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Target
3-phosphoinositide-dependent protein kinase 1
Ligand
BDBM17004
Substrate
PDK1 Peptide Substrate
Meas. Tech.
PDK1 Activity Assay (33P-filter paper)
IC50
6±n/a nM
Citation
 Islam, I; Bryant, J; Chou, YL; Kochanny, MJ; Lee, W; Phillips, GB; Yu, H; Adler, M; Whitlow, M; Ho, E; Lentz, D; Polokoff, MA; Subramanyam, B; Wu, JM; Zhu, D; Feldman, RI; Arnaiz, DO Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity. Bioorg Med Chem Lett 17:3814-8 (2007) [PubMed]  Article 
Target
Name:
3-phosphoinositide-dependent protein kinase 1
Synonyms:
3-Phosphoinositide-Dependent Protein Kinase 1 (PDK1) | 3-phosphoinositide dependent protein kinase-1 | 3-phosphoinositide-dependent protein kinase 1 | 3-phosphoinositide-dependent protein kinase 1 (PDK) | 3-phosphoinositide-dependent protein kinase 1 (PDK-1) | 3-phosphoinositide-dependent protein kinase 1 (PDK1)(Δ1-50) | Isoform 2 of 3-phosphoinositide-dependent protein kinase 1 | PDK1 | PDPK1 | PDPK1_HUMAN | Phosphoinositide-dependent protein kinase 1 (PDK1) | Pyruvate dehydrogenase kinase isoenzyme 1 (PDK1) | hPDK1
Type:
Enzyme
Mol. Mass.:
63157.65
Organism:
Homo sapiens (Human)
Description:
O15530
Residue:
556
Sequence:
MARTTSQLYDAVPIQSSVVLCSCPSPSMVRTQTESSTPPGIPGGSRQGPAMDGTAAEPRPGAGSLQHAQPPPQPRKKRPEDFKFGKILGEGSFSTVVLARELATSREYAIKILEKRHIIKENKVPYVTRERDVMSRLDHPFFVKLYFTFQDDEKLYFGLSYAKNGELLKYIRKIGSFDETCTRFYTAEIVSALEYLHGKGIIHRDLKPENILLNEDMHIQITDFGTAKVLSPESKQARANSFVGTAQYVSPELLTEKSACKSSDLWALGCIIYQLVAGLPPFRAGNEYLIFQKIIKLEYDFPEKFFPKARDLVEKLLVLDATKRLGCEEMEGYGPLKAHPFFESVTWENLHQQTPPKLTAYLPAMSEDDEDCYGNYDNLLSQFGCMQVSSSSSSHSLSASDTGLPQRSGSNIEQYIHDLDSNSFELDLQFSEDEKRLLLEKQAGGNPWHQFVENNLILKMGPVDKRKGLFARRRQLLLTEGPHLYYVDPVNKVLKGEIPWSQELRPEAKNFKTFFVHTPNRTYYLMDPSGNAHKWCRKIQEVWRQRYQSHPDAAVQ
  
Inhibitor
Name:
BDBM17004
Synonyms:
BX-517 | Indolinone based inhibitor, 4i | [(3Z)-2-oxo-3-[1-(1H-pyrrol-2-yl)ethylidene]-2,3-dihydro-1H-indol-5-yl]urea
Type:
Small organic molecule
Emp. Form.:
C15H14N4O2
Mol. Mass.:
282.2973
SMILES:
C\C(=C1\C(=O)Nc2ccc(NC(N)=O)cc12)c1ccc[nH]1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
PDK1 Peptide Substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
1557.82
Organism:
n/a
Description:
n/a
Residue:
14
Sequence:
ARRRGVTTKTFCGT