Related Experiment Videos
N-isonicotinoyl-(L)-4-aminophenylalanine derivatives as tight binding VLA-4 antagonists
George A Doherty1, Ginger X Yang, Edite Borges
1Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. george_doherty@merck.com
Bioorganic & Medicinal Chemistry Letters
|May 17, 2003
Abstract:
A series of isonicotinoyl-(L)-aminophenylalanine derivatives was prepared and evaluated as VLA-4 antagonists. These compounds exhibit subnanomolar binding affinity to VLA-4 and significant off-rates. The interplay between off-rate, protein binding and pharmacokinetics is discussed.