NPS R568 | |||
---|---|---|---|
pKB (95% CI) | Logαβ (95% CI) (αβ) | n | |
WT | 5.99 ± 0.05 (5.89–6.09) | 0.55 ± 0.01 (0.52–0.58) (3.5) | 17 |
F6121.39A | 6.39 ± 0.15 (6.03–6.75) | 0.35 ± 0.04a (0.28–0.43) (2.2) | 4 |
A6151.42V | 6.22 ± 0.13 (5.93–6.49) | 0.45 ± 0.04 (0.38–0.53) (2.8) | 6 |
F6682.56A | <5 | ND | 4 |
G670ECL1A | 6.39 ± 0.08 (6.23–6.55) | 0.09 ± 0.04a (−0.07–0.25) (1.2) | 4 |
F6843.36A | 5.28 ± 0.18a (4.79–5.63) | 0.35 ± 0.05a (0.28–0.51) (2.2) | 4 |
F6883.40A | 5.40 ± 0.16a (5.00–5.73) | 0.52 ± 0.05 (0.44–0.65) (3.3) | 5 |
E767ECL2A | 6.36 ± 0.22 (5.93–6.77) | 0.25 ± 0.03a (0.18–0.33) (1.8) | 3 |
A7725.39V | 6.33 ± 0.08 (6.17–6.48) | 0.38 ± 0.02a (0.35–0.42) (2.4) | 4 |
F7755.42A | 6.11 ± 0.07 (5.95–6.27) | 0.39 ± 0.02a (0.36–0.42) (2.5) | 4 |
L7765.43A | 6.40 ± 0.09 (6.20–6.58) | 0.46 ± 0.03 (0.40–0.51) (2.9) | 4 |
V8176.49A | 5.89 ± 0.26 (5.29–6.38) | 0.37 ± 0.05a (0.27–0.50) (2.3) | 4 |
W8186.50A | 5.88 ± 0.05 (5.77–5.98) | 0.55 ± 0.01 (0.52–0.58) (3.5) | 5 |
F8216.53A | 7.14 ± 0.18a (6.80–7.58) | 0.18 ± 0.02a (0.14–0.22) (1.5) | 4 |
Y8256.57A | 6.88 ± 0.11a,b (6.65–7.11) | 0.07 ± 0.02a,c (0.04–0.10) (1.2) | 4 |
K831ECL3A | 5.60 ± 0.15 (5.26–5.91) | 0.60 ± 0.05 (0.49–0.71) (4.0) | 4 |
V833ECL3A | 6.07 ± 0.11 (5.77–6.33) | 0.35 ± 0.02a (0.31–0.40) (2.2) | 4 |
E8377.32D | 7.13 ± 0.16a (6.85–7.52) | 0.26 ± 0.03a (0.22–0.32) (1.9) | 4 |
E8377.32I | <5 | ND | 7 |
A8407.35V | 6.31 ± 0.13 (6.05–6.56) | 0.33 ± 0.03a (0.28–0.39) (2.1) | 4 |
I8417.36A | NA | NA | 4 |
A8447.39V | 6.69 ± 0.09a (6.49–6.90) | 0.05 ± 0.09a (−0.17–0.26) (1.1) | 5 |
L8487.43A | 6.04 ± 0.13 (5.79–6.28) | 0.29 ± 0.02a (0.25–0.32) (1.9) | 4 |
CI, confidence interval; NA, negligible PAM activity; ND, not determined due to weak cooperativity or low affinity.
↵a significantly different to WT (P < 0.05, one-way ANOVA with Dunnett’s multiple comparisons post-test).
↵b pKB determined in interaction studies between AC265347 and NPS R568 (n = 3).
↵c pKB was fixed to 6.88 determined in interaction studies between AC265347 and NPS R568.