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. 2020 Feb 12;177(8):1917–1930. doi: 10.1111/bph.14961

Figure 3.

Figure 3

7TM and ECL mutations alter the affinity and cooperativity of CaS receptor NAMs. An operational model of allosterism (Equation 1) was fitted to concentration–response curves to Ca2+ o in the absence and the presence of each NAM determined in Ca2+ i mobilisation assays 1 to determine the change in NAM affinity (ΔpK B) and cooperativity (ΔLogαβ) at mutant CaS receptors in comparison to the WT receptor. White bars represent no significant change in pK B or Logαβ. Coloured bars that sit above and below zero represent a greater than twofold increase (light teal), greater than fivefold increase (dark blue), greater than twofold decrease (yellow), or greater than fivefold decrease (orange) significant change in pK B or Logαβ, respectively. Data are the ΔpK B or ΔLogαβ + SEM calculated from WT and mutant pK B or Logαβ values and experiment numbers shown in Table 1. *P < .05, significantly different from WT; one way ANOVA with Dunnett's multiple comparisons post test. NA refers to values that are not applicable or could not be accurately determined. For Y825A treated with Pfizer compound 1, the increase in Logαβ was too great to be accurately determined