ipatasertib [Ligand Id: 7887] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2177390 (Rg-7440, RG7440, Ipatasertib, GDC-0068, RG-7440)
  • Protein kinase G (PKG) 1/cGMP-dependent protein kinase 1 beta in Human [ChEMBL: CHEMBL4273] [GtoPdb: 1492] [UniProtKB: Q13976]
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  • AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
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  • AKT serine/threonine kinase 2/Serine/threonine-protein kinase AKT2 in Human [ChEMBL: CHEMBL2431] [GtoPdb: 1480] [UniProtKB: P31751]
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  • AKT serine/threonine kinase 3/Serine/threonine-protein kinase AKT3 in Human [ChEMBL: CHEMBL4816] [GtoPdb: 2286] [UniProtKB: Q9Y243]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Protein kinase G (PKG) 1/cGMP-dependent protein kinase 1 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4273] [GtoPdb: 1492] [UniProtKB: Q13976]
ChEMBL Inhibition of PRKG1alpha B 7.01 pIC50 98 nM IC50 J. Med. Chem. (2012) 55: 8110-8127 [PMID:22934575]
GtoPdb - - 7.16 pIC50 69 nM IC50 J Med Chem (2012) 55: 8110-27 [PMID:22934575]
ChEMBL Inhibition of PRKG1beta B 7.16 pIC50 69 nM IC50 J. Med. Chem. (2012) 55: 8110-8127 [PMID:22934575]
AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
ChEMBL Inhibition of Akt1 in human LNCAP cells assessed as phosphorylation of PRAS40 at Thr246 after 1.5 hrs B 6.8 pIC50 157 nM IC50 J. Med. Chem. (2012) 55: 8110-8127 [PMID:22934575]
ChEMBL Competitive inhibition of wild-type full-length amino-terminal polyhistidine-tagged human Akt1 expressed in recombinant baculovirus system using fluorescence labeled substrate after 60 mins by fluorescence polarization assay in presence of ATP B 8.3 pIC50 5 nM IC50 J. Med. Chem. (2012) 55: 8110-8127 [PMID:22934575]
GtoPdb - - 9 pIC50 1 nM IC50 J Med Chem (2012) 55: 8110-27 [PMID:22934575]
AKT serine/threonine kinase 2/Serine/threonine-protein kinase AKT2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2431] [GtoPdb: 1480] [UniProtKB: P31751]
GtoPdb - - 7.74 pIC50 18 nM IC50 J Med Chem (2012) 55: 8110-27 [PMID:22934575]
ChEMBL Competitive inhibition of wild-type full-length amino-terminal polyhistidine-tagged human Akt2 expressed in recombinant baculovirus system using fluorescence labeled substrate after 60 mins by fluorescence polarization assay in presence of ATP B 7.74 pIC50 18 nM IC50 J. Med. Chem. (2012) 55: 8110-8127 [PMID:22934575]
AKT serine/threonine kinase 3/Serine/threonine-protein kinase AKT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4816] [GtoPdb: 2286] [UniProtKB: Q9Y243]
ChEMBL Competitive inhibition of wild-type full-length amino-terminal polyhistidine-tagged human Akt3 expressed in recombinant baculovirus system using fluorescence labeled Crosstide as substrate after 60 mins by fluorescence polarization assay in presence of ATP B 8.1 pIC50 8 nM IC50 J. Med. Chem. (2012) 55: 8110-8127 [PMID:22934575]
GtoPdb - - 8.1 pIC50 8 nM IC50 J Med Chem (2012) 55: 8110-27 [PMID:22934575]

ChEMBL data shown on this page come from version 28:

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]