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Target
3-phosphoinositide-dependent protein kinase 1 [51-359,T222A]
Ligand
BDBM17055
Substrate
PDKtide
Meas. Tech.
PDK1 Kinase Activity Assay
pH
7.5000±n/a
Temperature
303.1500±n/a K
IC50
734±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,T222A]
Synonyms:
3-phosphoinositide-dependent protein kinase 1 | hPDK1 | PDPK1_HUMAN | PDPK1 | PDK1 | 3-Phosphoinositide-Dependent Protein Kinase 1 (PDK1) Mutant (T222A)
Type:
Kinase domain
Mol. Mass.:
35272.23
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:
MDGTAAEPRPGAGSLQHAQPPPQPRKKRPEDFKFGKILGEGSFSTVVLARELATSREYAIKILEKRHIIKENKVPYVTRERDVMSRLDHPFFVKLYFTFQDDEKLYFGLSYAKNGELLKYIRKIGSFDETCTRFYTAEIVSALEYLHGKGIIHRDLKPENILLNEDMHIQIADFGTAKVLSPESKQARANSFVGTAQYVSPELLTEKSACKSSDLWALGCIIYQLVAGLPPFRAGNEYLIFQKIIKLEYDFPEKFFPKARDLVEKLLVLDATKRLGCEEMEGYGPLKAHPFFESVTWENLHQQTPPKLT
  
Inhibitor
Name:
BDBM17055
Synonyms:
(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 | (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 | K00587a | Ruboxistaurin | LY-333531 | cid_153999 | LY 333531 | LY333531
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