2. Academic Validation
  3. Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor

Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor

  • Bioorg Med Chem Lett. 1998 Mar 17;8(6):631-4. doi: 10.1016/s0960-894x(98)00079-1.
Y S Oh 1,  M Yun,  S Y Hwang,  S Hong,  Y Shin,  K Lee,  K H Yoon,  Y J Yoo,  D S Kim,  S H Lee,  Y H Lee,  H D Park,  C H Lee,  S K Lee,  S Kim
Affiliations

Affiliation

  • 1 Biotech Research Institute, LG Chemical LTD, Taejon, Korea.
PMID: 9871573 DOI: 10.1016/s0960-894x(98)00079-1
Abstract

Systematic variation of the so-called P-pocket moiety of benzamidrazone-based selective Thrombin inhibitors led to the discovery of LB30057. It is potent (Ki = 0.38 nM for human Thrombin), selective (Ki = 3290 nM for bovine trypsin), and orally bioavailable (58% oral bioavailability in dogs). LB30057 was efficacious in thrombosis animal models.

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