Target
3-phosphoinositide-dependent protein kinase 1 [51-359]
Ligand
BDBM281916
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:
BDBM281916
Synonyms:
US10030016, Example 4.1.17 | US10030016, Example 4.1.18 | US10030016, Example 4.10 | US10030016, Example 4.11 | US10030016, Example 4.12 | US10030016, Example 4.13 | US10030016, Example 4.14 | US10030016, Example 4.15 | US10030016, Example 4.16 | US10030016, Example 4.17 | US10030016, Example 4.18 | US10030016, Example 4.19 | US10030016, Example 4.4 | US10030016, Example 4.5 | US10030016, Example 4.6 | US10030016, Example 4.7 | US10030016, Example 4.8 | US10030016, Example 4.9
Type:
Small organic molecule
Emp. Form.:
C35H35N5O6S
Mol. Mass.:
653.747
SMILES:
CCOC(=O)c1cccnc1NCc1cc(OC(C)C)cc(c1)-c1cn(c2ncc(cc12)C(=O)NC1CC1)S(=O)(=O)c1ccccc1
Structure:
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