Target
3-phosphoinositide-dependent protein kinase 1 [51-359]
Ligand
BDBM282154
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:
BDBM282154
Synonyms:
3-(4-(5-aminopyrazin-2-yl) benzylamino)-6-cyano- N-(4-fluorophenyl) pyrazine-2-carboxamide | US10030016, Example 34
Type:
Small organic molecule
Emp. Form.:
C23H17FN8O
Mol. Mass.:
440.4325
SMILES:
Nc1cnc(cn1)-c1ccc(CNc2ncc(nc2C(=O)Nc2ccc(F)cc2)C#N)cc1
Structure:
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