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. Author manuscript; available in PMC: 2022 Oct 18.
Published in final edited form as: J Med Chem. 2021 Jun 17;64(13):9010–9041. doi: 10.1021/acs.jmedchem.1c00099

Table 2.

TTR FP and RBP4 SPA In Vitro Assay Data for Conformationally Constrained Piperazine Isostere TTR Tetramer Kinetic Stabilizer Analogues (Core Scaffold Region SAR)

graphic file with name nihms-1842229-t0014.jpg
compound TTR FPa IC50 (μM)c RBP4 SPAb IC50 (μM)c
14 0.22 >3
32 2.82 >3
(±)−38 1.08 >3
44 >30 >3
a

IC50 values for the TTR FP assay obtained in the presence of a fixed, 25 μM concentration of fluorescein isothiocyanate (FITC)-coupled TTR FP probe.

b

IC50 values for the RBP4 SPA assay obtained in the presence of a fixed, 10 nM concentration of 3H-retinol.

c

For compounds tested multiple times (more than twice), the IC50 data is represented as the mean ± standard deviation. For those compounds that were only tested twice, the IC50 data is shown as the mean of two independent experiments and not as the mean ± standard deviation.