alpha (unknown origin) B 9.15 pIC50 <0.7 nM IC50 ACS Med Chem Lett (2017) 8: 808-813 [PMID:28835793]
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]
GtoPdb - - 7.28 pKi 53 nM Ki US20170015678. Benzoxazepin oxazolidinone compounds and methods of use (2017)
GtoPdb - - 8.04 pKi 9.1 nM Ki J Med Chem (2013) 56: 4597-610 [PMID:23662903]
ChEMBL Inhibition of PI3Kbeta (unknown origin) B 8.04 pKi 9.1 nM Ki J Med Chem (2013) 56: 4597-4610 [PMID:23662903]
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 - - 9.68 pKi 0.21 nM Ki J Med Chem (2013) 56: 4597-610 [PMID:23662903]
ChEMBL Inhibition of PI3Kdelta (unknown origin) B 9.92 pKi 0.12 nM Ki J Med Chem (2013) 56: 4597-4610 [PMID:23662903]
GtoPdb - - 10.1 pKi 0.08 nM Ki US20170015678. Benzoxazepin oxazolidinone compounds and methods of use (2017)
ChEMBL Inhibition of PI3K delta (unknown origin) B 9.15 pIC50 <0.7 nM IC50 ACS Med Chem Lett (2017) 8: 808-813 [PMID:28835793]
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 - - 8.84 pKi 1.43 nM Ki US20170015678. Benzoxazepin oxazolidinone compounds and methods of use (2017)
GtoPdb - - 9.01 pKi 0.97 nM Ki J Med Chem (2013) 56: 4597-610 [PMID:23662903]
ChEMBL Inhibition of PI3Kgamma (unknown origin) B 9.01 pKi 0.97 nM Ki J Med Chem (2013) 56: 4597-4610 [PMID:23662903]
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 mTOR (unknown origin) B 5.92 pKi 1200 nM Ki J Med Chem (2013) 56: 4597-4610 [PMID:23662903]

ChEMBL data shown on this page come from version 32:

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]