Target
3-phosphoinositide-dependent protein kinase 1 [51-359]
Ligand
BDBM281792
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:
BDBM281792
Synonyms:
2-({[5-(4-aminopyrido[3,4-d] pyrimidin-6-yl)thiophen-2-yl) methyl)amino)-N-(1-(4-fluoro- phenyl)ethyl)nicotinamide | US10030016, Example 2.13.2 | US10030016, Example 3.41
Type:
Small organic molecule
Emp. Form.:
C27H22F2N6OS
Mol. Mass.:
516.565
SMILES:
C[C@H](NC(=O)c1cccnc1NCc1ccc(s1)-c1ccc2ncnc(N)c2c1)c1ccc(F)c(F)c1 |r|
Structure:
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