Ontology highlight
ABSTRACT:
SUBMITTER: Kerns JK
PROVIDER: S-EPMC6295857 | biostudies-literature | 2018 Dec
REPOSITORIES: biostudies-literature
Kerns Jeffrey K JK Busch-Petersen Jakob J Fu Wei W Boehm Jeffrey C JC Nie Hong H Muratore Michael M Bullion Ann A Lin Guoliang G Li Huijie H Davis Roderick R Lin Xichen X Lakdawala Ami S AS Cousins Rick R Field Rita R Payne Jeremy J Miller David D DD Bamborough Paul P Christopher John A JA Baldwin Ian I Osborn Ruth R RR Yonchuk John J Webb Edward E Rumsey William L WL
ACS medicinal chemistry letters 20181030 12
IκB kinase β (IKKβ or IKK2) is a key regulator of nuclear factor kappa B (NF-κB) and has received attention as a therapeutic target. Herein we report on the optimization of a series of 3,5-disubstituted-indole-7-carboxamides for oral activity. In doing so, we focused attention on potency, ligand efficiency (LE), and physicochemical properties and have identified compounds <b>24</b> and (<i>R</i>)-<b>28</b> as having robust in vivo activity. ...[more]