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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 2. — Rate constants for binding to resting receptors. (A) LA association (k_on) and dissociation (k_off) rate constants for seven different agonists. k_on varies by ∼77-fold even though all agonists have approximately the same diffusion constant. (B) k_on and k_off for AChRs having a mutation of binding site residue GlyB2 (αG153) activated by nicotine (see Fig. 3). (C) k_on and k_off for AChRs having a mutation of binding site residue TrpD (εW55) activated by ACh (Bafna et al., 2009). (D) Rate–equilibrium plot for LA agonist binding. The slope, Φ^bind = 0.93 ± 0.04, indicates that at the binding TS, the agonist is boundlike in energy.