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Target
3-phosphoinositide-dependent protein kinase 1 [51-359]
Ligand
BDBM281902
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:
BDBM281902
Synonyms:
N-cyclopropyl-3-{3- [({3-[(3,4-difluoro- benzyl)carbamoyl] pyridin-2-yl}amino) methyl]-5-(propan- 2-yloxy)phenyl}-1H- pyrrolo[2,3-b] pyridine-5-carboxamide | US10030016, Example 4.1.3
Type:
Small organic molecule
Emp. Form.:
C34H32F2N6O3
Mol. Mass.:
610.6531
SMILES:
CC(C)Oc1cc(CNc2ncccc2C(=O)NCc2ccc(F)c(F)c2)cc(c1)-c1c[nH]c2ncc(cc12)C(=O)NC1CC1
Structure:
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