TABLE 4

Estimates of EC50, Emax, Hill slope, Kobs, and τobs for the simulated data in Fig. 4, a to c In this example, the allosteric modulator causes 10-fold increase in affinity (α = 0.1) and a 10-fold reduction in intrinsic efficacy (β = 0.1) of the agonist-receptor complex.

Allosteric Modulator
EC50
Emax
Hill Slope
Kobs
τobs
EmaxEC50′a
τobsKobs′a
Emax′EC50
 τobs′Kobs
M μM % μM RA
τ = 1
   0 5.00 50 1.0 10.0 1.00 1.00 1.00
   10–6 3.55 35.5 1.0 5.50 0.550 1.00 1.00
   10–5 1.54 15.4 1.0 1.82 0.182 1.00 1.00
   10–4 0.98 9.82 1.0 1.09 0.109 1.00 1.00
   10–3 0.92 9.17 1.0 1.01 0.101 1.00 1.00
τ = 10
   0 0.908 90.9 1.0 10.0 10.0 1.00 1.00
   10–6 0.847 84.6 1.0 5.50 5.50 1.00 1.00
   10–5 0.646 64.5 1.0 1.82 1.82 1.00 1.00
   10–4 0.521 52.1 1.0 1.09 1.09 1.00 1.00
   10–3 0.502 50.2 1.0 1.01 1.01 1.00 1.00
τ = 100
   0 0.0991 99.0 1.0 1.00 1.00
   10–6 0.098 98.2 1.0 1.00 1.00
   10–5 0.095 94.8 1.0 1.00 1.00
   10–4 0.092 91.6 1.0 1.00 1.00
   10–3
0.091
91.0
1.0
1.00
1.00

  • ↵ a EC50′, Emax′, Kobs′, and τobs′ denote the corresponding parameter values of EC50, Emax, Kobs, and τobs in the absence of allosteric modulator