Target
3-phosphoinositide-dependent protein kinase 1 [51-359,L159M]
Ligand
BDBM2691
Substrate
PDKtide
Meas. Tech.
PDK1 Kinase Activity Assay
pH
7.5±n/a
Temperature
303.15±n/a K
IC50
3000±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. Structure 12:215-26 (2004) [PubMed]  Article 
Target
Name:
3-phosphoinositide-dependent protein kinase 1 [51-359,L159M]
Synonyms:
3-Phosphoinositide-Dependent Protein Kinase 1 (PDK1) Mutant (L159M) | 3-phosphoinositide-dependent protein kinase 1 | PDK1 | PDPK1 | PDPK1_HUMAN | hPDK1
Type:
Kinase domain
Mol. Mass.:
35320.30
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:
MDGTAAEPRPGAGSLQHAQPPPQPRKKRPEDFKFGKILGEGSFSTVVLARELATSREYAIKILEKRHIIKENKVPYVTRERDVMSRLDHPFFVKLYFTFQDDEKLYFGMSYAKNGELLKYIRKIGSFDETCTRFYTAEIVSALEYLHGKGIIHRDLKPENILLNEDMHIQITDFGTAKVLSPESKQARANSFVGTAQYVSPELLTEKSACKSSDLWALGCIIYQLVAGLPPFRAGNEYLIFQKIIKLEYDFPEKFFPKARDLVEKLLVLDATKRLGCEEMEGYGPLKAHPFFESVTWENLHQQTPPKLT
  
Inhibitor
Name:
BDBM2691
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
Type:
Small organic molecule
Emp. Form.:
C23H20N4O2
Mol. Mass.:
384.4305
SMILES:
NCCCn1cc(C2=C(C(=O)NC2=O)c2c[nH]c3ccccc23)c2ccccc12 |t:7|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
PDKtide
Synonyms:
Synthetic PDK substrate peptide
Type:
Peptide
Mol. Mass.:
4766.24
Organism:
n/a
Description:
n/a
Residue:
39
Sequence:
KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC