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Bioorg Med Chem Lett. 2003 Jun 2;13(11):1891-5.

N-isonicotinoyl-(L)-4-aminophenylalanine derivatives as tight binding VLA-4 antagonists.

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. george_doherty@merck.com

Erratum in

  • Bioorg Med Chem Lett. 2003 Sep 1;13(17):2937-8.

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.

PMID:
12749892
DOI:
10.1016/s0960-894x(03)00308-1
[Indexed for MEDLINE]

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