Ontology highlight
ABSTRACT:
SUBMITTER: Kothiwale S
PROVIDER: S-EPMC6151389 | biostudies-literature | 2017 Sep
REPOSITORIES: biostudies-literature
Kothiwale Sandeepkumar S Borza Corina C Pozzi Ambra A Meiler Jens J
Molecules (Basel, Switzerland) 20170919 9
The discovery of selective inhibitors of biological target proteins is the primary goal of many drug discovery campaigns. However, this goal has proven elusive, especially for inhibitors targeting the well-conserved orthosteric adenosine triphosphate (ATP) binding pocket of kinase enzymes. The human kinome is large and it is rather difficult to profile early lead compounds against around 500 targets to gain an upfront knowledge on selectivity. Further, selectivity can change drastically during d ...[more]