Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: EC:2.7.11.2 (
PDK1
)
2,238
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
In this
Letter
is described the structure-based design of potent dihydro-pyrazoloquinazolines as
PDK1
inhibitors. Starting from low potency HTS hits with the aid of X-ray crystallography and modeling, a medicinal chemistry activity was carried out to improve potency versus
PDK1
and selectivity versus CDK2 protein kinase.
...
PMID:Structure-based optimization of potent PDK1 inhibitors. 2062 25
