Comparisons of in vitro Kd with in vivo potency EC50 properties
The EC50 values are calculated by means of eq. 2 based on the original model parameters given in (Betts et al., 2010).
Parameter | Rat | Monkey | Man |
---|---|---|---|
koff (d−1) | 1.72 | 16.2 | 0.1728 |
kon (nM−1 d−1) | 49.4 | 316 | 112 |
Kd (nM) | 0.0348 | 0.0513 | 0.00154 |
EC50 (nM) | 2.22 | 3.39 | 0.29 |
EC50 to Kd ratio | 64 | 66 | 188 |