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IV. Discovery of CXCR3 antagonists substituted with heterocycles as amide surrogates: improved PK, hERG and metabolic profiles.
Nair, Anilkumar G; Wong, Michael K C; Shu, Youheng; Jiang, Yueheng; Jenh, Chung-Her; Kim, Seong Heon; Yang, De-Yi; Zeng, Qingbei; Shao, Yuefei; Zawacki, Lisa Guise; Duo, Jingqi; McGuinness, Brian F; Carroll, Carolyn Diianni; Hobbs, Doug W; Shih, Neng-Yang; Rosenblum, Stuart B; Kozlowski, Joseph A.
Affiliation
  • Nair AG; Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. Electronic address: gopinadhan.anilkumar@Merck.com.
  • Wong MK; Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Shu Y; Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Jiang Y; Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Jenh CH; Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Kim SH; Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Yang DY; Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Zeng Q; Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Shao Y; Ligand Pharmaceuticals, 3000 Eastpark Boulevard, Cranbury, NJ 08512, USA.
  • Zawacki LG; Ligand Pharmaceuticals, 3000 Eastpark Boulevard, Cranbury, NJ 08512, USA.
  • Duo J; Ligand Pharmaceuticals, 3000 Eastpark Boulevard, Cranbury, NJ 08512, USA.
  • McGuinness BF; Ligand Pharmaceuticals, 3000 Eastpark Boulevard, Cranbury, NJ 08512, USA.
  • Carroll CD; Ligand Pharmaceuticals, 3000 Eastpark Boulevard, Cranbury, NJ 08512, USA.
  • Hobbs DW; Ligand Pharmaceuticals, 3000 Eastpark Boulevard, Cranbury, NJ 08512, USA.
  • Shih NY; Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Rosenblum SB; Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Kozlowski JA; Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
Bioorg Med Chem Lett ; 24(4): 1085-8, 2014 Feb 15.
Article in En | MEDLINE | ID: mdl-24486132
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Full text: 1 Database: MEDLINE Main subject: Ether-A-Go-Go Potassium Channels / Receptors, CXCR3 / Drug Discovery / Amides / Heterocyclic Compounds Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2014 Type: Article
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Full text: 1 Database: MEDLINE Main subject: Ether-A-Go-Go Potassium Channels / Receptors, CXCR3 / Drug Discovery / Amides / Heterocyclic Compounds Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2014 Type: Article