Ontology highlight
ABSTRACT:
SUBMITTER: Dockendorff C
PROVIDER: S-EPMC3297361 | biostudies-literature | 2012 Mar
REPOSITORIES: biostudies-literature
Dockendorff Chris C Aisiku Omozuanvbo O Verplank Lynn L Dilks James R JR Smith Daniel A DA Gunnink Susanna F SF Dowal Louisa L Negri Joseph J Palmer Michelle M Macpherson Lawrence L Schreiber Stuart L SL Flaumenhaft Robert R
ACS medicinal chemistry letters 20120130 3
A high-throughput screen of the NIH-MLSMR compound collection, along with a series of secondary assays to identify potential targets of hit compounds, previously identified a 1,3-diaminobenzene scaffold that targets protease-activated receptor 1 (PAR1). We now report additional structure-activity relationship (SAR) studies that delineate the requirements for activity at PAR1 and identify plasma-stable analogues with nanomolar inhibition of PAR1-mediated platelet activation. Compound 4 was declar ...[more]