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Target
3-phosphoinositide-dependent protein kinase 1 [51-359]
Ligand
BDBM282167
Substrate
n/a
Meas. Tech.
PDK1 kinase assay
IC50
<100±n/a nM
Citation
 Arndt, J; Chan, T; Guckian, K; Kumaravel, G; Lee, W; Lin, EY; Scott, D; Sun, L; Thomas, J; van Vloten, K; Wang, D; Zhang, L; Erlanson, 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:
BDBM282167
Synonyms:
2-((R)-1-(4-(4 - amino-7H-pyrrolo[2,3-d] pyrimidin-5-yl)phenyl)- 3-(methylamino)-3- oxopropylamino)-5-cyano- N-((S)-1-(4-fluorophenyl) ethyl)nicotinamide | US10030016, Example 47
Type:
Small organic molecule
Emp. Form.:
C31H28FN9O2
Mol. Mass.:
577.6115
SMILES:
CNC(=O)C[C@@H](Nc1ncc(cc1C(=O)N[C@@H](C)c1ccc(F)cc1)C#N)c1ccc(cc1)-c1c[nH]c2ncnc(N)c12 |r|
Structure:
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