Reaction Details Report a problem with these data
Target
3-phosphoinositide-dependent protein kinase 1 [51-359,E166D]
Ligand
BDBM2691
Substrate
PDKtide
Meas. Tech.
PDK1 Kinase Activity Assay
pH
7.5000±n/a
Temperature
303.1500±n/a K
IC50
5700±n/a nM
Citation
 Komander, D; Kular, GS; Schüttelkopf, AW; Deak, M; Prakash, KR; Bain, J; Elliott, M; Garrido-Franco, M; Kozikowski, AP; Alessi, DR; van 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,E166D]
Synonyms:
3-phosphoinositide-dependent protein kinase 1 | hPDK1 | PDPK1_HUMAN | PDPK1 | PDK1 | 3-Phosphoinositide-Dependent Protein Kinase 1 (PDK1) Mutant (E166D)
Type:
Kinase domain
Mol. Mass.:
35288.23
Organism:
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:
MDGTAAEPRPGAGSLQHAQPPPQPRKKRPEDFKFGKILGEGSFSTVVLARELATSREYAIKILEKRHIIKENKVPYVTRERDVMSRLDHPFFVKLYFTFQDDEKLYFGLSYAKNGDLLKYIRKIGSFDETCTRFYTAEIVSALEYLHGKGIIHRDLKPENILLNEDMHIQITDFGTAKVLSPESKQARANSFVGTAQYVSPELLTEKSACKSSDLWALGCIIYQLVAGLPPFRAGNEYLIFQKIIKLEYDFPEKFFPKARDLVEKLLVLDATKRLGCEEMEGYGPLKAHPFFESVTWENLHQQTPPKLT
  
Inhibitor
Name:
BDBM2691
Synonyms:
Bisindolyl deriv. 19 | 3-[1-(3-aminopropyl)-1H-indol-3-yl]-4-(1H-indol-3-yl)-2,5-dihydro-1H-pyrrole-2,5-dione | BIM-3
Type:
Small organic molecule
Emp. Form.:
TBD
Mol. Mass.:
TBD
SMILES:
TBD
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