Table 1.

Receptor	KD [3H] ZM241385 (nM)/logKD	KD [3H] NECA 0 mM NaCl (nM)/logKD	KD [3H] NECA 150 mM NaCl (nM)/logKD	KD [3H] CGS21680 (nM)	Ki UK432097 (nM)	EC50 UK432097 (nM)
A2AAR (WT)	7.69 nM −8.11 ± 0.06	23.4 nM −7.63 ± 0.11	290 nM −6.5 ± 0.14	13.6 ± 3.1 nM	17.3 ± 5.9 nM	0.45 ± 0.08 nM
A2AAR–D52N	9.63 nM −8.02 ± 0.05	9.16 nM −8.03 ± 0.10	10.4 nM −7.98 ± 0.11	7.35 ± 0.30 nM	22.4 ± 2.5 nM	No Signaling
A2AAR–S91A	7.0 ± 0.2 nM*	132 nM −6.88 ± 0.08	138 nM −6.86 ± 0.07	17.3 ± 6.12 nM	14.7 ± 0.7 nM	0.75 ± 0.09 nM
A2AAR–D52N–T4L	ND	ND	ND	12.0 ± 3.6 nM	25.2 ± 3.5 nM	ND
A2AAR–S91A–T4L	ND	ND	ND	10.0 ± 4.9 nM	20.0 ± 3.7 nM	ND

Radioligand binding and G protein signaling effects of A_2AAR variants. ZM241385 and NECA K_D measurements were done via homologous competition, and CGS21680 K_D measurement was done using saturation binding. K_D, K_i, and EC₅₀ values were calculated in Prism 7.0 software (GraphPAD, San Diego, CA) and data is displayed as means ± S.D. and 3 experiments were conducted in triplicate. Error is shown for either nM or logK_D depending on assay method as detailed in the methods section.

^*Denotes data previously published¹¹.

ND – not determined.