Table 3.

Derived pA₂/pK_B values of erenumab antagonising αCGRP, βCGRP, and amylin in Cos7 cells transfected with the CGRP or AMY₁ receptors.

Cos7 cells	CGRP receptor		AMY1 receptor
Agonist	αCGRP	βCGRP	αCGRP	βCGRP	Amylin
n	5	5	5	6	6
Schild analysis	9.04 ± 0.19	8.65 ± 0.13	7.04 ± 0.22*	6.61 ± 0.13^	6.64 ±0.13
Lew and Angus	9.11 ± 0.17	8.71 ± 0.14	7.06 ± 0.22*	6.63 ± 0.12^	6.62 ± 0.14
Global Gaddum-Schild	8.63 ± 0.37	8.22 ± 0.34	6.68 ± 0.27*	6.74 ± 0.28^	6.59 ± 0.15

Data are the mean ± SEM of n independent experiments. Data are pK_B in all cases except for αCGRP at the CGRP and AMY₁ receptors and βCGRP at the CGRP receptor analysed through global Gaddum-Schild analysis which is pA₂ (apparent pK_B); the Schild slope had a statistically significant difference from one through this analytical method (slopes of 1.64 ± 0.27 [n=5] and 1.64 ± 0.03 [n=5] for αCGRP at CGRP and AMY₁ receptor, respectively, and 2.08 ± 0.69 [n=6] for βCGRP at the CGRP receptor) meaning that the reported value is an estimate of the pK_B. The potency of erenumab against αCGRP was compared between the CGRP and AMY₁ receptors by Student’s t-test. The same analysis was used when comparing βCGRP at the CGRP and AMY₁ receptors, and when comparing αCGRP and βCGRP at the CGRP receptor. When comparing data from the AMY₁ receptor, one-way ANOVA was used; this did not reach statistical significance and thus no post-hoc test was performed. Statistical significance from αCGRP at the CGRP receptor indicated by * (asterisk), statistical significance from βCGRP at the CGRP receptor indicated by ^ (caret). The unequal number of n was due to performing some experiments before testing our Cos7 cells for endogenous receptor expression and so additional experiments were conducted to determine the level of influence that this might have on our curve fits.