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Target
3-phosphoinositide-dependent protein kinase 1
Ligand
BDBM19095
Substrate
Serine/threonine-protein kinase Sgk1
Meas. Tech.
ELISA assay
pH
7.4±n/a
Temperature
296.15±n/a K
IC50
300±n/a nM
Citation
 Gopalsamy, A; Shi, M; Boschelli, DH; Williamson, R; Olland, A; Hu, Y; Krishnamurthy, G; Han, X; Arndt, K; Guo, B Discovery of Dibenzo[c,f][2,7]naphthyridines as Potent and Selective 3-Phosphoinositide-Dependent Kinase-1 Inhibitors. J Med Chem 50:5547-9 (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:
BDBM19095
Synonyms:
16-methoxy-6-methyl-15-N-[2-(morpholin-4-yl)ethyl]-8,12-diazatetracyclo[8.8.0.0^{2,7}.0^{13,18}]octadeca-1(10),2(7),3,5,8,11,13,15,17-nonaene-5,9,15-triamine | Dibenzo[c,f][2,7]naphthyridine, 13
Type:
Small organic molecule
Emp. Form.:
C24H28N6O2
Mol. Mass.:
432.5181
SMILES:
COc1cc2c(cc1NCCN1CCOCC1)ncc1c(N)nc3c(C)c(N)ccc3c21
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Serine/threonine-protein kinase Sgk1
Synonyms:
SGK | SGK1 | SGK1_HUMAN | Serine/threonine-protein kinase Sgk1 | Serine/threonine-protein kinase Sgk1 (SGK) | Serum/glucocorticoid regulated kinase | Serum/glucocorticoid-regulated kinase 1 (SGK1)
Type:
Other Protein Type
Mol. Mass.:
48954.40
Organism:
Homo sapiens (Human)
Description:
Recombinant human SGK-1 enzyme produced in a baculovirus system.
Residue:
431
Sequence:
MTVKTEAAKGTLTYSRMRGMVAILIAFMKQRRMGLNDFIQKIANNSYACKHPEVQSILKISQPQEPELMNANPSPPPSPSQQINLGPSSNPHAKPSDFHFLKVIGKGSFGKVLLARHKAEEVFYAVKVLQKKAILKKKEEKHIMSERNVLLKNVKHPFLVGLHFSFQTADKLYFVLDYINGGELFYHLQRERCFLEPRARFYAAEIASALGYLHSLNIVYRDLKPENILLDSQGHIVLTDFGLCKENIEHNSTTSTFCGTPEYLAPEVLHKQPYDRTVDWWCLGAVLYEMLYGLPPFYSRNTAEMYDNILNKPLQLKPNITNSARHLLEGLLQKDRTKRLGAKDDFMEIKSHVFFSLINWDDLINKKITPPFNPNVSGPNDLRHFDPEFTEEPVPNSIGKSPDSVLVTASVKEAAEAFLGFSYAPPTDSFL