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. 2020 Dec 3;10(12):1634. doi: 10.3390/biom10121634

Figure 4.

Figure 4

pA2 determination of LTD4-induced IP1 production of BRI-12359. Inhibition of LTD4-induced IP1 production by selected compounds (fixed concentration of LTD4). Experiments were performed in HEK293 cells transiently expressing the wild-type CysLT1R (a) or CysLT2R (b). Curves correspond to normalized data; values from non-stimulated cells were set as 0% IP1 production and those from cells stimulated with LTD4 were set as 100% IP1 production. Schild analysis revealed that the pA2 values for compound BRI-12359 are 6.5 ± 0.1 and 4.0 ± 0.2 (KB = 0.34 ± 0.09 µM and 105 ± 37 µM) for the CysLT1R-WT and CysLT2R-WT, respectively. Data represent mean ± SEM of three independent experiments, tested in quadruplicate. NS = non-stimulated.