Testing of an expanded, 800-compound set of analogues of the earlier described Strecker-type alpha-aminonitriles (selected from publicly available Enamine Ltd. Screening Collection) in thermal shift assay against bovine carbonic anhydrase (bCA) led to further validation of this new class of inhibitors and identification a new, refined chemotype represented by inhibitors with 10-improved potency.


Original languageEnglish
Pages (from-to)165-171
Number of pages7
JournalJournal of Enzyme Inhibition and Medicinal Chemistry
Volume35
Issue number1
Early online date22 Nov 2019
DOIs
StatePublished - 1 Jan 2020

    Scopus subject areas

  • Drug Discovery
  • Pharmacology

    Research areas

  • Differential scanning fluorimetry, thermal shift assay, protein affinity, carbonic anhydrase II, AFFINITY, DESIGN, SITE, Humans, Structure-Activity Relationship, Fluorometry, Dose-Response Relationship, Drug, Animals, Nitriles/chemical synthesis, Carbonic Anhydrase Inhibitors/chemical synthesis, Cattle, Molecular Structure, Carbonic Anhydrase II/antagonists & inhibitors, Drug Evaluation, Preclinical

ID: 49497360