OSU-03012 [Ligand Id: 8005] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1650595 (Ar-12, OSU-03012, AR-12)
  • 3-phosphoinositide dependent protein kinase 1/3-phosphoinositide dependent protein kinase-1 in Human [ChEMBL: CHEMBL2534] [GtoPdb: 1519] [UniProtKB: O15530]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
3-phosphoinositide dependent protein kinase 1/3-phosphoinositide dependent protein kinase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2534] [GtoPdb: 1519] [UniProtKB: O15530]
ChEMBL Inhibition of recombinant PDK1 (unknown origin) using RPRAATF peptide as substrate assessed as substrate phosphorylation by scintillation counting analysis in presence of [gamma-32P]ATP B 5.3 pIC50 5000 nM IC50 J. Med. Chem. (2013) 56: 2726-2737 [PMID:23448267]
ChEMBL In Vitro Kinase Assay: PDK-1 kinase activity This in vitro assay was performed using a PDK-1 kinase assay kit (Upstate, Lake Placid, N.Y.) according to the vendor's instructions. This cell-free assay is based on the ability of recombinant PDK-1, in the presence of DMSO vehicle or the test agent, to activate its downstream kinase serum- and glucocorticoid-regulated kinase (SGK.) which, in turn, phosphorylates the Akt/SGK-specific peptide substrate RPRAATF with [γ-32]-ATP. The [32P]-phosphorylated peptide substrate was then separated from the residual [γ-32P]-ATP using PS1 phosphocellulose paper and quantitated by a scintillation counter after three washes with 0.75% phosphoric acid. B 5.3 pIC50 5000 nM IC50 US-8741944-B2. Anti-infective agents against intracellular pathogens (2014)
GtoPdb - - 8.05 pIC50 9 nM IC50 Cancer Res (2004) 64: 4309-18 [PMID:15205346]

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, 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]