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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 3.

TTR FP and RBP4 SPA In Vitro Assay Data for TTR Tetramer Kinetic Stabilizer Analogues Bearing 3,5-Dimethyl-1H-pyrazole Replacements (Head Group Region SAR)

graphic file with name nihms-1842229-t0015.jpg
Compound Head Group (R) TTR FPa
IC50 (μM)c 		RBP4 SPAb
IC50 (μM)c
14 graphic file with name nihms-1842229-t0016.jpg 0.22 >3
46 graphic file with name nihms-1842229-t0017.jpg 5.3 >3
48 graphic file with name nihms-1842229-t0018.jpg >30 >3
50 graphic file with name nihms-1842229-t0019.jpg 1.7 >3
52 graphic file with name nihms-1842229-t0020.jpg >30 >30
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.