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. 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 2.

RBP4 SPA Binding Affinity and RBP4 HTRF for Pyrimidine Carboxylic Acid Analogues

graphic file with name nihms785212t2.jpg
Compound R RBP4 SPAa
IC50 (nM)c 		RBP4 HTRFb
IC50 (nM)c
33 graphic file with name nihms785212t3.jpg 12.8 ± 0.4 43.6 ± 10.5
32 graphic file with name nihms785212t4.jpg 20.8 ± 0.5 79.7
34 graphic file with name nihms785212t5.jpg 9.6 88.0
35 graphic file with name nihms785212t6.jpg 12.8 ± 1.6 81.2 ± 7.6
36 graphic file with name nihms785212t7.jpg 153 ± 0.6 202
41 graphic file with name nihms785212t8.jpg 48.8 123
42 graphic file with name nihms785212t9.jpg 90.1 595
43 graphic file with name nihms785212t10.jpg 40.8 523
44 graphic file with name nihms785212t11.jpg 171 1864
46 graphic file with name nihms785212t12.jpg 3.3 248
47 graphic file with name nihms785212t13.jpg 7.5 175
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.