Lipophilic efficiency (LipE) is an important metric that has been increasingly applied in drug
discovery medicinal chemistry lead optimization programs. In this Perspective, using …

Herein, we discuss more than 50 cyclin-dependent kinase (CDK) inhibitors that have been
approved or have undergone clinical trials and their therapeutic application in multiple …

The majority of kinase inhibitors that have been developed so far—known as type I inhibitors—
target the ATP binding site of the kinase in its active conformation, in which the activation …

Aldehyde oxidase (AO, a EC 1.2. 3.1) has for many years been recognized as a
metabolizing enzyme contained within the cytosolic compartment of many tissues and in …

Introduction: Because of their important roles in disease and excellent 'druggability', kinases
have become the second largest drug target family. The great success of the BCR-ABL …

Protein kinase inhibitors are a well-established class of clinically useful drugs, particularly
for the treatment of cancer. Achieving inhibitor selectivity for particular protein kinases often …

Drug discovery is a complex and lengthy endeavor. 1 Many strategies exist to accelerate
target-to-clinical candidate selection, as well as to provide the highest quality candidate …

Kinase inhibitors that bind to the ATP cleft can be broadly classified into two groups: those
that bind exclusively to the ATP site with the kinase assuming a conformation otherwise …

Dieses für den deutschen Raum einzigartige Lehrbuch richtet sich an Studenten der
Pharmazie, Chemie und Biowissenschaften, aber auch an Quereinsteiger in Forschungs …

A series of amino acid ester prodrugs of the dual VEGFR-2/FGFR-1 kinase inhibitor 1 (BMS-
540215) was prepared in an effort to improve the aqueous solubility and oral bioavailability …