Table 1. Binding Kinetics and Affinity Estimates of Ligands at the D2R WTa.
receptor | ligand | koff (s–1) | kon (s–1 × M–1) | pKd | pKi |
---|---|---|---|---|---|
D2R WT | SWR-1-8 | 0.017 ± 0.002 (5) | 3.4 ± 0.4 × 105 (3–6) | 7.30 ± 0.04 | 8.01 ± 0.18 (3) |
D2R WT | SV-III-130 | 0.007 ± 0.001 (11) | 8.6 ± 0.5 × 105 (3–6) | 8.09 ± 0.04 | 8.57 ± 0.05 (3) |
D2R WT | SWR-1-14 | 0.021 ± 0.002 (4) | 3.0 ± 0.4 × 105 (4–7) | 7.15 ± 0.04 | 7.70 ± 0.13 (3) |
koff values were calculated from response recovery t1/2 as koff = ln (2)/t1/2. See the Methods section for derivation of kon. pKd was calculated from the koff and kon estimates as Kd = koff/kon, while pKi was calculated from the IC50 for GIRK channel inhibition using the Cheng–Prusoff equation,25 assuming a Kd of DA equaling its EC50 for GIRK activation in our assay; i.e., 33 nM. The number of oocytes is shown in parentheses; for kon, this corresponds to the number of oocytes for each data point (see Figure 1G). Data shown are means ± SEM.