Ontology highlight
ABSTRACT:
SUBMITTER: Skora L
PROVIDER: S-EPMC5467191 | biostudies-literature | 2017 Jun
REPOSITORIES: biostudies-literature
Skora Lukasz L Jahnke Wolfgang W
ACS medicinal chemistry letters 20170406 6
In modern kinase drug discovery, allosteric inhibitors have become a focus of attention due to their potential selectivity, but such compounds are difficult to identify. Here we describe an NMR-based competition assay using <sup>19</sup>F-containing reporter molecules, which allows for rapid identification and discrimination between ATP-competitive and allosteric kinase inhibitors. We illustrate the principle of such a dual-site competition assay with the example of catalytic and allosteric ABL1 ...[more]