Target
3-phosphoinositide-dependent protein kinase 1 [51-359]
Ligand
BDBM282467
Substrate
n/a
Meas. Tech.
PDK1 kinase assay
IC50
<100±n/a nM
Citation
 Arndt, JChan, TGuckian, KKumaravel, GLee, WLin, EYScott, DSun, LThomas, Jvan Vloten, KWang, DZhang, LErlanson, D Heterocyclic compounds useful as PDK1 inhibitors US Patent  US10030016 Publication Date 7/24/2018 
Target
Name:
3-phosphoinositide-dependent protein kinase 1 [51-359]
Synonyms:
3-Phosphoinositide-Dependent Protein Kinase 1 (PDK1) | 3-phosphoinositide-dependent protein kinase 1 | 3-phosphoinositide-dependent protein kinase 1 (aa 51-359) | PDK1 | PDK1 (aa 51-359) | PDPK1 | PDPK1_HUMAN | hPDK1
Type:
Enzyme Catalytic Domain
Mol. Mass.:
35302.26
Organism:
Homo sapiens (Human)
Description:
O15530[51-359]
Residue:
309
Sequence:
MDGTAAEPRPGAGSLQHAQPPPQPRKKRPEDFKFGKILGEGSFSTVVLARELATSREYAIKILEKRHIIKENKVPYVTRERDVMSRLDHPFFVKLYFTFQDDEKLYFGLSYAKNGELLKYIRKIGSFDETCTRFYTAEIVSALEYLHGKGIIHRDLKPENILLNEDMHIQITDFGTAKVLSPESKQARANSFVGTAQYVSPELLTEKSACKSSDLWALGCIIYQLVAGLPPFRAGNEYLIFQKIIKLEYDFPEKFFPKARDLVEKLLVLDATKRLGCEEMEGYGPLKAHPFFESVTWENLHQQTPPKLT
  
Inhibitor
Name:
BDBM282467
Synonyms:
3-amino-6-(4-((5-cyano- 3-((S)-1-(4-fluorophenyl) ethylcarbamoyl)pyridin- 2-ylamino)methyl)phenyl)- N-(2,3-dihydroxypropyl) pyrazine-2-carboxamide | US10030016, Example 347
Type:
Small organic molecule
Emp. Form.:
C29H30FN7O4
Mol. Mass.:
559.5914
SMILES:
C[C@H](NC(=O)c1cccnc1NCc1ccc(cc1)-c1cnc(N)c(n1)C(=O)NCC(O)CO)c1ccc(F)cc1 |r|
Structure:
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