pmid: 31752557,   nlmid 101150203,  doi:10.1080/14756366.2019.1693556

Further validation of strecker-type ?-aminonitriles as a new class of potent human carbonic anhydrase II inhibitors: hit expansion within the public domain using differential scanning fluorimetry leads to chemotype refinement.

Krasavin, Mikhail Kalinin, Stanislav Zozulya, Sergey Griniukova, Anastasia Borysko, Petro Angeli, Andrea Supuran, Claudiu T

Vol. 35, Issue 35, Dec.2020

Journal of enzyme inhibition and medicinal chemistry (J Enzyme Inhib Med Chem),  ISSN 1475-6374


Testing of an expanded, 800-compound set of analogues of the earlier described Strecker-type ?-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. [Formula: see text].

MESH Headings

Article Keywords

Differential scanning fluorimetry | carbonic anhydrase II | protein affinity | thermal shift assay |


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