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) |
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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 33:
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]
