2. Academic Validation
  3. Fragment-based discovery of hepatitis C virus NS5b RNA polymerase inhibitors

Fragment-based discovery of hepatitis C virus NS5b RNA polymerase inhibitors

  • Bioorg Med Chem Lett. 2008 May 1;18(9):2990-5. doi: 10.1016/j.bmcl.2008.03.056.
Stephen S Antonysamy 1,  Brandon Aubol,  Jeff Blaney,  Michelle F Browner,  Anthony M Giannetti,  Seth F Harris,  Normand Hébert,  Jörg Hendle,  Stephanie Hopkins,  Elizabeth Jefferson,  Charles Kissinger,  Vincent Leveque,  David Marciano,  Ethel McGee,  Isabel Nájera,  Brian Nolan,  Masaki Tomimoto,  Eduardo Torres,  Tobi Wright
Affiliations

Affiliation

  • 1 Medicinal Chemistry, SGX Pharmaceuticals, Inc., 10505 Roselle Street, San Diego, CA 92121, USA.
PMID: 18400495 DOI: 10.1016/j.bmcl.2008.03.056
Abstract

Non-nucleoside inhibitors of HCV NS5b RNA polymerase were discovered by a fragment-based lead discovery approach, beginning with crystallographic fragment screening. The NS5b binding affinity and biochemical activity of fragment hits and inhibitors was determined by surface plasmon resonance (Biacore) and an Enzyme inhibition assay, respectively. Crystallographic fragment screening hits with approximately 1-10mM binding affinity (K(D)) were iteratively optimized to give leads with approximately 200nM biochemical activity and low microM cellular activity in a Replicon assay.

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