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. 2012 Jul;140(1):17–28. doi: 10.1085/jgp.201210801

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© 2012 Jadey and Auerbach

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Figure 4. — Affinity–efficacy correlation for agonists. (A) The probability of being open within a cluster (P_o) versus agonist concentration. Agonists with higher maximum P_o values have lower EC₅₀ values (Table 4). Agonist structures are shown in Fig. 1 E. (B) Logarithmic plot of 1/K_d (resting affinity) versus E₂ (efficacy). Agonists that open the channel more effectively (have higher E₂ values) also bind to resting AChRs with higher affinity (higher 1/K_d values). Slope = 0.52 ± 0.03, intercept = −3.02 ± 0.03. (C) On a log–log scale, the LA association rate constant (k_on) is closely correlated with the equilibrium constant for HA binding (1/J_d).