2. Academic Validation
  3. Scaffold hopping and optimization towards libraries of glycogen synthase kinase-3 inhibitors

Scaffold hopping and optimization towards libraries of glycogen synthase kinase-3 inhibitors

  • Bioorg Med Chem Lett. 2002 Jun 3;12(11):1525-8. doi: 10.1016/s0960-894x(02)00169-5.
Lars Naerum 1,  Leif Nørskov-Lauritsen,  Preben H Olesen
Affiliations

Affiliation

  • 1 Medicinal Chemistry Research, Novo Nordisk A/S, Novo Nordisk Park, DK-2760 Måløv, Denmark.
PMID: 12031334 DOI: 10.1016/s0960-894x(02)00169-5
Abstract

Using a virtual screening strategy based on a methodology derived from the CATS molecular descriptor, a novel compound class with inhibitory activity against the GSK-3 Enzyme was identified through scaffold hopping. These compounds were readily synthesized, either by solid-phase or solution-phase chemistry. Compounds with inhibitory activity below 1 microM were identified.

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