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N-Isonicotinoyl-( l)-4-aminophenylalanine derivatives as tight binding VLA-4 antagonists

Doherty, George A ; Yang, Ginger X ; Borges, Edite ; Tong, Sharon ; Mccauley, Ermengilda D ; Treonz, Kelly M ; Van Riper, Gail ; Pacholok, Stephen ; Si, Qian ; Koo, Gloria C ; Shah, Kashmira ; Mumford, Richard A ; Hagmann, William K

Bioorganic & Medicinal Chemistry Letters, 2003, Vol.13(11), pp.1891-1895 [Peer Reviewed Journal]

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Title:
N-Isonicotinoyl-( l)-4-aminophenylalanine derivatives as tight binding VLA-4 antagonists
Author: Doherty, George A ; Yang, Ginger X ; Borges, Edite ; Tong, Sharon ; Mccauley, Ermengilda D ; Treonz, Kelly M ; Van Riper, Gail ; Pacholok, Stephen ; Si, Qian ; Koo, Gloria C ; Shah, Kashmira ; Mumford, Richard A ; Hagmann, William K
Description: 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.
Is Part Of: Bioorganic & Medicinal Chemistry Letters, 2003, Vol.13(11), pp.1891-1895
Identifier: ISSN: 0960-894X ; E-ISSN: 1464-3405 ; DOI: 10.1016/S0960-894X(03)00308-1
Subjects: Medicine ; Chemistry ; Anatomy & Physiology
Language: English

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