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. 2019 Nov 19;62(24):11035–11053. doi: 10.1021/acs.jmedchem.9b00742

Figure 2.

Figure 2

Characterization of ligands in U2OS-CCR2 and U2OS-CCR5. (a) [3H]-CCR2-RA-[R] displacement by increasing concentrations of triazolopyrimidinone derivatives 8, 39, and 43 in U2OS-CCR2 at 25 °C. Data are normalized to specific binding in the absence of compound (set as 100%). (b) Inhibition of CCL2-stimulated β-arrestin recruitment in U2OS-CCR2 by increasing concentrations of compounds 8, 39, and 43, after stimulation with an EC80 concentration of CCL2 (set as 100%). (c) Inhibition of CCL3-stimulated β-arrestin recruitment in U2OS-CCR5 by increasing concentrations of compounds 8, 39, and 43, after stimulation with an EC80 concentration of CCL3 (set as 100%). All data are from single, representative experiments performed in duplicate.