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Target
3-phosphoinositide-dependent protein kinase 1
Ligand
BDBM50340952
Substrate
n/a
Meas. Tech.
ChEMBL_739839 (CHEMBL1762899)
IC50
>30000±n/a nM
Citation
 Crew, AP; Bhagwat, SV; Dong, H; Bittner, MA; Chan, A; Chen, X; Coate, H; Cooke, A; Gokhale, PC; Honda, A; Jin, M; Kahler, J; Mantis, C; Mulvihill, MJ; Tavares-Greco, PA; Volk, B; Wang, J; Werner, DS; Arnold, LD; Pachter, JA; Wild, R; Gibson, NW Imidazo[1,5-a]pyrazines: orally efficacious inhibitors of mTORC1 and mTORC2. Bioorg Med Chem Lett 21:2092-7 (2011) [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:
BDBM50340952
Synonyms:
4-(8-amino-1-(1H-indol-2-yl)imidazo[1,5-a]pyrazin-3-yl)-N,N-dimethylpiperidine-1-carboxamide | CHEMBL1762114
Type:
Small organic molecule
Emp. Form.:
C22H25N7O
Mol. Mass.:
403.4802
SMILES:
CN(C)C(=O)N1CCC(CC1)c1nc(-c2cc3ccccc3[nH]2)c2c(N)nccn12
Structure:
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