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Target3-phosphoinositide dependent protein kinase-1
LigandBDBM17004
Substrate/CompetitorPDK1 Peptide Substrate
Meas. Tech.PDK1 Activity Assay (33P-filter paper)
IC50 6±n/a nM
Citation Islam, IBryant, JChou, YLKochanny, MJLee, WPhillips, GBYu, HAdler, MWhitlow, MHo, ELentz, DPolokoff, MASubramanyam, BWu, JMZhu, DFeldman, RIArnaiz, DO Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity. Bioorg Med Chem Lett17:3814-8 (2007) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
3-phosphoinositide dependent protein kinase-1
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 (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 | 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:
MARTTSQLYDAVPIQSSVVLCSCPSPSMVRTQTESSTPPGIPGGSRQGPAMDGTAAEPRP
GAGSLQHAQPPPQPRKKRPEDFKFGKILGEGSFSTVVLARELATSREYAIKILEKRHIIK
ENKVPYVTRERDVMSRLDHPFFVKLYFTFQDDEKLYFGLSYAKNGELLKYIRKIGSFDET
CTRFYTAEIVSALEYLHGKGIIHRDLKPENILLNEDMHIQITDFGTAKVLSPESKQARAN
SFVGTAQYVSPELLTEKSACKSSDLWALGCIIYQLVAGLPPFRAGNEYLIFQKIIKLEYD
FPEKFFPKARDLVEKLLVLDATKRLGCEEMEGYGPLKAHPFFESVTWENLHQQTPPKLTA
YLPAMSEDDEDCYGNYDNLLSQFGCMQVSSSSSSHSLSASDTGLPQRSGSNIEQYIHDLD
SNSFELDLQFSEDEKRLLLEKQAGGNPWHQFVENNLILKMGPVDKRKGLFARRRQLLLTE
GPHLYYVDPVNKVLKGEIPWSQELRPEAKNFKTFFVHTPNRTYYLMDPSGNAHKWCRKIQ
EVWRQRYQSHPDAAVQ
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM17004
NameBDBM17004
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
TypeSmall organic molecule
Emp. Form.C15H14N4O2
Mol. Mass.282.2973
SMILESC\C(=C1\C(=O)Nc2ccc(NC(N)=O)cc12)c1ccc[nH]1
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
PDK1 Peptide Substrate
Name:PDK1 Peptide Substrate
Synonyms:n/a
Type:Peptide
Mol. Mass.:1557.82
Organism:n/a
Description:n/a
Residue:14
Sequence:
ARRRGVTTKTFCGT