Ding_2021_Bioorg.Med.Chem_41_116216

Reference

Title : Discovery of soluble epoxide hydrolase inhibitors through DNA-encoded library technology (ELT) - Ding_2021_Bioorg.Med.Chem_41_116216
Author(s) : Ding Y , Belyanskaya S , DeLorey JL , Messer JA , Joseph Franklin G , Centrella PA , Morgan BA , Clark MA , Skinner SR , Dodson JW , Li P , Marino JP, Jr. , Israel DI
Ref : Bioorganic & Medicinal Chemistry , 41 :116216 , 2021
Abstract :

Inhibition of soluble epoxide hydrolase (sEH) has recently emerged as a new approach to treat cardiovascular disease and respiratory disease. Inhibitors based on 1,3,5-triazine chemotype were discovered through affinity selection against two triazine-based DNA-encoded libraries. The structure and activity relationship study led to the expansion of the original 1,4-cycloalkyl series to related aniline, piperidine, quinoline, aryl-ether and benzylic series. The 1,3-cycloalkyl chemotype led to the discovery of a clinical candidate (GSK2256294) for COPD.

PubMedSearch : Ding_2021_Bioorg.Med.Chem_41_116216
PubMedID: 34023664

Related information

Inhibitor GSK2256294A

Citations formats

Ding Y, Belyanskaya S, DeLorey JL, Messer JA, Joseph Franklin G, Centrella PA, Morgan BA, Clark MA, Skinner SR, Dodson JW, Li P, Marino JP, Jr., Israel DI (2021)
Discovery of soluble epoxide hydrolase inhibitors through DNA-encoded library technology (ELT)
Bioorganic & Medicinal Chemistry 41 :116216

Ding Y, Belyanskaya S, DeLorey JL, Messer JA, Joseph Franklin G, Centrella PA, Morgan BA, Clark MA, Skinner SR, Dodson JW, Li P, Marino JP, Jr., Israel DI (2021)
Bioorganic & Medicinal Chemistry 41 :116216