Target
3-phosphoinositide-dependent protein kinase 1 [51-359]
Ligand
BDBM282441
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:
BDBM282441
Synonyms:
2-(4-(4-amino-7H-pyrrolo [2,3-d]pyrimidin-5-yl) benzylamino)-N-(4- fluorophenyl)-5- (trifluoromethyl)nicotinamide | US10030016, Example 321
Type:
Small organic molecule
Emp. Form.:
C26H19F4N7O
Mol. Mass.:
521.469
SMILES:
Nc1ncnc2[nH]cc(-c3ccc(CNc4ncc(cc4C(=O)Nc4ccc(F)cc4)C(F)(F)F)cc3)c12
Structure:
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