Exploring & Exploiting Allosteric Inhibitors & Covalent Inhibitors

In this application note, Discoverx determine the binding constant (Kd) for the non-ATP-competitive inhibitor BMS-345541 against IKK-beta. They also analyse the Kd of slowly dissociating inhibitors in comparison to irreversible inhibitors. Target selectivity remains a common challenge in small molecule kinase drug development and has led to multiple different approaches to developing more selective compounds.