Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
Target3-Phosphoinositide-Dependent Protein Kinase 1 (PDK1) Mutant (A162V)
LigandBDBM17055
Substrate/CompetitorPDKtide
Meas. Tech.PDK1 Kinase Activity Assay
pH7.5±n/a
Temperature303.15±n/a K
IC50 743±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. Structure12:215-26 (2004) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
3-Phosphoinositide-Dependent Protein Kinase 1 (PDK1) Mutant (A162V)
Name:3-Phosphoinositide-Dependent Protein Kinase 1 (PDK1) Mutant (A162V)
Synonyms:3-phosphoinositide-dependent protein kinase 1 | hPDK1
Type:Kinase domain
Mol. Mass.:35330.31
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:
MDGTAAEPRPGAGSLQHAQPPPQPRKKRPEDFKFGKILGEGSFSTVVLARELATSREYAI
KILEKRHIIKENKVPYVTRERDVMSRLDHPFFVKLYFTFQDDEKLYFGLSYVKNGELLKY
IRKIGSFDETCTRFYTAEIVSALEYLHGKGIIHRDLKPENILLNEDMHIQITDFGTAKVL
SPESKQARANSFVGTAQYVSPELLTEKSACKSSDLWALGCIIYQLVAGLPPFRAGNEYLI
FQKIIKLEYDFPEKFFPKARDLVEKLLVLDATKRLGCEEMEGYGPLKAHPFFESVTWENL
HQQTPPKLT
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM17055
NameBDBM17055
Synonyms:(18S)-18-[(dimethylamino)methyl]-17-oxa-4,14,21-triazahexacyclo[19.6.1.1^{7,14}.0^{2,6}.0^{8,13}.0^{22,27}]nonacosa-1(28),2(6),7(29),8(13),9,11,22(27),23,25-nonaene-3,5-dione | (9S)-9-[(dimethylamino)methyl]-6,7,10,11-tetrahydro-9H,18H-5,21:12,17-di(metheno)dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecine-18,20(19H)-dione | K00587a | LY 333531 | LY-333531 | LY333531 | Ruboxistaurin | cid_153999
TypeSmall organic molecule
Emp. Form.C28H28N4O3
Mol. Mass.468.5469
SMILESCN(C)C[C@@H]1CCn2cc(C3=C(C(=O)NC3=O)c3cn(CCO1)c1ccccc31)c1ccccc21 |r,t:10|
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
PDKtide
Name:PDKtide
Synonyms:Synthetic PDK substrate peptide
Type:Peptide
Mol. Mass.:4766.24
Organism:n/a
Description:n/a
Residue:39
Sequence:
KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC