TABLE 2.
HTRF whole cell binding affinities of NAPS and R-22 at chimera and mutant constructs
Statistical significance was determined by one-way analysis of variance with the Bonferroni post hoc test. None of the mutations significantly altered the pKi values for NAPS (P > 0.1).
| Construct | NAPS |
R-22 |
||||||
|---|---|---|---|---|---|---|---|---|
| pKi | S.E.M. | Fold Affinity Increasea | Fold Affinity Decreaseb | pKi | S.E.M. | Fold Affinity Increasea | Fold Affinity Decreaseb | |
| D3R | 9.21 | 0.14 | 1.2 | 1.0 | 8.37 | 0.13 | 48.0 | 1.0 |
| D3R(Δ94G) | 9.41 | 0.19 | 0.6 | 6.99c | 0.23 | 24.1 | ||
| D2R_D3R(EL1) | 9.60 | 0.15 | 2.9 | 7.78d | 0.02 | 12.4 | ||
| D2R_D3R(EL2) | 9.21 | 0.12 | 1.2 | 6.41d | 0.04 | 0.5 | ||
| D2R_D3R(EL1_EL2) | 9.44 | 0.08 | 2.0 | 8.10e | 0.02 | 25.9 | ||
| D2R_D3R(NT-TM1-IL1) | 9.51 | 0.10 | 2.4 | 6.62c | 0.01 | 0.9 | ||
| D2R_D3R(NT-TM1-IL1_EL1) | 9.47 | 0.15 | 2.2 | 7.83d | 0.05 | 13.7 | ||
| D2R_D3R(NT-TM1-IL1_EL2) | 9.28 | 0.08 | 1.4 | 6.57c | 0.03 | 0.8 | ||
| D2R_D3R(NT-TM1-IL1_EL1_EL2) | 9.04 | 0.08 | 0.8 | 7.89e | 0.01 | 15.9 | ||
| D2R(98-99GGV) | 9.57 | 0.18 | 2.8 | 7.76d | 0.00 | 11.7 | ||
| D2R(98-99GGE) | 9.56 | 0.13 | 2.7 | 7.89e | 0.03 | 15.9 | ||
| D2R(E99V) | 9.53 | 0.11 | 2.5 | 6.33d | 0.02 | 0.4 | ||
| D2R(E181V) | 9.49 | 0.17 | 2.3 | 6.28d | 0.02 | 0.4 | ||
| D2R | 9.13 | 0.24 | 1.0 | 1.2 | 6.69 | 0.08 | 1.0 | 48.0 |
a
Relative to D2R wild-type.
b
Relative to D3R wild-type.
c
pKi is significantly different from that at D3R (P < 0.001) but not at D2R (P > 0.1).
d
pKi is significantly different from that at D2R (P < 0.001) but also at D3R (P < 0.05).
e
pKi is significantly different from that at D2R (P < 0.001) but not at D3R (P > 0.1).