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Target3-phosphoinositide dependent protein kinase-1
LigandBDBM50418251
Substrate/Competitorn/a
Meas. Tech.ChEMBL_742329
IC50 10.0±n/a nM
Citation Medina, JRBecker, CJBlackledge, CWDuquenne, CFeng, YGrant, SWHeerding, DLi, WHMiller, WHRomeril, SPScherzer, DShu, ABobko, MAChadderton, ARDumble, MGardiner, CMGilbert, SLiu, QRabindran, SKSudakin, VXiang, HBrady, PGCampobasso, NWard, PAxten, JM Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors. J Med Chem54:1871-95 (2011) [PubMed]  Article
More Info.:Get all data from this article,  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:n/a
Residue:556
Sequence:
MARTTSQLYDAVPIQSSVVLCSCPSPSMVRTQTESSTPPGIPGGSRQGPAMDGTAAEPRP
GAGSLQHAQPPPQPRKKRPEDFKFGKILGEGSFSTVVLARELATSREYAIKILEKRHIIK
ENKVPYVTRERDVMSRLDHPFFVKLYFTFQDDEKLYFGLSYAKNGELLKYIRKIGSFDET
CTRFYTAEIVSALEYLHGKGIIHRDLKPENILLNEDMHIQITDFGTAKVLSPESKQARAN
SFVGTAQYVSPELLTEKSACKSSDLWALGCIIYQLVAGLPPFRAGNEYLIFQKIIKLEYD
FPEKFFPKARDLVEKLLVLDATKRLGCEEMEGYGPLKAHPFFESVTWENLHQQTPPKLTA
YLPAMSEDDEDCYGNYDNLLSQFGCMQVSSSSSSHSLSASDTGLPQRSGSNIEQYIHDLD
SNSFELDLQFSEDEKRLLLEKQAGGNPWHQFVENNLILKMGPVDKRKGLFARRRQLLLTE
GPHLYYVDPVNKVLKGEIPWSQELRPEAKNFKTFFVHTPNRTYYLMDPSGNAHKWCRKIQ
EVWRQRYQSHPDAAVQ
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50418251
NameBDBM50418251
Synonyms:CHEMBL1614776
TypeSmall organic molecule
Emp. Form.C22H30N8O2
Mol. Mass.438.526
SMILESC[C@H]1CC[C@H](CN1c1cc(nc(N)n1)-c1ccc2c(N)[nH]nc2c1)NC(=O)OC(C)(C)C |r|
Structure
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n/a