Reaction Details Report a problem with these data
Target
3-phosphoinositide-dependent protein kinase 1 [51-359]
Ligand
BDBM282386
Substrate
n/a
Meas. Tech.
PDK1 kinase assay
IC50
550±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:
BDBM282386
Synonyms:
(S)-2-(4-(3-amino-1H-pyrazolo [3,4-b]pyridin-5-yl) benzylamino)-N-1-(4- fluorophenyl)-2-hydroxyethyl)- 5-(trifluoromethyl) nicotinamide | US10030016, Example 266
Type:
Small organic molecule
Emp. Form.:
C28H23F4N7O2
Mol. Mass.:
565.5215
SMILES:
Nc1n[nH]c2ncc(cc12)-c1ccc(CNc2ncc(cc2C(=O)N[C@H](CO)c2ccc(F)cc2)C(F)(F)F)cc1 |r|
Structure:
Search PDB for entries with ligand similarity: