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

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ChEMBL ligand: CHEMBL1650595 (Ar-12, AR-12, OSU-03012, Pdk1 inhibitor 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 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]