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Page 1
A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists.
Hale JJ, Lynch CL, Neway W, Mills SG, Hajdu R, Keohane CA, Rosenbach MJ, Milligan JA, Shei GJ, Parent SA, Chrebet G, Bergstrom J, Card D, Ferrer M, Hodder P, Strulovici B, Rosen H, Mandala S. Hale JJ, et al. Among authors: chrebet g. J Med Chem. 2004 Dec 30;47(27):6662-5. doi: 10.1021/jm0492507. J Med Chem. 2004. PMID: 15615513
Highly selective and potent agonists of sphingosine-1-phosphate 1 (S1P1) receptor.
Vachal P, Toth LM, Hale JJ, Yan L, Mills SG, Chrebet GL, Koehane CA, Hajdu R, Milligan JA, Rosenbach MJ, Mandala S. Vachal P, et al. Among authors: chrebet gl. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3684-7. doi: 10.1016/j.bmcl.2006.04.064. Epub 2006 May 6. Bioorg Med Chem Lett. 2006. PMID: 16682185
Discovery of potent 3,5-diphenyl-1,2,4-oxadiazole sphingosine-1-phosphate-1 (S1P1) receptor agonists with exceptional selectivity against S1P2 and S1P3.
Li Z, Chen W, Hale JJ, Lynch CL, Mills SG, Hajdu R, Keohane CA, Rosenbach MJ, Milligan JA, Shei GJ, Chrebet G, Parent SA, Bergstrom J, Card D, Forrest M, Quackenbush EJ, Wickham LA, Vargas H, Evans RM, Rosen H, Mandala S. Li Z, et al. Among authors: chrebet g. J Med Chem. 2005 Oct 6;48(20):6169-73. doi: 10.1021/jm0503244. J Med Chem. 2005. PMID: 16190743
Discovery of 3-arylpropionic acids as potent agonists of sphingosine-1-phosphate receptor-1 (S1P1) with high selectivity against all other known S1P receptor subtypes.
Yan L, Huo P, Doherty G, Toth L, Hale JJ, Mills SG, Hajdu R, Keohane CA, Rosenbach MJ, Milligan JA, Shei GJ, Chrebet G, Bergstrom J, Card D, Quackenbush E, Wickham A, Mandala SM. Yan L, et al. Among authors: chrebet g. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3679-83. doi: 10.1016/j.bmcl.2006.04.084. Epub 2006 May 11. Bioorg Med Chem Lett. 2006. PMID: 16697189
SAR studies of 3-arylpropionic acids as potent and selective agonists of sphingosine-1-phosphate receptor-1 (S1P1) with enhanced pharmacokinetic properties.
Yan L, Huo P, Hale JJ, Mills SG, Hajdu R, Keohane CA, Rosenbach MJ, Milligan JA, Shei GJ, Chrebet G, Bergstrom J, Card D, Mandala SM. Yan L, et al. Among authors: chrebet g. Bioorg Med Chem Lett. 2007 Feb 1;17(3):828-31. doi: 10.1016/j.bmcl.2006.10.057. Epub 2006 Oct 25. Bioorg Med Chem Lett. 2007. PMID: 17092714
Identification of Leu276 of the S1P1 receptor and Phe263 of the S1P3 receptor in interaction with receptor specific agonists by molecular modeling, site-directed mutagenesis, and affinity studies.
Deng Q, Clemas JA, Chrebet G, Fischer P, Hale JJ, Li Z, Mills SG, Bergstrom J, Mandala S, Mosley R, Parent SA. Deng Q, et al. Among authors: chrebet g. Mol Pharmacol. 2007 Mar;71(3):724-35. doi: 10.1124/mol.106.029223. Epub 2006 Dec 14. Mol Pharmacol. 2007. PMID: 17170199
The discovery of 3-(N-alkyl)aminopropylphosphonic acids as potent S1P receptor agonists.
Hale JJ, Doherty G, Toth L, Li Z, Mills SG, Hajdu R, Ann Keohane C, Rosenbach M, Milligan J, Shei GJ, Chrebet G, Bergstrom J, Card D, Rosen H, Mandala S. Hale JJ, et al. Among authors: chrebet g. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3495-9. doi: 10.1016/j.bmcl.2004.04.069. Bioorg Med Chem Lett. 2004. PMID: 15177460
20 results