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[Preprint]. 2024 Mar 11:2023.09.09.557002. Originally published 2023 Sep 12. [Version 2] doi: 10.1101/2023.09.09.557002

Figure 4: Medicinal chemistry leads to novel CFTR potentiators and inhibitors.

Figure 4:

(a) General formula of newly synthesized ‘853 analogs. (b) Effects of ‘853 analogs on currents measured in inside-out excised membrane patches containing fully phosphorylated WT CFTR. Measurements were made with 3 mM ATP. Data represent means and SEs of 2 to 46 patches. (c) The structures and dose-response curves of three of the most efficacious potentiators. Data represent means and SEs of 5–11 patches. (d) The structures and dose-response curves of the two most efficacious inhibitors. The dose-responses of the Y304A and S308A variants in response to I1412 perfusion were also shown (left). Data represent means and SEs of 2–8 patches.