Reaction Details Report a problem with these data
Target
3-phosphoinositide-dependent protein kinase 1 [51-359]
Ligand
BDBM2695
Substrate
PDKtide
Meas. Tech.
PDK1 Kinase Activity Assay
pH
7.5±n/a
Temperature
303.15±n/a K
IC50
1000±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:
BDBM2695
Synonyms:
3-[1-(3-aminopropyl)-1H-indol-3-yl]-4-(1-methyl-1H-indol-3-yl)-2,5-dihydro-1H-pyrrole-2,5-dione | BIM-8 | Bisindolylmaleimide VIII | Bisindolylmaleimide deriv. 2b | ROCHE screening, 49 | Ro 31-7549
Type:
Small organic molecule
Emp. Form.:
C24H22N4O2
Mol. Mass.:
398.4571
SMILES:
Cn1cc(C2=C(C(=O)NC2=O)c2cn(CCCN)c3ccccc23)c2ccccc12 |t:4|
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