Compile Data Set for Download or QSAR
Report error Found 4 Enz. Inhib. hit(s) for PDB: 1Z5M
Target3-phosphoinositide-dependent protein kinase 1(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM17053(N-(3-{[5-bromo-2-({3-[(pyrrolidin-1-ylcarbonyl)ami...)
Affinity DataIC50: 30nMAssay Description:Inhibition of N terminal His-tagged human recombinant PDK1 using H2NARRRGVTTKTFCGT peptide as substrate assessed as substrate phosphorylation after 4...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
Target3-phosphoinositide-dependent protein kinase 1(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM17053(N-(3-{[5-bromo-2-({3-[(pyrrolidin-1-ylcarbonyl)ami...)
Affinity DataIC50: 39nMpH: 7.2 T: 2°CAssay Description:The coupled assay can detect inhibitors of AKT2 activation, as well as direct inhibitors of PDK1 or AKT2. Inactive AKT2 is activated in situ by incub...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/2/2007
Entry Details Article
PubMedPDB3D3D Structure (crystal)
Target3-phosphoinositide-dependent protein kinase 1(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM17053(N-(3-{[5-bromo-2-({3-[(pyrrolidin-1-ylcarbonyl)ami...)
Affinity DataIC50: 39nMAssay Description:Inhibition of PDK1 using [gamma33P]-ATP as substrate after 30 mins by scintillation countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/22/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
Target3-phosphoinositide-dependent protein kinase 1(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM17053(N-(3-{[5-bromo-2-({3-[(pyrrolidin-1-ylcarbonyl)ami...)
Affinity DataIC50: 39nMAssay Description:Inhibition of human recombinant PDK1 assessed as PtdIns-3,4-P2-mediated AKT2 activation using biotin-ARRRDGGGAQPFRPRAATF as substrate after 2 hrs by ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/18/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)