. 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 4.

TTR FP and RBP4 SPA In Vitro Assay Data for Primary Carboxamide and Tetrazole TTR Tetramer Kinetic Stabilizer Analogues (Bottom-Group Region SAR)


compound	TTR FP^a IC₅₀ (μM)^d	RBP4 SPA^b IC₅₀ (μM)^d	RBP4–TTR HTRF^c IC₅₀ (μM)^d
14	0.22	>3	0.845
53	0.67	>3	ND^e
54	0.26	>3	9.58

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.

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

IC₅₀ values for the HTRF assay obtained in the presence of a 1 μM concentration of retinol.

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.

ND, not determined.