Discovery of 9-Cyclopropylethynyl-2-((
Acetates
/ chemistry
Allosteric Regulation
/ drug effects
Animals
Caco-2 Cells
Cells, Cultured
Dogs
Drug Discovery
/ methods
Drug Evaluation, Preclinical
/ methods
Female
HEK293 Cells
Humans
Male
Mice
Mice, Inbred BALB C
Microsomes, Liver
/ drug effects
Rats
Rats, Sprague-Dawley
Receptors, G-Protein-Coupled
/ antagonists & inhibitors
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:
25 11 2020
25 11 2020
Historique:
pubmed:
10
9
2020
medline:
1
1
2021
entrez:
9
9
2020
Statut:
ppublish
Résumé
GPR84 is a medium chain free fatty acid-binding G-protein-coupled receptor associated with inflammatory and fibrotic diseases. As the only reported antagonist of GPR84 (PBI-4050) that displays relatively low potency and selectivity, a clear need exists for an improved modulator. Structural optimization of GPR84 antagonist hit
Identifiants
pubmed: 32902984
doi: 10.1021/acs.jmedchem.0c00272
doi:
Substances chimiques
Acetates
0
GPR84 protein, human
0
Receptors, G-Protein-Coupled
0
setogepram
879OVM0Y1S
Types de publication
Clinical Trial, Phase II
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM