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Target
3-phosphoinositide-dependent protein kinase 1
Ligand
BDBM50316348
Substrate
n/a
Meas. Tech.
ChEMBL_627903 (CHEMBL1103719)
IC50
18±n/a nM
Citation
Nittoli, T; Dushin, RG; Ingalls, C; Cheung, K; Floyd, MB; Fraser, H; Olland, A; Hu, Y; Grosu, G; Han, X; Arndt, K; Guo, B; Wissner, A The identification of 8,9-dimethoxy-5-(2-aminoalkoxy-pyridin-3-yl)-benzo[c][2,7]naphthyridin-4-ylamines as potent inhibitors of 3-phosphoinositide-dependent kinase-1 (PDK-1). Eur J Med Chem 45:1379-86 (2010) [PubMed] Article
More Info.:
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:
BDBM50316348
Synonyms:
2-(5-{[(2R)-2-Amino-4-methylpentyl]oxy}pyridin-3-yl)-8,9-dimethoxybenzo[c]-2,7-naphthyridin-4-amine | CHEMBL1094637
Type:
Small organic molecule
Emp. Form.:
C25H29N5O3
Mol. Mass.:
447.5295
SMILES:
COc1cc2ncc3c(N)nc(cc3c2cc1OC)-c1cncc(OC[C@H](N)CC(C)C)c1 |r|