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 3.

RBP4 SPA Binding Affinity and RBP4 HTRF for Pyridine and Other Heteroaromatic Carboxylic Acid Analogues

graphic file with name nihms785212t14.jpg
Compound R RBP4 SPAa
IC50 (nM)c 		RBP4 HTRFb
IC50 (nM)c
33 graphic file with name nihms785212t15.jpg 12.8 ± 0.4 43.6 ± 10.5
48 graphic file with name nihms785212t16.jpg 14.1 295
49 graphic file with name nihms785212t17.jpg 53.3 228
50 graphic file with name nihms785212t18.jpg 584 4908
51 graphic file with name nihms785212t19.jpg >3000 ND
52 graphic file with name nihms785212t20.jpg 83.2 3956
53 graphic file with name nihms785212t21.jpg 68.4 2005
54 graphic file with name nihms785212t22.jpg 43.8 381
55 graphic file with name nihms785212t23.jpg 166 ND
56 graphic file with name nihms785212t24.jpg 23.0 437
57 graphic file with name nihms785212t25.jpg 29.3 495
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. ND = not determined.