Investigating the Structure–Activity Relationship of 1,2,4-Triazine G-Protein-Coupled Receptor 84 (GPR84) Antagonists
Amit Mahindra, Laura Jenkins, Sara Marsango, Mark Huggett, Margaret Huggett, Lindsay E. Robinson, Jonathan Gillespie, Muralikrishnan Rajamanickam, Angus J. Morrison, Stuart P. McElroy, Irina G. Tikhonova, Graeme Milligan, Andrew G. Jamieson
Abstract
is a potent GPR84 antagonist with a favorable pharmacokinetic (PK) profile suitable for further drug development.
Topics & Concepts
ChemistryAntagonistPharmacologyAgonistCompetitive antagonistReceptorG protein-coupled receptorDocking (animal)Partial agonistBiochemistryBiologyMedicineNursingReceptor Mechanisms and SignalingMonoclonal and Polyclonal Antibodies ResearchAdenosine and Purinergic Signaling