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Target3-phosphoinositide dependent protein kinase-1
LigandBDBM17023
Substrate/CompetitorSerine/threonine-protein kinase AKT2
Meas. Tech.PDK1-mediated AKT2 Activation Assay (cAKT2 33P-SPA)
pH7.2±n/a
Temperature295.15±n/a K
IC50 80±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
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BDBM17023
NameBDBM17023
Synonyms:(3Z)-5-hydroxy-3-[1-(1H-pyrrol-2-yl)ethylidene]-2,3-dihydro-1H-indol-2-one | Indolinone based inhibitor, 2a
TypeSmall organic molecule
Emp. Form.C14H12N2O2
Mol. Mass.240.2573
SMILESC\C(=C1\C(=O)Nc2ccc(O)cc12)c1ccc[nH]1
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
Serine/threonine-protein kinase AKT2
Name:Serine/threonine-protein kinase AKT2
Synonyms:AKT2 | PKB beta | Protein kinase Akt-2 | Protein kinase B (Akt 2) | Protein kinase B beta (AKT2) | Protein kinase B, beta | RAC-PK-beta | RAC-alpha serine/threonine-protein kinase (AKT2) | RAC-beta serine/threonine-protein kinase | RAC-beta serine/threonine-protein kinase (AKT2) | Serine/threonine-protein kinase AKT
Type:Enzyme
Mol. Mass.:55766.64
Organism:Homo sapiens (Human)
Description:n/a
Residue:481
Sequence:
MNEVSVIKEGWLHKRGEYIKTWRPRYFLLKSDGSFIGYKERPEAPDQTLPPLNNFSVAEC
QLMKTERPRPNTFVIRCLQWTTVIERTFHVDSPDEREEWMRAIQMVANSLKQRAPGEDPM
DYKCGSPSDSSTTEEMEVAVSKARAKVTMNDFDYLKLLGKGTFGKVILVREKATGRYYAM
KILRKEVIIAKDEVAHTVTESRVLQNTRHPFLTALKYAFQTHDRLCFVMEYANGGELFFH
LSRERVFTEERARFYGAEIVSALEYLHSRDVVYRDIKLENLMLDKDGHIKITDFGLCKEG
ISDGATMKTFCGTPEYLAPEVLEDNDYGRAVDWWGLGVVMYEMMCGRLPFYNQDHERLFE
LILMEEIRFPRTLSPEAKSLLAGLLKKDPKQRLGGGPSDAKEVMEHRFFLSINWQDVVQK
KLLPPFKPQVTSEVDTRYFDDEFTAQSITITPPDRYDSLGLLELDQRTHFPQFSYSASIR
E
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