On-rate based optimization of structure –kinetic relationship – surfing the kinetic map

This article reviews various approaches to monitor SKR and suggests using the on-rate as the key monitoring parameter. The literature is reviewed and examples of compound series with low variability as well as with significant changes in on-rates are highlighted. Furthermore, findings of kinetic on-rate changes are presented and potential underlying rationales are discussed.
Source: Drug Discovery Today: Technologies - Category: Drugs & Pharmacology Source Type: research