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Target
3-phosphoinositide-dependent protein kinase 1 [51-359]
Ligand
BDBM2694
Substrate
PDKtide
Meas. Tech.
PDK1 Kinase Activity Assay
pH
7.5±n/a
Temperature
303.15±n/a K
IC50
14000±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]
Synonyms:
3-Phosphoinositide-Dependent Protein Kinase 1 (PDK1) | 3-phosphoinositide-dependent protein kinase 1 | 3-phosphoinositide-dependent protein kinase 1 (aa 51-359) | PDK1 | PDK1 (aa 51-359) | PDPK1 | PDPK1_HUMAN | hPDK1
Type:
Enzyme Catalytic Domain
Mol. Mass.:
35302.26
Organism:
Homo sapiens (Human)
Description:
O15530[51-359]
Residue:
309
Sequence:
MDGTAAEPRPGAGSLQHAQPPPQPRKKRPEDFKFGKILGEGSFSTVVLARELATSREYAIKILEKRHIIKENKVPYVTRERDVMSRLDHPFFVKLYFTFQDDEKLYFGLSYAKNGELLKYIRKIGSFDETCTRFYTAEIVSALEYLHGKGIIHRDLKPENILLNEDMHIQITDFGTAKVLSPESKQARANSFVGTAQYVSPELLTEKSACKSSDLWALGCIIYQLVAGLPPFRAGNEYLIFQKIIKLEYDFPEKFFPKARDLVEKLLVLDATKRLGCEEMEGYGPLKAHPFFESVTWENLHQQTPPKLT
  
Inhibitor
Name:
BDBM2694
Synonyms:
3-(1H-indol-3-yl)-4-{1-[2-(1-methylpyrrolidin-2-yl)ethyl]-1H-indol-3-yl}-2,5-dihydro-1H-pyrrole-2,5-dione | BIM-2 | Bisindolyl deriv. 22 | CHEMBL218328
Type:
Small organic molecule
Emp. Form.:
C27H26N4O2
Mol. Mass.:
438.5209
SMILES:
CN1CCCC1CCn1cc(C2=C(C(=O)NC2=O)c2c[nH]c3ccccc23)c2ccccc12 |t:12|
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