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]
ChEMBL Binding affinity to AKT1 (unknown origin) B 9.8 pKi 0.16 nM Ki J Med Chem (2022) 65: 893-921 [PMID:33539089]
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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]