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. Author manuscript; available in PMC: 2023 May 20.
Published in final edited form as: ACS Chem Biol. 2022 Apr 13;17(5):1249–1258. doi: 10.1021/acschembio.2c00175

Table 2.

Agonist activities of the fatty diacid-modified stapled DA4 analogs

Agonist activity (nM)
Name Stapler structure GLP-1R GIPR
DA4-Bph-OH a graphic file with name nihms-1835324-t0002.jpg 0.98 0.42
DA4-Bpp-OH b graphic file with name nihms-1835324-t0003.jpg 0.64 0.21
DA4-Bph-C10 c graphic file with name nihms-1835324-t0004.jpg 1.45 0.15
DA4-Bph-C18-isomer1 graphic file with name nihms-1835324-t0005.jpg 25.43 2.13
DA4-Bph-C18-isomer2 graphic file with name nihms-1835324-t0006.jpg 14.31 1.80
DA4-Bpp-C10-isomer1 graphic file with name nihms-1835324-t0007.jpg 0.14 0.07
DA4-Bpp-C10-isomer2 graphic file with name nihms-1835324-t0008.jpg 0.25 0.11
DA4-Bpp-C18-isomer1 graphic file with name nihms-1835324-t0009.jpg 2.04 0.48
DA4-Bpp-C18-isomer2 graphic file with name nihms-1835324-t0010.jpg 2.29 0.70
a, b, c

DA4-Bph-OH, DA4-Bpp-OH, and DA4-Bph-C10 were used as a mixture of regioisomers.