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Target3-Phosphoinositide-Dependent Protein Kinase 1 (PDK1) Mutant (A162V)
LigandBDBM2691
Substrate/CompetitorPDKtide
Meas. Tech.PDK1 Kinase Activity Assay
pH7.5±n/a
Temperature303.15±n/a K
IC50 3400±n/a nM
Citation Komander, DKular, GSSchüttelkopf, AWDeak, MPrakash, KRBain, JElliott, MGarrido-Franco, MKozikowski, APAlessi, DRvan Aalten, DM Interactions of LY333531 and other bisindolyl maleimide inhibitors with PDK1. Structure12:215-26 (2004) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
3-Phosphoinositide-Dependent Protein Kinase 1 (PDK1) Mutant (A162V)
Name:3-Phosphoinositide-Dependent Protein Kinase 1 (PDK1) Mutant (A162V)
Synonyms:3-phosphoinositide-dependent protein kinase 1 | hPDK1
Type:Kinase domain
Mol. Mass.:35330.31
Organism:Homo sapiens (Human)
Description:The mutant enzyme was generated using site-directed mutagenesis and expressed as glutathione-S-transferase (GST) fusion proteins in insect cells.
Residue:309
Sequence:
MDGTAAEPRPGAGSLQHAQPPPQPRKKRPEDFKFGKILGEGSFSTVVLARELATSREYAI
KILEKRHIIKENKVPYVTRERDVMSRLDHPFFVKLYFTFQDDEKLYFGLSYVKNGELLKY
IRKIGSFDETCTRFYTAEIVSALEYLHGKGIIHRDLKPENILLNEDMHIQITDFGTAKVL
SPESKQARANSFVGTAQYVSPELLTEKSACKSSDLWALGCIIYQLVAGLPPFRAGNEYLI
FQKIIKLEYDFPEKFFPKARDLVEKLLVLDATKRLGCEEMEGYGPLKAHPFFESVTWENL
HQQTPPKLT
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  Blast E-value cutoff:
BDBM2691
NameBDBM2691
Synonyms:3-[1-(3-aminopropyl)-1H-indol-3-yl]-4-(1H-indol-3-yl)-2,5-dihydro-1H-pyrrole-2,5-dione | BIM-3 | Bisindolyl deriv. 19
TypeSmall organic molecule
Emp. Form.C23H20N4O2
Mol. Mass.384.4305
SMILESNCCCn1cc(C2=C(C(=O)NC2=O)c2c[nH]c3ccccc23)c2ccccc12 |t:7|
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
PDKtide
Name:PDKtide
Synonyms:Synthetic PDK substrate peptide
Type:Peptide
Mol. Mass.:4766.24
Organism:n/a
Description:n/a
Residue:39
Sequence:
KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC