Ontology highlight
ABSTRACT:
SUBMITTER: Frankowski KJ
PROVIDER: S-EPMC3378255 | biostudies-literature | 2012 Mar
REPOSITORIES: biostudies-literature
Frankowski Kevin J KJ Hedrick Michael P MP Gosalia Palak P Li Kelin K Shi Shenghua S Whipple David D Ghosh Partha P Prisinzano Thomas E TE Schoenen Frank J FJ Su Ying Y Vasile S S Sergienko Eduard E Gray Wilson W Hariharan Santosh S Milan Loribelle L Heynen-Genel Susanne S Mangravita-Novo Arianna A Vicchiarelli Michael M Smith Layton H LH Streicher John M JM Caron Marc G MG Barak Lawrence S LS Bohn Laura M LM Chung Thomas D Y TD Aubé Jeffrey J
ACS chemical neuroscience 20120120 3
Herein we present the outcome of a high throughput screening (HTS) campaign-based strategy for the rapid identification and optimization of selective and general chemotypes for both kappa (κ) opioid receptor (KOR) activation and inhibition. In this program, we have developed potent antagonists (IC(50) < 120 nM) or agonists of high binding affinity (K(i) < 3 nM). In contrast to many important KOR ligands, the compounds presented here are highly modular, readily synthesized and, in most cases, ach ...[more]