Referenced in: none

Automatically associated channels: Kv11.1

Title: Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate.

Authors: Christian Harcken, Doris Riether, Pingrong Liu, Hossein Razavi, Usha Patel, Thomas Lee, Todd Bosanac, Yancey Ward, Mark Ralph, Zhidong Chen, Donald Souza, Richard M Nelson, Alison Kukulka, Tazmeen N Fadra-Khan, Ljiljana Zuvela-Jelaska, Mita Patel, David S Thomson, Gerald H Nabozny

Journal, date & volume: ACS Med Chem Lett, 2014 Dec 11 , 5, 1318-23

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/25516791

Abstract
A series of nonsteroidal "dissociated" glucocorticoid receptor agonists was optimized for drug-like properties such as cytochrome P450 inhibition, metabolic stability, aqueous solubility, and hERG ion channel inhibition. This effort culminated in the identification of the clinical candidate compound ( R )-39.