Table 1 NanoBRET XAC-630 saturation binding parameters (specific binding)

From: Molecular basis of ligand binding and receptor activation at the human A3 adenosine receptor

A3 adenosine receptor

pKd (n)

P valuea

Bmax as% WT

P valuea

WT

7.2 ± 0.1 (6)

–

99.3 ± 0.7

–

Y15A1.35

6.8 ± 0.1 (5)

0.0347

28.8 ± 5.7

<0.0001

S73A2.65

6.9 ± 0.1 (3)

0.2205

85.7 ± 5.8

0.8987

T94A3.36

7.0 ± 0.04 (3)

0.6910

37.5 ± 2.4

0.0003

H95A3.37

6.6 ± 0.07 (4)

0.0006

34.7 ± 13.4

<0.0001

H95F3.37

6.4 ± 0.2 (3)

0.0001

34.3 ± 3.0

0.0001

V169E45.53

6.9 ± 0.01 (3)

0.3234

83.5 ± 2.2

0.8027

M174A5.35

6.7 ± 0.04 (5)

0.0040

54.0 ± 16.5

0.0020

N250A6.55

N.D. (3)

–

N.D.

–

Y265A7.36

7.4 ± 0.03 (3)

0.8202

102.0 ± 6.2

>0.9999

S271A7.42

7.6 ± 0.1 (3)

0.0799

90.6 ± 1.7

0.9925

H272A7.43

N.D. (3)

–

N.D.

–

  1. pKd values represent the mean ± SEM of the negative logarithm of the equilibrium dissociation constant from (n) experiments performed in duplicate.
  2. ND not determined due to no measurable specific binding. Bmax values were normalised to WT for each experiment.
  3. aSignificant differences vs WT were determined by one-way ANOVA (Prism 10.3.1) with a Dunnett’s multiple comparison post hoc test (P < 0.05).
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