865110-84-5Relevant articles and documents
Discovery of N-{N-[(3-cyanophenyl)sulfonyl]-4(R)-cyclobutylamino-(L)- prolyl}-4-[(3′,5′-dichloroisonicotinoyl)amino]-(L)-phenylalanine (MK-0668), an extremely potent and orally active antagonist of very late antigen-4
Lin, Linus S.,Lanza Jr., Thomas,Jewell, James P.,Liu, Ping,Jones, Carrie,Kieczykowski, Gerard R.,Treonze, Kelly,Si, Qian,Manior, Salony,Koo, Gloria,Tong, Xinchun,Wang, Junying,Schuelke, Anne,Pivnichny, James,Wang, Regina,Raab, Conrad,Vincent, Stella,Davies, Philip,MacCoss, Malcolm,Mumford, Richard A.,Hagmann, William K.
supporting information; experimental part, p. 3449 - 3452 (2010/03/25)
Extremely potent very late antigen-4 (VLA-4) antagonists with picomolar, whole blood activity and slow dissociation rates were discovered by incorporating an amino substituent on the proline fragment of the initial lead structure. This level of potency ag