A-443654 [Ligand Id: 8204] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL379300 (A-443654, A-4436554)
  • 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
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 presence of 10 uM ATP B 9.8 pKi 0.16 nM Ki Bioorg. Med. Chem. Lett. (2006) 16: 3740-3744 [PMID:16678413]
ChEMBL Inhibition of AKT1 B 9.8 pKi 0.16 nM Ki Nat. Chem. Biol. (2009) 5: 484-493 [PMID:19465931]
GtoPdb - - 9.8 pKi 0.16 nM Ki Mol Cancer Ther (2005) 4: 977-86 [PMID:15956255]
ChEMBL Inhibition of myristoylated wild type AKT1 expressed in HEK293T cells by in vitro immunoprecipitation kinase assay B 8.6 pIC50 2.5 nM IC50 Nat. Chem. Biol. (2009) 5: 484-493 [PMID:19465931]
ChEMBL Inhibition of human Akt1 B 9.8 pIC50 0.16 nM IC50 J. Med. Chem. (2007) 50: 2990-3003 [PMID:17523610]
ChEMBL Inhibition of Akt B 9.8 pIC50 0.16 nM IC50 Eur. J. Med. Chem. (2009) 44: 4090-4097 [PMID:19497644]
AKT serine/threonine kinase 2/Serine/threonine-protein kinase AKT2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2431] [GtoPdb: 1480] [UniProtKB: P31751]
GtoPdb - - 9.8 pKi ~0.16 nM Ki Mol Cancer Ther (2005) 4: 977-86 [PMID:15956255]
ChEMBL Inhibition of myristoylated wild type AKT2 expressed in HEK293T cells by in vitro immunoprecipitation kinase assay B 7.52 pIC50 30 nM IC50 Nat. Chem. Biol. (2009) 5: 484-493 [PMID:19465931]
AKT serine/threonine kinase 3/Serine/threonine-protein kinase AKT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4816] [GtoPdb: 2286] [UniProtKB: Q9Y243]
GtoPdb - - 9.8 pKi ~0.16 nM Ki Mol Cancer Ther (2005) 4: 977-86 [PMID:15956255]
ChEMBL Inhibition of myristoylated wild type AKT3 expressed in HEK293T cells by in vitro immunoprecipitation kinase assay B 7.29 pIC50 51 nM IC50 Nat. Chem. Biol. (2009) 5: 484-493 [PMID:19465931]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]