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 4.

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

graphic file with name nihms785212t26.jpg
Compound R RBP4 SPAa
IC50 (nM)c 		RBP4 HTRFb
IC50 (nM)c
33 graphic file with name nihms785212t27.jpg 12.8 ± 0.4 43.6 ± 10.5
61 graphic file with name nihms785212t28.jpg 46.3 ± 1.1 33.4 ± 1.8
62 graphic file with name nihms785212t29.jpg 196 ND
63 graphic file with name nihms785212t30.jpg 532 ± 198 347
64 graphic file with name nihms785212t31.jpg 137 504
65 graphic file with name nihms785212t32.jpg 51.8 ± 1.5 821 ± 142
66 graphic file with name nihms785212t33.jpg 31.1 ± 1.9 719 ± 22.4
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.