Structure-Based Design and Preclinical Characterization of Selective and Orally Bioavailable Factor XIa Inhibitors: Demonstrating the Power of an Integrated S1 Protease Family Approach.
Journal
Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531
Informations de publication
Date de publication:
13 08 2020
13 08 2020
Historique:
pubmed:
20
6
2020
medline:
26
11
2020
entrez:
20
6
2020
Statut:
ppublish
Résumé
The serine protease factor XI (FXI) is a prominent drug target as it holds promise to deliver efficacious anticoagulation without an enhanced risk of major bleeds. Several efforts have been described targeting the active form of the enzyme, FXIa. Herein, we disclose our efforts to identify potent, selective, and orally bioavailable inhibitors of FXIa. Compound
Identifiants
pubmed: 32551603
doi: 10.1021/acs.jmedchem.0c00279
doi:
Substances chimiques
Factor Xa Inhibitors
0
Factor XIa
EC 3.4.21.27
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM