Table 4.

Affinity of selected hits from the LOPAC library at the A₃AR, A₁AR, and β₂AR: Compounds were tested on CHO cells expressing the A₃AR, A₁AR, and β₂AR in the HTS format fluorescent ligand binding assay using 25 nM CA200645 as the tracer for A₃AR and A₁AR and 10 nM of BODIPY-TMR-CGP for β₂AR.

Position in primary screen	Compound	A3AR	A1AR	β2AR
		pKi	pKi	% Total binding at 10 μM
2	SU 6656	6.17 ± 0.08	ND	128.4 ± 18.4
5	K114	6.43 ± 0.04	6.56 ± 0.11	95.8 ± 5.5
8	Retinoic acid p-hydroxyanilide	6.13 ± 0.18	6.04 ± 0.21	102.7 ± 5.1
9	CGS 15943	7.24 ± 0.14	8.14 ± 0.09	115.4 ± 5.0

Data represents mean ± SEM from three experiments performed in triplicate. ND, Not determined as accurate curve could not be generated.