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 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]
