Strained contacts with the cell membrane may influence ligand affinity to G protein coupled receptors: a case of free fatty acid receptor 1 agonists

• Main Authors: Alexey Lukin (Author), Anna Bakholdina (Author), Mikhail Chudinov (Author), Oleksandra Onopchenko (Author), Elena Zhuravel (Author), Sergey Zozulya (Author), Maxim Gureev (Author), Mikhail Krasavin (Author)
• Format: Book
• Published: Taylor & Francis Group, 2021-01-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

A set of 1,3,4-thiadiazole-2-carboxamides bearing a substituted biphenyl in the amide portion was synthesised and tested for agonistic activity towards free fatty acid receptor 1 (FFA1). The observed activity trends were impossible to rationalised based solely on the docking energy scores of Glide S...