TABLE 1

Effects of mutation of negatively charged residues in CXCR3 on protein expression, CXCL11 binding, and affinities of small-molecule CXCR3 antagonists VUF11211 and NBI-74330

Overview of both total receptor expression levels determined using whole cell–based ELISA, and affinity data for the three compounds. The latter was generated by performing [¹²⁵I]CXCL11 radioligand displacement binding studies on membranes prepared from HEK293T cells transiently expressing CXCR3 WT or mutants. Values are presented as the mean ± S.E.M. from at least three individual experiments. The Ballesteros–Weinstein residue numbers are indicated in superscript for residues in TM helices, whereas the numbering scheme proposed by de Graaf and colleagues is used to enumerate residues in EL2 (Ballesteros and Weinstein, 1995; de Graaf et al., 2008).