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Target
3-phosphoinositide-dependent protein kinase 1
Ligand
BDBM50393342
Substrate
n/a
Meas. Tech.
ChEMBL_850924 (CHEMBL2156907)
IC50
>3600±n/a nM
Citation
Leahy, JW; Buhr, CA; Johnson, HW; Kim, BG; Baik, T; Cannoy, J; Forsyth, TP; Jeong, JW; Lee, MS; Ma, S; Noson, K; Wang, L; Williams, M; Nuss, JM; Brooks, E; Foster, P; Goon, L; Heald, N; Holst, C; Jaeger, C; Lam, S; Lougheed, J; Nguyen, L; Plonowski, A; Song, J; Stout, T; Wu, X; Yakes, MF; Yu, P; Zhang, W; Lamb, P; Raeber, O Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors. J Med Chem 55:5467-82 (2012) [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