Reaction Details Report a problem with these data
Target
3-phosphoinositide-dependent protein kinase 1 [51-359]
Ligand
BDBM17054
Substrate
PDKtide
Meas. Tech.
PDK1 Kinase Activity Assay
pH
7.5000±n/a
Temperature
303.1500±n/a K
IC50
5±n/a nM
Citation
 Komander, D; Kular, GS; Bain, J; Elliott, M; Alessi, DR; Van Aalten, DM Structural basis for UCN-01 (7-hydroxystaurosporine) specificity and PDK1 (3-phosphoinositide-dependent protein kinase-1) inhibition. Biochem J 375:255-62 (2003) [PubMed]  Article 
Target
Name:
3-phosphoinositide-dependent protein kinase 1 [51-359]
Synonyms:
3-phosphoinositide-dependent protein kinase 1 (aa 51-359) | 3-Phosphoinositide-Dependent Protein Kinase 1 (PDK1) | 3-phosphoinositide-dependent protein kinase 1 | PDK1 (aa 51-359) | hPDK1 | PDPK1_HUMAN | PDPK1 | PDK1
Type:
Enzyme Catalytic Domain
Mol. Mass.:
35302.26
Organism:
Human
Description:
O15530[51-359]
Residue:
309
Sequence:
MDGTAAEPRPGAGSLQHAQPPPQPRKKRPEDFKFGKILGEGSFSTVVLARELATSREYAIKILEKRHIIKENKVPYVTRERDVMSRLDHPFFVKLYFTFQDDEKLYFGLSYAKNGELLKYIRKIGSFDETCTRFYTAEIVSALEYLHGKGIIHRDLKPENILLNEDMHIQITDFGTAKVLSPESKQARANSFVGTAQYVSPELLTEKSACKSSDLWALGCIIYQLVAGLPPFRAGNEYLIFQKIIKLEYDFPEKFFPKARDLVEKLLVLDATKRLGCEEMEGYGPLKAHPFFESVTWENLHQQTPPKLT
  
Inhibitor
Name:
BDBM17054
Synonyms:
(5S,6R,7R,9R,16R)-16-hydroxy-6-methoxy-5-methyl-7-(methylamino)-6,7,8,9,15,16-hexahydro-5H,14H-5,9-epoxy-4b,9a,15-triazadibenzo[b,h]cyclonona[1,2,3,4-jkl]cyclopenta[e]-as-indacen-14-one | 7-Hydroxystaurosporine | (2S,3R,4R,6R,18R)-18-hydroxy-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1^{2,6}.0^{7,28}.0^{8,13}.0^{15,19}.0^{20,27}.0^{21,26}]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-16-one | UCN-01
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