Abstract:
: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 24 and (R)-28 as having robust in vivo activity.
journal_name
ACS Med Chem Lettjournal_title
ACS medicinal chemistry lettersauthors
Kerns JK,Busch-Petersen J,Fu W,Boehm JC,Nie H,Muratore M,Bullion A,Lin G,Li H,Davis R,Lin X,Lakdawala AS,Cousins R,Field R,Payne J,Miller DD,Bamborough P,Christopher JA,Baldwin I,Osborn RR,Yonchuk J,Webb E,Rumdoi
10.1021/acsmedchemlett.8b00291subject
Has Abstractpub_date
2018-10-30 00:00:00pages
1164-1169issue
12issn
1948-5875journal_volume
9pub_type
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