Table 1. Association Rates, Dissociation Rates, and Dissociation t1/2 Values of Clozapine and ML321 Binding to the D2Ra.
koff (min–1) | kon(M–1 min–1) | t1/2 (min) | Kd (nM) | |
---|---|---|---|---|
clozapine | 1.6 ± 0.23 | 4.6 ± 0.7 × 107 | 0.47 ± 0.06 | 34.8 ± 0.06 |
ML321 | 1.3 ± 0.22 | 2.3 ± 0.4 × 107 | 0.60 ± 0.07 | 56.5 ± 0.23 |
Time-resolved fluorescence resonance energy transfer assays were used to measure association (kon) and dissociation (koff) rates and dissociation t1/2 values as described in the Methods. Data are the means ± SEM of five (clozapine) or six (ML321) independent experiments performed in triplicate.