Skip to main content
. Author manuscript; available in PMC: 2016 Jun 10.
Published in final edited form as: J Med Chem. 2015 Aug 4;58(15):5863–5888. doi: 10.1021/acs.jmedchem.5b00423

Table 1.

RBP4 SPA Binding Affinity, RBP4 HTRF, and Liver Microsomal Stability Data for 6-Methylpyrimidine-4-carboxylic Acid and Methyl Ester Analogues

graphic file with name nihms785212t1.jpg
microsomal stability (% remaining)
compd RBP4 SPAa IC50 (nM)c RBP4 HTRFb IC50 (nM)c HLMd RLMe
3 15.0 ± 0.005 122 ± 0.035 3 85
4 72.7 294 100 75
9 4.1 132 ND ND
10 35.3 188 68 96
13 9.7 1402 0.0 0.0
14 89.5 511 18 63
17 3.9 74.0 ND ND
18 57.4 140 80 76
28 6.3 100 0.2 9.8
33 12.8 ± 0.4 43.6 ± 10.5 94 93
a

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

b

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

c

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

d

HLM = human liver microsomes.

e

RLM = rat liver microsomes. Compound concentration was 10 µM, and incubation time with either human or rat microsomes was 30 min. ND = not determined.